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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-CCS1477
CCS1477

Chemical Structure : CCS1477

CAS No.: 2222941-37-7

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CCS1477 (CCS 1477, Inobrodib)

货号: PC-38126Not For Human Use, Lab Use Only.

CCS1477 (Inobrodib) is an orally bioavailable, potent, and selective inhibitor of the p300/CBP bromodomain, binds to p300 and CBP with Kds of 1.3 and 1.7 nM respectively.

规格 价格 库存 数量
5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3580 In stock
50 mg ￥5580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CCS1477 (Inobrodib) is an orally bioavailable, potent, and selective inhibitor of the p300/CBP bromodomain, binds to p300 and CBP with Kds of 1.3 and 1.7 nM respectively.
CCS1477 (Inobrodib) displays > 170/130-fold selectivity compared with BRD4, CCS1477 binding to cellular histones in an in-cell BRET assay, with an IC50 of 19 nM for p300 and 1060 nM for BRD4.
CCS1477 (Inobrodib) has only minimal binding to BRD2, 3, 4, 9 and WDR9 (14-33% of control at 1 uM) in a bromoscan assay of 32 bromodomains.
CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases AR- and C-MYC-regulated gene expression.
CCS1477 has antitumor activity, regulating AR and C-MYC signaling in AR-SV-driven models.
CCS1477 modulates KLK3 blood levels and regulates CRPC biopsy biomarker expression.

物理化学性质&存储条件

分子量 535.636
分子式 C31H35F2N3O3
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 1 Month
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(3R)-2-(3,4-difluorophenyl)-3-(5-(3,5-dimethyl-4,5-dihydroisoxazol-4-yl)-1-((1r,4R)-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)cyclohexan-1-one

参考文献

1. Jonathan Welti, et al. Cancer Discov. 2021 May;11(5):1118-1137.

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