Tel: +1-832-582-8158

Product Categories

EPZ5676

Catalog No.S7062

EPZ-5676 is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.

Price Stock Quantity  
USD 270 In stock
USD 970 In stock
Contact Us
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Selleck USA Tel: +1-832-582-8158[email protected]
EPZ5676 Chemical Structure

EPZ5676 Chemical Structure
Molecular Weight: 562.71

Validation & Quality Control

In 2013, 1068 articles cited Selleck products, including the listed 11 with IF>30.

Quality Control & MSDS

Histone Methyltransferase Inhibitors with Unique Features

  • Most Potent DOT1L Inhibitor

    SGC 0946 DOT1L, IC50=0.3 nM.

  • FDA-approved Inhibitor

    Entacapone Approved by FDA for Parkinson's disease.

  • Newest HMT Inhibitor

    EPZ004777 Potent, selective DOT1L inhibitor with IC50 of 0.4 nM.

  • Classic HMT Inhibitor

    UNC1999 Potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.

Product Information

  • Compare Histone Methyltransferase Inhibitors
    Compare Histone Methyltransferase Products
  • Research Area

Product Description

Biological Activity Protocol Clinical Trial Information Chemical Information Tech Support & FAQs

Biological Activity

Description EPZ-5676 is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.
Targets DOT1L
IC50 80 pM [1](Ki)
In vitro EPZ-5676 reduces H3K79 dimethylation with a cellular IC50 of 2.6 nM in MV4-11 cells. EPZ-5676 treatment results in concentration- and time-dependent reduction of H3K79 methylation without effect on the methylation status of other histone sites, which leads to inhibition of key MLL target genes and selective, apoptotic cell killing in MLL-rearranged leukemia cells. EPZ-5676 inhibits proliferation of MLL-AF4 rearranged cell line MV4-11 with an IC50 of 9 nM.
In vivo EPZ-5676 continuously intravenous infusion for 21 days to xenograft model of MLL-rearranged leukemia, leads to dose-dependent anti-tumor activity. At the highest dose of 70.5 mg/kg/day, complete tumor regressions are achieved with no regrowth for up to 32 days after the cessation of treatment. No significant weight loss or obvious toxicity is observed in rats treated with EPZ-5676 during efficacy study.
Features

Protocol(Only for Reference)

1

References

[1] Robert A. Protein methyltransferases in cancer. AACR Annual Meeting, 2013.

[2] Pollock RM, 54th ASH Annual Meeting and Exposition, 2012, Abst 2379

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators 		Start Date Phases
NCT01684150 Recruiting Acute Myeloid Leukemia|Acute Lymphoblastic Leukemia|Myelodysplastic Syndrome|Myeloproliferative Disorders|Chronic Myeloid Leukemia Epizyme, Inc.|Celgene Corporation 2012-09 Phase 1

Chemical Information

Molecular Weight (MW) 562.71
Formula

C30H42N8O3
CAS No. 1380288-87-8
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 100 mg/mL (177 mM)
Water <1 mg/mL (<1 mM)
Ethanol 100 mg/mL (177 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 9H-Purin-6-amine, 9-[5-deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-
Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Customers Who Bought This Item Also Bought

  • EPZ-6438

    EPZ-6438 is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.

  • BIX 01294

    BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases.

  • Trametinib (GSK1120212)

    Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2.

    Features:More potent than PD0325901 or AZD6244.

  • Ceritinib (LDK378)

    LDK378 is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3.

    Features:Does not cross react with c-Met, and has an improved in vivo glucose homeostasis profile relative to TAE684. May be active in Crizotinib-relapsed tumors.

  • C646

    C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM. Preferentially selective for p300 versus other acetyltransferases.

    Features:Extensively used as a pharmacologic probe in cancer cells. Potential use for prostate and lung cancers.

  • VX-680 (Tozasertib, MK-0457)

    VX-680 (Tozasertib, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. Phase 2.

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions
Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Histone Methyltransferase Products

  • EPZ-6438

    EPZ-6438 is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.

  • GSK343

    GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.

    Features:A chemical probe for the SGC epigenetics initiative. Potential use in a variety of solid tumors.

  • UNC1999

    UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.

    Features:The first orally bioavailable inhibitor of EZH2 and EZH1.

  • Entacapone

    Entacapone inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM.

  • BIX 01294

    BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases.

  • SGC 0946

    SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM, is inactive against a panel of 12 PMTs and DNMT1.

  • 3-Deazaneplanocin A (DZNeP)

    3-deazaneplanocin A (DZNeP), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.

  • EPZ004777 HCl

    EPZ004777 HCl is the hydrochloride salt of EPZ004777, which is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.

  • (+)-JQ1

    (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2), binding to all bromodomains of the BET family, but not to bromodomains outside the BET family.

    Features:(+)-JQ1 is more effective than (-)-JQ1.

  • Decitabine

    Decitabine is a potent inhibitor of DNA methylation with IC50 of 438 nM and 4.38 nM in HL-60 and KG1a cells, respectively.

Recently Viewed Items

Tags: buy EPZ5676 | EPZ5676 supplier | purchase EPZ5676 | EPZ5676 cost | EPZ5676 manufacturer | order EPZ5676 | EPZ5676 distributor
Contact Us