BRD-4770

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种 SAM 模拟物，可选择性抑制组蛋白甲基转移酶 (HMT) 的子集。

A SAM mimetic that selectively inhibits a subset of Histone Methyltransferase (HMTs), including G9a, in biochemical assays and in cells; decreases H3K9 trimethylation level in PANC-1 cells with EC50 of 5 uM; induces senescence, and inhibits both anchorage-dependent and -independent proliferation in PANC-1 cells; also increases LC3-II levels and the autophagosome number in PANC-1 cells combined with Gossypol.

BRD4770 (0-20 μM; 72 hours; PANC-1 cells) treatment reduces the number of cells after 72 h.BRD4770 (2.5-5 μM; 24 hours; PANC-1 cells) treatment decreases H3K9 trimethylation level by 23% in PANC-1 cells.BRD4770 induces a senescent phenotype in a pancreatic cancer cell line. BRD4770 also inhibits both anchorage-dependent and -independent cell proliferation and induces G2/M cell-cycle arrest. BRD4770 activates the ataxia telangiectasia mutated (ATM) pathway without inducing DNA damage, while the ataxia telangiectasia and Rad3-related protein (ATR) pathway is not affected.BRD4770 also induces increased levels of lysine acetylation in cells without inhibiting histone deacetylases. Cell Viability Assay Cell Line:PANC-1 cells Concentration:0 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM Incubation Time:72 hours Result:Reduced the number of cells after 72 h.Western Blot Analysis Cell Line:PANC-1 cells Concentration:2.5 μM, 5 μM Incubation Time:24 hours Result:Decreased H3K9 trimethylation level by 23% in PANC-1 cells.

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BRD 4770 | BRD4770

Chromatin/Epigenetic

HMTase

G9a

Cancer

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1374601-40-7

413.4684

C25H23N3O3

>98% (HPLC)

10 mM in DMSO

O=C(C1=CC=C2C(N=C(NC(C3=CC=CC=C3)=O)N2CCCC4=CC=CC=C4)=C1)OC

1H-Benzimidazole-5-carboxylic acid, 2-(benzoylamino)-1-(3-phenylpropyl)-, methyl ester

(-20℃)

With Ice Pack

≥ 2 years