new products - resources.tocris.com · require the assistance of coenzymes or cofactors in order to...

New Products

Ginkgo FlowersGinkgo BilobaA Source of Ginkgolic Acid

Products by Pharmacology• 7-TM Receptors• Enzymes• Nuclear Receptors

Products for Cell Biology• Epigenetics• Aptamers• Fluorescent Imaging

Spring and Summer 2018

New Products by Pharmacology

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7-TM Receptors7-TM receptors are integral membrane proteins containing seven membrane-spanning helices that are coupled to G proteins on the intracellular face of the membrane. Upon ligand binding, the receptor undergoes a conformational change, activating the G protein and triggering signal transduction.

New Products – Spring and Summer 2018Welcome to our New Product Guide, containing the latest additions to our product range over the last six months. Products are categorized by biological targets for easy identification, or simply browse the guide to see what is newly available. Our products are of the highest purity and full respect for third party intellectual property rights comes as standard.

7-TM Receptors

–

Cl

NH

N

N+ CH3O

N

Clozapine N-oxide dihydrochloride (6329)Activator of muscarinc DREADDs

Glp-Arg-Arg-Cys-Met-Pro-Leu-His-Ser-Arg-Val-Pro-Phe-Pro

ELA-14 (Human) (6293)Potent apelin (APJ) receptor agonist

Gln-Arg-Pro-Val-Asn-Leu-Thr-Met-Arg-Arg-

Lys-Leu-Arg-Lys-His-Asn-Cys-Leu-Gln-Arg-

Arg-Cys-Met-Pro-Leu-His-Ser-Arg-Val-Pro-

Phe-Pro

ELA-32 (Human) (6291)Potent, high affinity apelin (APJ) receptor agonist;

stimulates angiogenesis

N

O

N

O

ON

ER 819762 (5924)Potent EP4 receptor antagonist; orally bioavailable

F

NN

S OO

N

O

N

O

LEI 101 (5826)Potent and selective CB2 partial agonist;

orally biovailable

OO

HN

O

HN

Cl

Cl

AR 420626 (6163)FFA3 agonist

Leu-Glu-Asn-Pro-Ser-Pro-Gln-Ala-Pro-Ala-Arg-Arg-Leu-Leu-Pro-Pro

BigLEN (Mouse) (6304)GPR171 agonist

O

NH

OHO

OH

O

MS 15203 (6299)Potent and selective GPR171 partial agonist

Featured 7-TM Receptor Products

5-HT1 Receptors

Agonists 6202 Vilazodone Potent 5-HT1A partial agonist and SSRI; antidepressant 10 mg

50 mg

5-HT2 Receptors

Antagonists 6336 Trazodone 5-HT2A and α1 adrenoceptor antagonist; also enhances neural differentiation; antidepressant and neuroprotectant

50 mg

Adrenergic β2 Receptors

Agonists 6219 Arformoterol Long-acting β2 agonist (LABA) 10 mg

50 mg

Calcium-Sensing Receptor

Modulators 6165 AC 265347 CaSR biased allosteric modulator 10 mg

50 mg

Category Cat. No. Product Name Description Unit Size

NEW PRODUCTS – SPRING AND SUMMER 2018

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7TM Receptors (PEN, SNAP, TASP)

Ala-Ala-Asp-His-Asp-Val-Gly-Ser-Glu-Leu-Pro-Pro-Glu-Gly-Val-Leu-Gly-Ala-Leu-Leu-Arg-Val

PEN (Human) (6307)GPR83 agonist

Ser-Val-Asp-Gln-Asp-Leu-Gly-Pro-Glu-Val-Pro-Pro-Glu-Asn-Val-Leu-Gly-Ala-Leu-Leu-Arg-Val

PEN (mouse) (6308)GPR83 agonist

Ala-Val-Asp-Gln-Asp-Leu-Gly-Pro-Glu-Val-Pro-Pro-Glu-Asn-Val-Leu-Gly-Ala-Leu-Leu-Arg-Val

PEN (rat) (6309)GPR83 agonist

N

N

O

O

N

CF3

SNAP 398299 (5426)Potent and selective GAL3 antagonist

N

N

N

NH

OO

ON

O

F

Cl

TASP 0390325 (5729)Potent and selective V1B receptor antagonist;

orally bioavailable

Featured 7-TM Receptor Products (continued)

CB1 Receptors

Antagonists 6193 AM 4113 Selective, high affinity CB1 antagonist 10 mg

50 mg

CB2 Receptors

Agonists 5826 LEI 101 Potent and selective CB2 partial agonist; orally biovailable 10 mg

Estrogen (GPER) Receptor

Antagonists 6116 BHPI ERα antagonist; also activates unfolded protein response; active in vivo

10 mg

50 mg

Free Fatty Acid Receptors

Agonists 6163 AR 420626 FFA3 agonist 5 mg

25 mg

Glutamate (Metabotropic) Receptors

Other 6329 Clozapine N-oxide dihydrochloride Activator of muscarinic DREADDs; water soluble 10 mg

50 mg

GPR171

Agonists 6304 BigLEN (mouse) GPR171 agonist 1 mg

6306 BigLEN (rat) Potent GPR171 agonist 1 mg

6299 MS 15203 Potent and selective GPR171 partial agonist 5 mg

25 mg

Antagonists 6298 MS 21570 GPR171 antagonist 10 mg

50 mg

Orphan 7-TM Receptors

Agonists 6277 7α,25-Dihydroxycholesterol Highly potent GPR183 (EBI2) agonist 10 mg

6307 PEN (human) GPR83 agonist 1 mg

6308 PEN (mouse) GPR83 agonist 1 mg

6309 PEN (rat) GPR83 agonist 1 mg

Peptide Receptors

Agonists 6264 Caerulein CCK agonist 1 mg

6293 ELA-14 (human) Potent apelin (APJ) receptor agonist 1 mg

6291 ELA-32 (human) Potent, high affinity apelin receptor agonist; stimulates angiogenesis 100 µg

6303 Parathyroid hormone (1-34) (bovine) Parathyroid hormone (PTH) receptor agonist 1 mg

6301 Parathyroid hormone (1-34) (rat) Parathyroid hormone (PTH) receptor agonist 1 mg

6288 Peptide YY (3-36) human NPY Y2 receptor agonist 500 µg



4 |

New Compound Libraries

Tocris has launched a range of new compound libraries composed of biologically active molecules that have proven pharmacological activity against a wide range of targets. Use them in your phenotypic screening studies, drug repurposing campaigns or for validation of new molecular targets. Compounds are supplied pre-dissolved in DMSO, and full chemical and biological data are available. All compounds have the same proven solubility, purity and stability as all those in the Tocris catalog.

Tocriscreen Plus (Cat. No. 5840)A unique library of 1280 biologically active compounds, with many exclusive to Tocris (250 mL 10 mM DMSO solutions)

Tocriscreen Library of FDA Approved Compounds (Cat. No. 5932)A library of 160 FDA-approved compounds (250 mL 10 mM DMSO solutions)

Tocris also has available single plate Toolboxes for Kinase Inhibitors, Stem Cells and Epigenetics

For more information visit www.tocris.com/tocriscreen

7-TM Receptors – continued


Antagonists 6332 Atosiban Potent oxytocin receptor antagonist 10 mg

5426 SNAP 398299 Potent and selective GAL3 antagonist 5 mg

5729 TASP 0390325 Potent and selective V1B receptor antagonist; orally bioavailable 10 mg

50 mg

Inverse Agonists 6347 PF 04628935 Potent ghrelin receptor inverse agonist 5 mg

25 mg

6350 PF 05190457 High affinity and selective ghrelin receptor inverse agonist 5 mg

25 mg

Other 6294 ELA-14 negative control Negative control for ELA-14 (Cat.No. 6293) 1 mg

6292 ELARR>GG Negative control for ELA-32 (Cat.No. 6291) 100 µg

6190 Retrobradykinin Reverse analog of Bradykinin 1 mg

Prostanoid Receptors

Antagonists 6240 DG 041 Potent and selective EP3 antagonist; antiplatelet and antithrombotic 10 mg

50 mg

5924 ER 819762 Potent EP4 receptor antagonist; orally bioavailable 5 mg

Purinergic P2Y Receptors

Antagonists 6078 BPTU P2Y1 allosteric antagonist 10 mg

50 mg

6317 Prasugrel Irreversible P2Y12 antagonist; antiplatelet and orally active 10 mg

50 mg

Smoothened Receptors

Agonists 6390 SAG dihydrochloride Dihydrochloride salt of SAG; Smo receptor agonist 1 mg


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EnzymesEnzymes are proteins that catalyze a chemical change in a substrate. Some enzymes act independently, but others require the assistance of coenzymes or cofactors in order to function correctly. Enzymes can be classified into numerous groups according to their substrate or the type of chemical reaction they catalyze.

Enzyme products

N

N

NH

O

OH OH

N

N

OPP

ONaOH

OO

NaO

PSB 12379 (6083)Ecto-5’-nucleotidase (CD73) inhibitor

NBr

F

Br

O

(R)-CE3F4 (5969)Epac inhibitor

Cl

O

O

ClCl

Cl

ST 034307 (6271)Adenylyl cyclase 1 (AC1) inhibitor

HO

NH

OO

OO

B I09 (6009)IRE1 endonuclease inhibitor

O

O NS

NN

N

Lalistat 2 (6099)Selective lysosomal acid lipase inhibitor

O

N

O

NH

NN

N

F3C

PF 04457845 (6374)Potent and selective irreversible FAAH inhibitor

Cl

Cl

N

N

N

O

NH

O

OMe

O

Nutlin 3a (6075)MDM2 antagonist; active enantiomer of

Nutlin-3 (Cat.No. 3984)

NH2O

N ONH

O

O

Pomalidomide (6302)Cereblon ubiquitination inhibitor

Featured Enzyme Products

ATPases/GTPases

Inhibitors 6248 EHop 016 Rac inhibitor 5 mg

25 mg

6407 Fendiline K-Ras inhibitor; inhibits K-Ras localization to the plasma membrane 10 mg

50 mg

6180 NMS 873 Potent and selective p97 ATPase (VCP) allosteric inhibitor 10 mg

50 mg

6083 PSB 12379 Ecto-5ʹ-nucleotidase (CD73) inhibitor 10 mg

5969 (R)-CE3F4 Epac inhibitor 10 mg

Cyclases

Inhibitors 6271 ST 034307 Adenylyl cyclase 1 (AC1) inhibitor; analgesic and active in vivo 10 mg

50 mg

Dehydrogenases

Inhibitors 6084 ASP 9521 Potent 17β-hydroxysteroid dehydrogenase type 5 inhibitor; orally bioavailable

10 mg

50 mg

6196 Brequinar sodium Potent and selective DHODH inhibitor 10 mg

50 mg

Esterases

Inhibitors 6009 B I09 IRE1 endonuclease inhibitor; cell permeable 10 mg

50 mg



6 |

Hydrolases

Inhibitors 5865 KLH 45 Potent DDHD2 inhibitor 10 mg

50 mg

6098 Lalistat 1 Potent and selective lysosomal acid lipase (LAL) inhibitor 10 mg

50 mg

6099 Lalistat 2 Selective lysosomal acid lipase inhibitor 10 mg

50 mg

5956 NF 1819 Potent and selective irreversible MAGL inhibitor; membrane permeable and brain penetrant

10 mg

6370 Nor NOHA Arginase inhibitor 10 mg

6374 PF 04457845 Potent and selective irreversible FAAH inhibitor 5 mg

25 mg

5334 TH 588 Potent MTH1 inhibitor 5 mg

25 mg

Kinases

Activators 6049 PF 04937319 Glucokinase partial activator 5 mg

25 mg

6345 PF 04991532 Potent hepatoselective glucokinase activator 5 mg

25 mg

5343 TPPB High affinity PKC activator; also APP modulator 1 mg

Inhibitors 5675 AZ PFKFB3 26 Potent and selective PFKFB3 inhibitor 10 mg

50 mg

5123 BMX-IN-1 Potent and selective BMX inhibitor 5 mg

6258 CC 401 High affinity JNK inhibitor; also inhibits HCMV replication 10 mg

50 mg

5922 CRT 0066854 PKCι and PKCζ inhibitor 10 mg

50 mg

6174 CVT 313 cdk2 inhibitor 10 mg

50 mg

6188 Everolimus mTOR inhibitor; immunosuppressant 10 mg

6051 G 5555 High affinity group 1 PAK inhibitor 10 mg

50 mg

5768 HS 38 ATP-competitive inhibitor of DAPK and ZIPK 5 mg

4322 JH 295 Irreversible Nek2 inhibitor 1 mg

2 mg

6289 JH-II-127 Potent and selective LRRK2 inhibitor 10 mg

50 mg

5700 ML 315 Inhibitor of Clk and DYRK kinases 10 mg

50 mg

5150 NCL 00017509 Potent and reversible NIMA related kinase 2 (Nek2) inhibitor 1 mg

5818 NVP BSK 805 Potent JAK2 inhibitor; orally bioavailable 10 mg

50 mg

6132 NVS PAK1 1 Potent and selective PAK1 inhibitor 5 mg

25 mg

6012 OXSI 2 Potent Syk kinase inhibitor; also inhibits assembly of NLRP3 inflammasomes

10 mg

50 mg

6073 P21d Potent and selective Brk inhibitor 5 mg

6373 PF 06650833 Potent and selective IRAK4 inhibitor 5 mg

6346 PF 5006739 Potent CK1δ/ε inhibitor 5 mg

25 mg

6221 PKI (5-24) High affinity PKA inhibitor 1 mg

5452 SKI 178 Non-lipid sphingosine kinase 1 (SphK1) inhibitor 10 mg

50 mg

6036 STK16-IN-1 Serine/threonine protein kinase 16 (STK16) inhibitor; also inhibits PI 3Kδ, PI 3Kγ and mTOR kinases.

10 mg



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Featured Kinase products

OHN

O

N

N

O

N

N

N

O

PF 04937319 (6049)Glucokinase partial activator

N

NH

O

F3C OH

NH

O

TPPB (5343)High affinity PKC activator; also APP modulator

N

O

N

HN

NN

HN

CC 401 (6258)High affinity JNK inhibitor;

also inhibits HCMV replication

HN

N

O N

ONH2

O

N

ClN

G 5555 (6051)High affinity group 1 PAK inhibitor

N

NH

O

S

O

NH2N

N

Cl

HS 38 (5768)ATP-competitive inhibitor of DAPK and ZIPK

NH

O

NH

N

HN

O

JH 295 (4322)Irreversible Nek2 inhibitor

N

N NH

N

NH

O

H2N

NCL 00017509 (5150)Potent and reversible Nek2 inhibitor

N

NH

S

H2N

OO

O

OXSI 2 (6012)Potent Syk kinase inhibitor

F

HN

N

N

N

NHN

O

N

O

P21d (6073)Potent and selective Brk inhibitor

O

NO

H2N

O

HN

O F

PF 06650833 (6373)Potent and selective IRAK4 inhibitor

MeO

NHNHN

O

N

OMe

OMe

SKI 178 (5452)Non-lipid sphingosine kinase 1 (SphK1) inhibitor

Featured Enzyme Products (continued)

Enzymes – continued

6125 TC JL 37 Potent TYK2 inhibitor 10 mg

50 mg

6061 XMD 8-87 Potent Ack1/TNK2 inhibitor 10 mg

50 mg

Other 6286 st-Ht31 Inhibits PKA/AKAP interactions; cell permeable 1 mg

6287 st-Ht31 P Negative control for st-Ht31 (Cat.No. 6286) 1 mg

Ligases

Inhibitors 6326 Ginkgolic acid Inhibits SUMOylation by binding E1 10 mg

50 mg

6075 Nutlin 3a MDM2 antagonist; active enantiomer of Nutlin-3 (Cat.No. 3984) 5 mg

25 mg



8 |

Enzymes - 2

O

HN

O

N

OH

OHN

N S

NC

VH 298 (6156)High-affinity inhibitor of VHL

N

NH2

NN

N

NN

S

ON

PF 04671536 (6024)Potent and selective PDE8B/8A inhibitor

ONH

O

N

O

NaN S

O

NaO

O

T 26c disodium salt (6134)Highly potent and selective MMP13 inhibitor

HONH

HN

NH

NH2

O

O

O

O

TAPI 0 (5523)ADAM-17 (TACE) and MMP inhibitor

P

S

Au OMe

D9 (5921)Potent thioredoxin reductase (TrxR) inhibitor

H

H

H

HNO

H

MK 386 (5842)Potent, selective human type 1

5α-reductase inhibitor

N NH

N N

NCl

NN

O

PF 06424439 (6348)Potent and selective DGAT2 inhibitor

O

N

N

OH

O

SPT Imidazopyridine 1 (6055)Potent serine palmitoyl transferase inhibitor

Featured Enzyme Products (continued)


6302 Pomalidomide Cereblon ubiquitination inhibitor; also TNF-α inhibitor and antiangiogenic

10 mg

50 mg

6156 VH 298 High-affinity inhibitor of VHL 10 mg

50 mg

Other 6305 Lenalidomide Cereblon binder; induces ubiquitination and degradation of CK1α by E3 ubiquitin ligase

100 mg

Oxygenases/Oxidases

Inhibitors 6119 OB 24 Potent and selective heme oxygenase 1 (HO-1) inhibitor 10 mg

50 mg

Phosphodiesterases

Inhibitors 6035 (S)-C33 Potent PDE9 inhibitor 10 mg

50 mg

6024 PF 04671536 Potent and selective PDE8B/8A inhibitor 5 mg

25 mg

6405 PF 05180999 Potent and selective PDE2A inhibitor 5 mg

25 mg

Polymerases

Inhibitors 6234 Entecavir Potent and selective hepatitis B virus inhibitor 10 mg

50 mg


tocris.com | 9

Enzymes – continued


Proteases

Inhibitors 5706 BAY 678 Potent and selective cell-permeable human neutrophil elastase (HNE) inhibitor

5 mg

25 mg

6172 INF 4E Caspase-1 and NLRP3 inflammasome inhibitor 10 mg

6423 Pep 2-8 Potent PCSK9 inhibitor 1 mg

6333 Phosphoramidon Neutral endopeptidase and endothelin converting enzyme inhibitor 5 mg

6414 Rupintrivir Potent and selective irreversible human rhinovirus 3C protease inhibitor

5 mg

6187 SK 216 Plasminogen activator inhibitor-1 (PAI-1) inhibitor 10 mg

50 mg

6134 T 26c Highly potent and selective MMP13 inhibitor 5 mg

25 mg

5523 TAPI 0 ADAM-17 (TACE) and MMP inhibitor 1 mg



6194 TM 5441 Plasminogen activator inhibitor-1 (PAI-1) inhibitor 10 mg

50 mg

Other 6389 BAY 677 Inactive control for BAY 678 (Cat.No. 5706) 5 mg

25 mg

Reductases

Inhibitors 5921 D9 Potent thioredoxin reductase (TrxR) inhibitor 10 mg

50 mg

5842 MK 386 Potent, selective human type 1 5α-reductase inhibitor 1 mg

6189 Myricetin Irreversible TrxR inhibitor 10 mg

50 mg

6185 Pemetrexed High affinity dihydrofolate reductase inhibitor; also inhibits thymidylate synthase, GARFT and AICART

50 mg

6343 Rosuvastatin calcium Potent HMG-CoA reductase inhibitor 10 mg 50 mg

Synthases/Synthetases

Inhibitors 1993 Halofuginone High affinity competitive proyly-tRNA synthetase inhibitor 50 mg

Transferases

Inhibitors 6265 Lonafarnib Potent farnesyl transferase inhibitor 10 mg

50 mg

5863 PF 04620110 Potent and selective DGAT-1 inhibitor; orally bioavailable 5 mg

25 mg

6348 PF 06424439 Potent and selective DGAT2 inhibitor 5 mg

6055 SPT Imidazopyridine 1 Potent serine palmitoyl transferase inhibitor 10 mg

50 mg


10 |

Enzyme-Linked ReceptorsEnzyme-linked receptors are a group of multi-subunit transmembrane proteins that contain either intrinsic enzyme activity on their intracellular domain, or associate directly with an intracellular enzyme. Upon ligand binding, a conform-ational change is transmitted via a transmembrane helix. This activates the enzyme, initiating signaling cascades.

Featured Enzyme-Linked Receptor Products

OH

O

HN O

NS

O

O

N

N

N

NH

S

O+ NN

OO

-O3S

.CH3CO2H

OO

N

R-BC154 (6048)High affinity fluorescent α4β1/α9β1

inhibitor; mobilizes HSCs

N NH

NN

N

N

LDN 212854 (6151)Potent bone morphogenetic protein

type I (ALK) inhibitor

N

NH2N

S

CL 075 (6142)TLR8 agonist

Featured Enzyme-Linked Receptor Products

Cytokine receptors

Agonists 5372 Bioymifi DR5 (TRAIL receptor) agonist; induces apoptosis 5 mg

Integrins

Inhibitors 6048 R-BC154 High affinity fluorescent α4β1/α9β1 inhibitor; mobilizes HSCs 1 mg

Receptor Serine/Threonine Kinases (RSTKs)

Inhibitors 6016 IN 1130 Potent and selective inhibitor of TGF-βRI 5 mg

6151 LDN 212854 Potent bone morphogenetic protein type I (ALK) inhibitor 10 mg

50 mg

6152 LDN 214117 Potent and selective ALK2 inhibitor 10 mg

50 mg

Receptor Tyrosine Kinases (RTKs)

Inhibitors 6069 BMS 605541 Potent ATP-competitive VEGFR-2 inhibitor 10 mg

50 mg

6231 Dacomitinib Potent irreversible pan ErbB inhibitor 10 mg

50 mg

Toll-like Receptors

Agonists 6142 CL 075 TLR8 agonist 5 mg

Antagonists 6191 TH 1020 TLR5/Flagellin complex antagonist 10 mg

50 mg

Inhibitors 5705 M62812 TLR4 inhibitor 10 mg

50 mg



tocris.com | 11

Ion Channels Ion channels are pore-forming membrane proteins that allow the passage of ions across the plasma membrane. Hundreds of different ion channels have been identified in the membranes of all mammalian cells; they can be broadly classified by different properties including the gating mechanism (e.g. voltage or ligand) or ion selectivity of their pore.

Featured Ion Channel Products

N

N

NH

N O

Cl

CMPI (5963)Potent positive allosteric modulator

of α4β2 nAChRs

O

NH

O

N N

O

PZ-II-029 (6192)α6β3γ2-selective GABAA

channel modulator

OCF3

ClHN

ONH

JNJ 55511118 (6278)Selective, high affinity negative modulator

of AMPA receptors containing TARP-γ8

N

N

O

NN

ClNO

N

AM 0902 (5914)Potent and selective TRPA1 antagonist

NH2

N

O

Cl

NC

SAR 7334 (5831)Potent TRPC6 inhibitor

Featured Ion Channels Products

Acetylcholine (Nicotinic) Receptors

Agonists 6140 NS 6784 α7 nAChR agonist 10 mg

50 mg

Modulators 5963 CMPI Potent positive allosteric modulator of α4β2 nAChRs; also inhibitor of (α4)2(β2)3, muscle-type and Torpedo nAChRs

10 mg

GABAA and GABAA-ρ Receptors

Modulators 6192 PZ-II-029 α6β3γ2-selective GABAA channel modulator 5 mg

25 mg

Glutamate (Ionotropic) Receptors

Modulators 6278 JNJ 55511118 Selective, high affinity negative modulator of AMPA receptors containing TARP-γ8

5 mg

25 mg

Other 6226 IC 87201 nNOS-PSD95 protein-protein interaction inhibitor; also antinociceptive and antidepressant

10 mg

50 mg

Voltage-Gated Potassium Channels

Blockers 6318 Azimilide Kv11.1 (hERG) channel blocker 10 mg

50 mg

Transient Receptor Potential Channels

Blockers 5914 AM 0902 Potent and selective TRPA1 antagonist 10 mg 50 mg

5831 SAR 7334 Potent TRPC6 inhibitor 5 mg



12 |

Nuclear Receptors Nuclear receptors (also known as nuclear hormone receptors) are a large family of transcription factors that bind directly to DNA to regulate the expression of target genes. They regulate the cellular response to hormones such as sex steroids, vitamin D3, adrenal steroids and other metabolic ligands, and are involved in metabolism, development and reproduction.

Tocriscreen Compound LibrariesTocriscreen compound libraries are composed of biologically active compounds that have proven pharmacological activity against GPCRs, ion channels, kinases, enzymes, nuclear receptors and transporters. Compounds are supplied pre-dissolved in DMSO, and full chemical and biological data are available. All compounds have the same proven solubility, purity and stability as all those in the Tocris catalog.

Highly potent and muscle-selective androgen receptor (AR) agonist

BMS 564929 Cat. No. 5274BMS 564929 is a highly potent and muscle selective androgen receptor (AR) agonist (EC50 = 0.44 nM). It is selective for ARs over estrogen, glucocorticoid and mineralocorticoid receptors. This compound is also selective for muscle ARs over prostate ARs. Active in vivo and orally bioavailable.

Featured Nuclear Receptor Products

NN

O

OHO H

Cl

CN

BMS 564929 (5274)Highly potent and muscle-selective

androgen receptor (AR) agonist

Androgen Receptor

Agonists 5274 BMS 564929 Highly potent and muscle-selective androgen receptor (AR) agonist 5 mg

Inhibitors 6161 Ailanthone Potent inhibitor of androgen receptor (AR) 5 mg

Estrogen and Related Receptors

Agonists 6158 (S)-Equol Potent estrogen receptor β (ERβ) agonist; dihydrotestosterone antagonist

10 mg

50 mg

Modulators 6342 Tamoxifen Estrogen receptor partial agonist/antagonist 100 mg

Glucocorticoid Receptors

Other 6357 Ciclesonide Glucocorticoid antiasthmatic prodrug 5 mg

25 mg

Other Nuclear Receptors

Activators 5821 C-DIM 12 Nurr1 activator; inhibits NF-κB-dependent gene expression 10 mg

50 mg

Agonists 6376 DIM-C-pPhOCH3 Nur77 agonist 5 mg

25 mg

Antagonists 6377 DIM-C-pPhOH Nur77 antagonist 5 mg

25 mg

Progesterone Receptor

Inhibitors 6285 Megestrol Synthetic progesterone analog 50 mg

Retinoid X Receptors

Agonists 5920 LG 100268 Potent and selective RXR agonist; also activates RXR/PPARγ heterodimers

5 mg

25 mg

Retinoic Acid-related Orphan Receptors

Inhibitors 5987 (+/-)-ML 209 RORγt inverse agonist; suppresses Th17 cell differentiation 10 mg

50 mg

Rev-Erb Receptors

Agonists 6038 SR 10067 Selective Rev-Erbα/β agonist; anxiolytic 10 mg

50 mg

Tocriscreen Toolboxes

Other 5933 Tocriscreen Kinase Inhibitor Toolbox I

A library of 80 kinase inhibitor compounds (250 μL 10 mM DMSO solutions)

1 Set

6268 Tocriscreen Kinase Inhibitor Toolbox I & II


1 Set

6225 Tocriscreen Kinase Inhibitor Toolbox II


1 Set




tocris.com | 13

TransportersTransporters are specialized membrane-spanning proteins that aid the movement of ions, peptides, small molecules, lipids and macromolecules across a lipid bilayer. There are three main classes of transporter: ABC transporters, P-type ATPases and the solute carrier family. Transporters can move substances either actively or passively.

Other Pharmacology

Featured Antiviral Products

HO

OH

OH

OO

HOH

O

O

H

O

OH

HO

O

ONa

O

Nanchangmycin (6183)Antiviral; active against Zika, West Nile

and dengue viruses

NH2

N

O

HO

OH

OHN

N

NITD 008 (6045)Antiviral; selective flavivirus inhibitor

Featured Other Pharmacology Products

Glucose Transporters

Inhibitors 6100 Fasentin GLUT1/GLUT4 inhibitor; also Fas-sensitizer 10 mg

50 mg

Ion Pumps/Transporters

Inhibitors 5658 AR-C 141990 MCT1 inhibitor 1 mg

6164 SEA 0400 Potent Na+/Ca2+ exchanger (NCX) inhibitor 10 mg

50 mg

Antibiotics

6442 Gentamicin Aminoglycoside antibiotic 5 mg

3637 Salinomycin Antibiotic; also selectively inhibits cancer stem cells 10 mg

Antivirals

5741 25-Hydroxycholesterol Antiviral; also α-crystallin (cryAB) chaperone 10 mg

6183 Nanchangmycin Antiviral; active against Zika, West Nile and dengue viruses 10 mg

6339 Netilmicin Inhibits HIV-1 replication; also semisynthetic aminoglycoside antibiotic

10 mg

6045 NITD 008 Antiviral; selective flavivirus inhibitor 1 mg



14 |

New Products for Cell Biology

ApoptosisApoptosis is a form of programmed cell death that involves caspase-dependent intracellular signaling, resulting in phagocytosis of unwanted cells. The cell cycle is a regulatory network that controls cell proliferation and detects DNA damage. In the event that DNA damage cannot be repaired, the cell is destroyed through apoptotic mechanisms.

AptamersAptamers are short, single-stranded DNA or RNA molecules that bind with high selectivity and affinity to a target of interest. They are highly versatile and are used as molecular tools in life science research, therapeutics or diagnostics.

Aptamers – New from TocrisEp23, 5 -́DY647 (#6102) is a high affinity, fluorescently tagged aptamer for epithelial cell adhesion molecule (EpCam), a transmembrane glycoprotein which mediates calcium dependent cell adhesion in epithelia. Ep23, 5 -́DY647 is efficiently internalized upon binding to EpCAM and exhibits rapid penetration of tumorspheres in vitro, as well as superior penetration, accumulation and retention in tumor xenografts in vivo compared to an antibody to the same target.

Key features of Aptamers• Short, single stranded DNA or RNA• High affinity for target• Unique 3D structure gives high target specificity• Readily modified by addition of a fluorophore or

photolabile group• Suitable for use in unfixed cell imaging, flow

cytometry and fixed tissue imaging• Sold under license from Deakin University (Australia)

Ep23, 5 -́DY647 in HT29 cells, applied at 100 nM concentration, magnification 40x. Image kindly provided by Birte Aggeler, Bio-Techne.

Apoptosis

Inhibitors 5733 ML 311 Inhibits Mcl-1-BIM interaction 10 mg

50 mg

Aptamers

6103 CD133-A15, 5ʹ-DY647 High affinity fluorescently tagged aptamer for CD133 (AC133 epitope) 50 µg

6104 CD133-B19, 5ʹ-DY647 High affinity fluorescently tagged aptamer for CD133 (extracellular domain epitope)

50 µg

6102 Ep23, 5ʹ-DY647 High affinity fluorescently tagged aptamer for EpCam 50 µg




tocris.com | 15

Cell Metabolism Cellular metabolism describes a set of chemical reactions that occur in living organisms in order to maintain life. Cellular metabolism involves complex sequences of controlled biochemical reactions, better known as metabolic pathways. These processes allow organisms to grow and reproduce, maintain their structures, and respond to environmental changes.

Cytoskeleton and Motor ProteinsThe cytoskeleton is a dynamic structure contained in the cytoplasm of both eukaryotic and prokaryotic cells. The cytoskeletal system has a role in cell division, cell motility, intracellular transport and organelle organization. Motor proteins are responsible for muscle contraction and the active transport of most protein within the cytoplasm.

ECM and Adhesion MoleculesThe extracellular matrix provides the physical microenvironment in which cells exist. It provides a substrate for cell anchorage, serves as a tissue scaffold, guides cell migration during embryonic development and wound repair, and has a key role in tissue morphogenesis. The extracellular matrix is also responsible for transmitting environmental signals to cells, ultimately affecting cell proliferation, differentiation and death.

Connexin43 mimetic peptide.

Peptide5 Cat. No. 639Peptide5 reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal injury, in vitro and in vivo. The product also exhibits analgesic effects in models of neuropathic pain.

Val-Asp-Cys-Phe-Leu-Ser-Arg-Pro-Thr-Glu-Lys-Thr

Featured ECM and Adhesion Molecule Products

Peptide 5 (6394)Connexin43 mimetic peptide. Peptide 5 reduces swelling,astrogliosis, neuroinflammation and neuronal cell death

following spinal injury, in vitro and in vivo. Also exhibits analgesiceffects in models of neuropathic pain.

DNA, RNA and Protein Synthesis

Inhibitors 6359 Nelarabine Purine nucleoside analog; inhibits DNA synthesis 10 mg

50 mg

6222 PFM 01 MRE11 endonuclease inhibitor 10 mg

50 mg

Caged Amino Acid Compounds

6121 NB-caged Tyrosine ortho-nitrobenzyl caged L-tyrosine 100 mg

Ferroptosis

Activators 6280 FIN 56 Ferroptosis activator 5 mg

25 mg

Oxidative Phosphorylation

Inhibitors 6358 Atovaquone Inhibits complex III of mitochondrial electron transport chain in parasites; also inhibits DHODH

10 mg

50 mg


Actin

Inhibitors 3974 Latrunculin B Inhibitor of actin polymerization 1 mg


Cell Adhesion Molecules

Other 6394 Peptide5 Connexin43 mimetic peptide 1 mg

RAGE

Antagonists 6259 RAGE antagonist peptide RAGE antagonist 1 mg



16 |

Featured Epigenetics Products

N N

O

HN

NHO

OO

NOHN

O

O

NS

N

Cl

dBET1 (6327)(+)-JQ1 based PROTAC that selectivelydegrades BET bromodomains in cells

OHNO

N

OH

O

NH

NS

O

O

SN

NN

N

Cl

O

O

HN

MZ1 (6154)(+)-JQ1 based PROTAC that selectively

degrades BRD4 in cells

NH

NN

NN

N

L Moses (6251)High affinity and selective PCAF

bromodomain inhibitor

Featured Epigenetics Products

EpigeneticsEpigenetics is the study of acquired changes or modifications in chromatin structure that arise independently of a change in the underlying DNA nucleotide sequence. Epigenetic modifications alter the accessibility of DNA to transcription machinery, thereby influencing gene expression.

Bromodomains

Inhibitors 6251 L Moses High affinity and selective PCAF bromodomain inhibitor 10 mg

50 mg

6181 OTX 015 BET bromodomain inhibitor; orally bioavailable 10 mg

50 mg

Other 6155 cis MZ 1 Negative Control for MZ1 5 mg

6327 dBET1 (+)-JQ1 based PROTAC that selectively degrades BET bromodomains in cells

5 mg

6154 MZ 1 (+)-JQ1 based PROTAC that selectively degrades BRD4 in cells 5 mg

6105 TC AC 28 High affinity BET bromodomain ligand 1 mg

Histone Acetyltransferases

Inhibitors 5103 Lys-CoA Selective p300 inhibitor 1 mg

Histone Deacetylases

Inhibitors 6284 BRD 73954 Dual histone deacetylase (HDAC) 6/8 inhibitor 10 mg

50 mg

6208 MS 275 HDAC (Class I) inhibitor 10 mg

50 mg

6270 Tubastatin A Potent HDAC6 inhibitor 10 mg

Histone Demethylases

Inhibitors 6384 Ciclopirox Pan-histone demethylase inhibitor 10 mg

50 mg

Histone Peptides

Substrates 6214 H3K4(Me) (1-20) Histone H3 peptide 1 mg

6215 H3K4(Me2) (1-20) Histone H3 peptide 1 mg


6217 Histone H3 (1-34) Histone H3 peptide 1 mg

6211 H3K27(Me) (15-34) Histone H3 peptide 1 mg





tocris.com | 17

OH

OP

HO

HO O

O

OP

O

P O

HO

HN

HN

S

HN

NH2

O

HN

O

O

O

O

OHO

HO O

N N

N

H2N

N

Lys-CoA (5103)Selective p300 inhibitor

HONH

O O

NH

BRD 73954 (6284)Dual histone deacetylase (HDAC) 6/8 inhibitor

HN

O

NH

O

ON NH2

MS 275 (6208)HDAC (Class I) inhibitor

HN O

NN

N

N

N

O

HN

GSK 343 (6128)Potent and selective SAM-competitive

EZH2 inhibitor

N

HN

ONHO

HN

OHNO

ONH

OH

O

O

UNC 3866 (6096)High affinity CBX4 and CBX7 inhibitor

Epigenetics - 2

NH2N

SO

HNO

AZD 1208 (6310)Potent pan Pim kinase inhibitor

O

N

O

F

N

NH

O

AZD 2461 (6060)Potent PARP inhibitor; orally bioavailable

N

N

O

NH

OH

Tubastatin A (6270)Potent HDAC6 inhibitor

Featured Epigenetics Products (continued)

Lysine Methyltransferases

Inhibitors 6167 A 196 Potent and selective SUV420H1/H2 inhibitor 10 mg

50 mg

6282 BRD 4770 G9a inhibitor and S-adenosyl methionine mimetic; cell permeable 10 mg

50 mg

6128 GSK 343 Potent and selective SAM-competitive EZH2 inhibitor 10 mg 50 mg

4930 UNC 2399 Biotinylated UNC 1999 (Cat.No. 4904) 1 mg

6096 UNC 3866 High affinity CBX4 and CBX7 inhibitor 10 mg

Pim Kinase

Inhibitors 6310 AZD 1208 Potent pan Pim kinase inhibitor 10 mg

50 mg

Poly(ADP-ribose) Polymerases

Inhibitors 6060 AZD 2461 Potent PARP inhibitor; orally bioavailable 10 mg

50 mg

6230 Rucaparib camsylate PARP inhibitor 10 mg

50 mg



18 |

Fluorescent ImagingFluorescent probes and dyes facilitate the visualization of subcellular components in live and fixed cells with high sensitivity and selectivity and enable monitoring of dynamic intracellular biochemical reactions. Fluorescent dyes may also be conjugated to antibodies for immunohistochemistry and flow cytometry use.

Janelia Fluor® DyesFluorescence imaging is an essential tool in biological research, requiring the precise labeling of biomolecules with bright fluorophores to enable visualization of proteins in live and fixed cells. Janelia Fluor® dyes are new, rhodamine based fluorescent dyes first developed at the Janelia Research Campus, Howard Hughes Medical Institute (HHMI), and sold under license by Tocris.

Key features of Janelia Fluor® dyes • Bright, photostable and cell-permeable• Supplied as NHS esters to allow conjugation to

antibodies• Compatible with self-labeling systems

(e.g.: HaloTag® and SNAP-tag®) • Compatible with confocal microscopy• Compatible with super-resolution microscopy (SRM)

techniques, including direct stochastic optical reconstruction microscopy (dSTORM)

• Photoactivatable derivatives developed for use in photoactivated localization microscopy (PALM) (#6149 and #6150).

Adult pig cardiac muscle tissue section (10 µm), labeled with antibodies against sarco/endoplasmic reticulum Ca2+-ATPase (SERCA). Secondary antibody conjugated to Janelia Fluor® 549, SE and imaged using dSTORM. Far superior detail compared to widefield image (bottom left). Scale bar = 400 nm.

Fluorescent Dyes

5435 Cyanine 3, SE Orange fluorescent dye for labeling of amines 10 mg

5437 Cyanine 7, SE Near-infrared fluorescent dye for labeling of amines 10 mg

6418 Janelia Fluor® 585, SE Cell permeable orange fluorescent dye; supplied as NHS ester 2 mg

6419 Janelia Fluor® 635, SE Cell permeable red fluorescent dye; supplied as NHS ester 2 mg

6420 Janelia Fluor® 669, SE Cell permeable red fluorescent dye; supplied as NHS ester 2 mg

6149 PA Janelia Fluor® 549, SE Photoactivatable cell permeable fluorescent dye; supplied as NHS ester 5 mg

6150 PA Janelia Fluor® 646, SE Photoactivatable cell permeable fluorescent dye; supplied as NHS ester 5 mg



tocris.com | 19

Signal TransductionSignal transduction, or intracellular signaling, is the transmission of molecular signals from a cell’s exterior to its interior. This process is initiated by cell surface receptors, and is required to ensure an appropriate cellular response. Signal transmission is propagated by either biochemical changes within the cell, or by membrane potential alterations.

Stem CellsStem cells are pluripotent or multipotent cells that are capable of self-renewal through mitotic cell division, and which may be induced to form more specialized cells of a tissue or organ by a process termed cellular differentiation. Key morphogens, such as Wnt, Hedgehog and Notch, influence stem cell self-renewal and differentiation.

Scientific ReviewsProduct Guides & Listings Life Science Posters

• GPCRs• Kinases • Cancer Research• Neurodegeneration

• Vascular Reactivity• Gut Hormones • Cancer Metabolism• Addiction

• Ras Oncoproteins• Nicotinic ACh Receptors• Dopamine Receptors• Stem Cells

Life Science Literature from TocrisTocris also provides a wide range of scientific literature free of charge, including the following titles:

To download or request copies, please visit www.tocris.com/requestliterature

Calcium Signaling

Inhibitors 5976 Ned K NAADP signaling inhibitor 10 mg

50 mg

Cytokine and NF-κB Signaling

Inhibitors 6218 Galiellalactone STAT3 inhibitor; active in vivo 500 µg

Gap Channels

Blockers 6227 TAT-Gap19 Cx43 hemichannel blocker 1 mg

Inflammasomes

Other 6366 Muramyl dipeptide Activates NOD2 receptors 1 mg


Stem Cell Differentiation

6385 Phenanthroline Enhances hPSC differentiation into cranial placode cells 100 mg

6424 Sodium cromoglicate Promotes ESC/iPSC differentiation into pancreatic endocrine islet cells 50 mg


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