hmt hdm enzymes and assays 20150413 · epigenetic regulation of transcription is governed by dna...

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Epigenetic regulation of transcription is governed by DNA methylation and post-translational histone modifications. While histone acetylation is well-characterized, the study of histone methylation is more nascent. Histone methyltransferases (HMTs) and histone demethylases are critical for transcriptional regulation in both normal and diseased states, and are important targets for drug discovery. H H i i s s t t o o n n e e M M e e t t h h y y l l a a t t i i o o n n Assay Kits Catalog # Amount EZH2 Assay Kit-Luminescent 52009L 96 rxns EZH2 (Y641F) Assay Kit-Luminescent 52075 96 rxns EZH2 (Y641N) Assay Kit-Luminescent 52076 96 rxns G9a Assay Kit-Luminescent 52001L 96 rxns LSD1 Assay Kit-Fluorescent 50106 96 rxns LSD1 Assay Kit- Fluorescent 50107 384 rxns LSD1 Assay Kit- Luminescent 50109 96 rxns JMJD2C Assay Kit-Luminescent 50405 96 rxns JMJD2D Assay Kit-Luminescent 50418 96 rxns MLL1 Complex Assay Kit- Luminescent 53008 96 rxns NSD1 Assay Kit-Luminescent 53010 96 rxns. NSD2 Assay Kit-Luminescent 53009 96 rxns. PRMT1 Assay Kit-Luminescent 52004L 96 rxns PRMT3 Assay Kit-Luminescent 52005L 96 rxns PRMT4 (CARM1) Assay Kit-Luminescent 52041L 96 rxns PRMT5 Assay Kit-Luminescent 52002L 96 rxns PRMT6 Assay Kit-Luminescent 52046 96 rxns SETD2 Assay Kit-Luminescent 52060 96 rxns Set7/9 Assay Kit-Luminescent 52003L 96 rxns SUV39H1 Assay Kit-Luminescent 52045 96 rxns SUV39H2 Assay Kit-Luminescent 52008 96 rxns SUV4-20H1 Assay Kit – Luminescent 53011 96 rxns. Histone H3(K9) Universal Assay Kit 52072 96 rxns Histone H4(R3) Universal Assay Kit 52074 96 rxns LSD1 (Cat. #50100) demethylase activity measured with the LSD1 Fluorescent Assay Kit, Cat. #50106. Methylation Assay Kits BPS Bioscience produces a unique portfolio of epigenetic assay kits for methylation research, including enzyme activity assays for histone demethylation (LSD1, JMJD2A- C), and histone methylation of arginine (PRMT) or lysine (EZH2, G9a, Set7/9, SUV39H1/2). These simple, sensitive assays provide precise measurement of methylation activity for drug discovery research. PRMT4/CARM1 (Cat. #51047) inhibition by S-adenosyl- homocysteine, measured using the PRMT4 Assay Kit, Cat. #52041L. Homogenous Assay Kits Cat. # Amount G9a Assay Kit, Homogeneous 52051 384 rxns EZH2 Assay Kit, Homogeneous 52059 384 rxns FBXL10, Homogeneous 50610 384 rxns FBXL11, Homogeneous 50611 384 rxns JARID1A, Homogeneous 50510 384 rxns JARID1B, Homogeneous 50512 384 rxns JARID1C, Homogeneous 50511 384 rxns JHDM1D Assay Kit, Homogeneous 50420 384 rxns JMJD2A Assay Kit, Homogeneous 50413 384 rxns JMJD2B Assay Kit, Homogeneous 50414 384 rxns JMJD2C Assay Kit, Homogeneous 50415 384 rxns JMJD2E Assay Kit, Homogeneous 50417 384 rxns JMJD3 Assay Kit, Homogeneous 50416 384 rxns LSD1 Assay Kit, Homogeneous 50108 384 rxns PHF8 Assay Kit, Homogeneous 50515 384 rxns PRMT1 Assay Kit, Homogeneous 52054 384 rxns PRMT3 Assay Kit, Homogeneous 52055 384 rxns PRMT5 Assay Kit, Homogeneous 52052 384 rxns PRMT6 Assay Kit, Homogeneous 52056 384 rxns PRMT8 Assay Kit, Homogeneous 52058 384 rxns UTX Assay Kit, Homogeneous 50516 384 rxns In Italia: - Vinci-Biochem – T. 0571 568 147 [email protected] - www.vincibiochem.it

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Epigenetic regulation of transcription

is governed by DNA methylation

and post-translational histone

modifications. While histone

acetylation is well-characterized, the

study of histone methylation is more

nascent. Histone methyltransferases

(HMTs) and histone demethylases are critical for transcriptional

regulation in both normal and diseased states, and are important

targets for drug discovery.

HHiissttoonnee MMeetthhyyllaattiioonn

Assay Kits Catalog # Amount

EZH2 Assay Kit-Luminescent 52009L 96 rxns

EZH2 (Y641F) Assay Kit-Luminescent 52075 96 rxns

EZH2 (Y641N) Assay Kit-Luminescent 52076 96 rxns

G9a Assay Kit-Luminescent 52001L 96 rxns

LSD1 Assay Kit-Fluorescent 50106 96 rxns

LSD1 Assay Kit- Fluorescent 50107 384 rxns

LSD1 Assay Kit- Luminescent 50109 96 rxns

JMJD2C Assay Kit-Luminescent 50405 96 rxns

JMJD2D Assay Kit-Luminescent 50418 96 rxns

MLL1 Complex Assay Kit- Luminescent 53008 96 rxns

NSD1 Assay Kit-Luminescent 53010 96 rxns.

NSD2 Assay Kit-Luminescent 53009 96 rxns.

PRMT1 Assay Kit-Luminescent 52004L 96 rxns

PRMT3 Assay Kit-Luminescent 52005L 96 rxns

PRMT4 (CARM1) Assay Kit-Luminescent 52041L 96 rxns

PRMT5 Assay Kit-Luminescent 52002L 96 rxns

PRMT6 Assay Kit-Luminescent 52046 96 rxns

SETD2 Assay Kit-Luminescent 52060 96 rxns

Set7/9 Assay Kit-Luminescent 52003L 96 rxns

SUV39H1 Assay Kit-Luminescent 52045 96 rxns

SUV39H2 Assay Kit-Luminescent 52008 96 rxns

SUV4-20H1 Assay Kit – Luminescent 53011 96 rxns.

Histone H3(K9) Universal Assay Kit 52072 96 rxns

Histone H4(R3) Universal Assay Kit 52074 96 rxns

LSD1 (Cat. #50100) demethylase activity measured with the LSD1 Fluorescent Assay Kit, Cat. #50106.

Methylation Assay Kits BPS Bioscience produces a unique portfolio of epigenetic

assay kits for methylation research, including enzyme

activity assays for histone demethylation (LSD1, JMJD2A-

C), and histone methylation of arginine (PRMT) or lysine

(EZH2, G9a, Set7/9, SUV39H1/2). These simple, sensitive

assays provide precise measurement of methylation activity

for drug discovery research.

PRMT4/CARM1 (Cat. #51047) inhibition by S-adenosyl-homocysteine, measured using the PRMT4 Assay Kit, Cat. #52041L.

Homogenous Assay Kits Cat. # Amount

G9a Assay Kit, Homogeneous 52051 384 rxns

EZH2 Assay Kit, Homogeneous 52059 384 rxns

FBXL10, Homogeneous 50610 384 rxns

FBXL11, Homogeneous 50611 384 rxns

JARID1A, Homogeneous 50510 384 rxns

JARID1B, Homogeneous 50512 384 rxns

JARID1C, Homogeneous 50511 384 rxns

JHDM1D Assay Kit, Homogeneous 50420 384 rxns

JMJD2A Assay Kit, Homogeneous 50413 384 rxns

JMJD2B Assay Kit, Homogeneous 50414 384 rxns

JMJD2C Assay Kit, Homogeneous 50415 384 rxns

JMJD2E Assay Kit, Homogeneous 50417 384 rxns

JMJD3 Assay Kit, Homogeneous 50416 384 rxns

LSD1 Assay Kit, Homogeneous 50108 384 rxns

PHF8 Assay Kit, Homogeneous 50515 384 rxns

PRMT1 Assay Kit, Homogeneous 52054 384 rxns

PRMT3 Assay Kit, Homogeneous 52055 384 rxns

PRMT5 Assay Kit, Homogeneous 52052 384 rxns

PRMT6 Assay Kit, Homogeneous 52056 384 rxns

PRMT8 Assay Kit, Homogeneous 52058 384 rxns

UTX Assay Kit, Homogeneous 50516 384 rxns

In Italia: - Vinci-Biochem – T. 0571 568 147 [email protected] - www.vincibiochem.it

Methylation Enzymes

BPS Bioscience manufactures the most extensive line of

methylation-related enzymes available. These highly

active enzymes are suitable for enzymatic profiling,

inhibitor screening assays, and drug discovery.

EZH2 Complex (Cat. #51004) inhibition by S-adenosyl-homocysteine, measured using the EZH2 Assay Kit, Cat. #52059.

Histone Methyltransferases

Enzyme Cat. # Amount

EZH2/EED/SUZ12 Complex 51003 50 µg

EZH2/EED/SUZ12/RbAp48 Complex 51099 50 µg

EZH2/EED/SUZ12/RbAp48/AEBP2 Complex (KMT6A)

51004 50 µg

EZH2/SUZ12/RbAp48 Complex 51098 20 µg

G9a (KMT1C), E. coli expression 51000 50 µg

G9a (KMT1C), Sf9 expression 51001 20 µg

Metnase (SETMAR) 51018 20 µg

MLL1/WDR5/Ash2L/RbBP5/DPY30 51021 50 µg

NSD1 (KMT3B), 1849-end 51024 50 µg

NSD2 (MMSET, REIIBP), 941-end 51026 50 µg

NSD2(MMSET, REIIBP), 782-end 51025 20 µg

NSD3 (1021-1322) 51036 50 µg

PRDM2 (RIZ1) 51030 100 µg

PRDM12 50320 50 µg

PRDM14 50321 50 µg

PRMT1, E. coli expression 51040 50 µg

PRMT1, Sf9 expression 51041 20 µg

PRMT3 51043 50 µg

PRMT4 (CARM1), HEK293 expression 51047 20 µg

PRMT5/MEP50, HEK293 expression 51045 20 µg

PRMT5/MEP50 Complex 51048 20 µg

PRMT6 51049 20 µg

PRMT7 51054 20 µg

PRMT8 51052 20 µg

PRMT9 51053 20 µg

SET2 (KMT3A, HYPB) 51012 100 µg

SET7/SET9 (KMT7) (E. coli) 51010 100 µg

SET7/SET9 (KMT7) (Sf9) 50019 50 µg SET7/SE

SET8 (KMT5A) 51008 50 µg

SMYD2 (KMT3C) 51014 20 µg

SMYD3 (KMT3E), 35-end 51015 20 µg

SMYD3 (KMT3E), full length 51016 20 µg

SUV39H1 (KMT1A), 82-end 51070 50 µg

SUV39H1 (KMT1A), full length 51071 5 µg

SUV39H2 (KMT1B) 51080 50 µg

SUV4-20H1 (KMT5B) 51090 50 µg

SUV4-20H2 (KMT5C) 51060 50 µg

SUZ12 50282 20 µg

Histone Methyltransferases

Enzyme Cat. # Amount

AEBP2 50281 50 µg

Dot1L (KMT4) 51005 50 µg

EHMT1 (GLP) 51020 50 µg

EZH1/EED/SUZ12 Complex 51006 50 µg

EZH1/EED/SUZ12/RbAp48/AEBP2 Complex (KMT6B)

51007 50 µg

EZH2 non-complexed 50279 20 µg

EZH2/EED inactive 51002 20 µg

EZH2 A677T/EED/SUZ12/RbAp48/ AEBP2 Complex

51039 20 µg

EZH2 Y641F/EED/SUZ12/RbAp48/ AEBP2 Complex

51017 20 µg

EZH2 Y641H/EED/SUZ12/RbAp48/ AEBP2 Complex

51011 20 µg

EZH2 Y641S/EED/SUZ12/RbAp48/ AEBP2 Complex

51013 20 µg

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Histone Demethylases

Enzyme Cat. # Amount

FBXL10 (KDM2B) 50120 20 µg

FBXL11 (KDM2A), FLAG-Avi-tags 50156 20 µg

JARID1A (KDM5A) 50110 20 µg

JARID1A (KDM5A), His-Avi-tags 50155 20 �g

JARID1B (KDM5B, PLU-1) 50122 20 µg

JARID1C (KDM5C, SMCX) 50112 20 µg

JARID1D (KDM5D, SMCY) 50113 20 µg

JHDM1D, FLAG-tag 50419 20 µg

JMJD1A (KDM3A) 50130 20 µg

JMJD2A (KDM4A) 50123 100 µg

JMJD2B (KDM4B), FLAG tag 50104 100 µg

JMJD2B (KDM4B), GST tag 50111 100 µg

JMJD2C (KDM4C) 50105 100 µg

JMJD2D (KDM4D) 50117 100 µg

JMJD2E (KDM4DL) 50118 100 µg

JMJD3 (KDM6B) 50115 20 µg

JMJD6 (RDM) 50140 20 µg

LSD1 (KDM1A) 50100 50 µg

LSD1, cleaved GST-tag 50097 50 µg

PHF8 (KDM7B) 50131 20 �g

PHF8 (KDM7B), full length 50132 20 �g

UTX (KDM6A),C-term FLAG-tag 50116 20 µg

UTX (KDM6A), N-term FLAG-tag 50119 20 µg

Activity, measured with the SUV39H2 Direct Activity Assay Kit (Cat. #52008) and purity of SUV39H2 (Cat. #51080) lysine methyltransferase.

DNA Demethylases

Enzyme Cat. # Amount

TET1 50161 50 �g

In Italia: - Vinci-Biochem – T. 0571 568 147 [email protected] - www.vincibiochem.it

Substrates and Inhibitors

BPS Bioscience offers both substrates for histone

methyltransferases (HMTs) and histone demethylases, as well

as inhibitors for HMTs. These products are useful in screening

small molecule activity.

Histone Demethylase Inhibitor

Enzyme Cat. # Amount

Tranylcypromine (2-PCPA) 27305 100 mg

HMT Inhibitors

Enzyme Cat. # Amount

AMI-1 (sodium salt) 27307 25 mg

BIX01294 27220 10 mg

Chaetocin 27221 1 mg

3-deazaneplanocin A 27617 500 �g

Ellagic acid 27219 100 mg

UNC0224 27303 5 mg

UNC0321 (trifluoroacetate salt) 27306 50 mg

UNC0638 27222 5 mg

Substrates

Substrate Cat. # Amount

[Lys(Me1)K27] Histone H3 Peptide, 21-44

52020 40 nmole

Di-Methylated K4 H3 Peptide 50101 500 µL

Di-Methylated K9 H3 Peptide 50351 500 µL

Di-Methylated R3 H4 Peptide 51200 500 µL

Histone H1, full length* 52043 100 µg

Histone H2A, Biotinylated* 52049 50 µg

Histone H2A, full length* 52021 1 mg

Histone H2B, full length* 52022 1 mg

Histone H3 K27C, Full Length 52080 100 µg

Histone H3 K27cMe1, Full Length 52081 100 µg

Histone H3 K27cMe2, Full Length 52082 100 µg

Histone H3 K27cMe3, Full Length 52083 100 µg

Histone H3 K27M 52101 100 µg

Histone H3 Peptide, 1-21* 52011 80 nmole

Histone H3 Peptide, 21-44* 52017 80 nmole

Histone H3, 2-58 52013 500 µg

Histone H3, Biotinylated* 52053 50 µg

Histone H3.1, full length* 52023 1 mg

Histone H3/H4 Tetramer ,full length 52064 100 µg

Histone H3-H4 Tetramer H3K27C Unmodified

52084 50 µg

Histone H3-H4 Tetramer H3K27C Unmodified

52088 50 µg

Histone H3-H4 Tetramer H3K27cMe2 52086 50 µg

Histone H3-H4 Tetramer H3K27cMe3 52087 50 µg

Histone H4 Peptide, 1-21* 52018 80 nmole

Histone H4, 2-58 52019 500 µg

Histone H4, full length* 52024 1 mg

*Also available in additional sizes.

Cofactors/Related Proteins

Protein Catalog # Amount

CoREST 50274 100 µg

EED 50280 50 µg

Purity and gel image of CoREST, BPS Catalog # 50274.

6044 Cornerstone Court West, Ste. E, San Diego, CA 92121

ph 858.829.3082

fax 858.481.8694

www.bpsbioscience.com Rev. Apr 2015

In Italia: - Vinci-Biochem – T. 0571 568 147 [email protected] - www.vincibiochem.it