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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-B029-2
B029-2

Chemical Structure : B029-2

CAS No.: 2379410-19-0

B029-2 (SYY-B029-2)

货号: PC-28014Not For Human Use, Lab Use Only.

B029-2 (SYY-B029-2) is a potent p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 of 0.49/7.1 nM for p300/CBP rspectively, shows anti-proliferation on ovarian cancer cell line OVCAR-3 with IC50 of 153 nM.

规格 价格 库存 数量
25 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

B029-2 (SYY-B029-2) is a potent p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 of 0.49/7.1 nM for p300/CBP rspectively, shows anti-proliferation on ovarian cancer cell line OVCAR-3 with IC50 of 153 nM.
B029-2 shows no activity against HATs including p300, GCN5, NatD, PCAF, KAT7 and MOF, as long as some Non-HATs histone modification enzyme including JMJD2A, LSD1, HDAC1 and HDAC2.
B029-2 strongly inhibits the activity of p300/CBP in ovarian cancer cell lines and affect downstream signaling pathways.
B029-2 (30 mg/kg, qd). significantly enhances the antitumor effect in OVCAR-3 xenograft models.
B029-2 specifically decreased H3K18Ac and H3K27Ac and displayed significant antitumor effects in HCC cells in vitro and in vivo.

物理化学性质&存储条件

分子量 522.53
分子式 C27H27FN4O6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-((R)-3'-(2-((R)-3-cyclopropyl-7-fluoro-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)-2-oxoethyl)-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-5-yl)-3-methylurea

参考文献

1. Cai LY, et al. Cancer Res. 2021 Feb 15;81(4):860-872.

2. Hong Ding, et al. Bioorg Med Chem. 2021 Dec 15:52:116512.

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