Pinometostat (EPZ5676) - Moligand™, 10mM in DMSO , Inhibitor of DOT1 like histone lysine methyltransferase, CAS No.1380288-87-8, Inhibitor of DOT1 like histone lysine methyltransferase

CAS: 1380288-87-8 Cat. No.: P408332 Peso molecular: 562.71

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

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]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Pinometostat (EPZ5676) Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K i of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibi
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.
Cell Data

cell lines：Splenocytes

Concentrations：

Incubation Time：

Powder Purity:≥97%

Specifications

Sinónimos

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]-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K_i of 80 pM in a cell-free assay, demonstrating >37, 000-fold selectivity against all other PMTs tested, inhibits H3K79 met

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of DOT1 like histone lysine methyltransferase

Nombres e identificadores

• Isómeros SMILES: CC(C)N(C[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)N)O)O)C4CC(C4)CCC5=NC6=C(N5)C=C(C=C6)C(C)(C)C
• Peso molecular: 562.71
• Reaxy-Rn: 28683701
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=28683701&ln=

Objetivos asociados (humanos)

DOT1L Tchem Histone-lysine N-methyltransferase, H3 lysine-79 specific (2 Activities)

Discover Target: DOT1L

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)