EPZ5676

EPZ5676

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Histone Methyltransferase Inhibitors with Unique Features

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Protocol(Only for Reference)

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-01-26)

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In 2014, 2352 articles (32 with IF>20) cited Selleck products.

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Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

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Catalog No.S7062

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

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10mg	USD 270	In stock
50mg	USD 970	In stock

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

EPZ5676 Chemical Structure
Molecular Weight: 562.71

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.

Compare Histone Methyltransferase Inhibitors

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Inhibitory Selectivity
Solubility

Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S7062	EPZ5676	<1 mg/mL	100 mg/mL	100 mg/mL
S7004	EPZ005687	<1 mg/mL	2 mg/mL	<1 mg/mL
S7164	GSK343	<1 mg/mL	1 mg/mL	4 mg/mL
S8006	BIX 01294	98 mg/mL	98 mg/mL	8 mg/mL
S7128	EPZ-6438	<1 mg/mL	29 mg/mL	<1 mg/mL
S7120	3-deazaneplanocin A (DZNeP) HCl	52 mg/mL	52 mg/mL	<1 mg/mL
S7165	UNC1999	<1 mg/mL	100 mg/mL	100 mg/mL
S7265	MM-102	100 mg/mL	100 mg/mL	100 mg/mL
S7079	SGC 0946	<1 mg/mL	100 mg/mL	100 mg/mL
S3147	Entacapone	<1 mg/mL	61 mg/mL	2 mg/mL
S7353	EPZ004777	<1 mg/mL	100 mg/mL	100 mg/mL
S7294	PFI-2	4 mg/mL	99 mg/mL	66 mg/mL
S7619	MI-3 (Menin-MLL Inhibitor)	<1 mg/mL	19 mg/mL	19 mg/mL
S7618	MI-2 (Menin-MLL Inhibitor)	<1 mg/mL	75 mg/mL	75 mg/mL
S7610	UNC0631	<1 mg/mL	100 mg/mL	5 mg/mL

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

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

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m²)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
K_m factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B K_m
	Animal A K_m

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse K_m(3)	= 11.2 mg/kg
	rat K_m(6)

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

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

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT02141828	Recruiting	Leukemia\|Acute Myeloid Leukemia\|Acute Lymphocytic Leukemia\|Acute Leukemias	Epizyme, Inc.\|Celgene Corporation	May 2014	Phase 1
NCT02141828	Recruiting	Leukemia\|Acute Myeloid Leukemia\|Acute Lymphocytic Leukemia\|Acute Leukemias	Epizyme, Inc.\|Celgene Corporation	May 2014	Phase 1
NCT01684150	Recruiting	Acute Myeloid Leukemia\|Acute Lymphoblastic Leukemia\|Myelodysplastic Syndrome\|Myeloproliferative Disorders	Epizyme, Inc.\|Celgene Corporation	September 2012	Phase 1
NCT01684150	Recruiting	Acute Myeloid Leukemia\|Acute Lymphoblastic Leukemia\|Myelodysplastic Syndrome\|Myeloproliferative Disorders	Epizyme, Inc.\|Celgene Corporation	September 2012	Phase 1

Molecular Weight (MW)	562.71
Formula	C₃₀H₄₂N₈O₃
CAS No.	1380288-87-8

Storage	3 years -20℃Powder
Storage	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	100 mg/mL (177.71 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	100 mg/mL (177.71 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]-

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EPZ-6438
EPZ-6438 is a potent, and selective EZH2 inhibitor with K_i 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.
MM-102
MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
EPZ004777
EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
OG-L002
OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.

Features:This selective LSD1 inhibitor was discovered in 2013. Potential for use in viral diseases such as HSV and VZV.
MK-2206 2HCl
MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

Features:The first allosteric small molecule inhibitor of Akt to enter clinical development.
Selumetinib (AZD6244)
Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.

Features:First MEK inhibitor being tested in Phase II clinical trials.

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

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MI-3 (Menin-MLL Inhibitor)
MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
MI-2 (Menin-MLL Inhibitor)
MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
PFI-2
PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with K_{i (app)} and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
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.
EPZ-6438
EPZ-6438 is a potent, and selective EZH2 inhibitor with K_i 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.
3-deazaneplanocin A (DZNeP) HCl
3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with K_i of 50 pM.
EPZ004777
EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 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.
MM-102
MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
EPZ005687
EPZ005687 is a potent and selective inhibitor of EZH2 with K_i of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

Description

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

DOT1L ^[1]

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.

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.