TPOP146

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

一种有效的选择性 CBP/p300 布罗莫结构域抑制剂，CBP 布罗莫结构域的 Kd 为 134 nM。

A potent and selective CBP/p300 bromodomain inhibitor with Kd of 134 nM for CBP bromodomain, displays excellent selectivity over other bromodomains (>30-fold over BRD4 (1)); targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments.

Exposure to 1 μM TPOP146 results in a significant decrease of recovery half-life that is comparable to the construct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146 targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments. They are for reference only.

——

TPOP-146 | TPOP 146

Chromatin/Epigenetic

Bromodomain

Bromodomain

——

——

2018300-62-2

481.5839

C27H35N3O5

>98% (HPLC)

DMSO

COC1=CC(C2=CC(C(N[C@H]3CCCN(C)C3)=O)=C(OCCN(C(CC)=O)C4)C4=C2)=CC(OC)=C1

1,4-Benzoxazepine-9-carboxamide, 7-(3,5-dimethoxyphenyl)-2,3,4,5-tetrahydro-N-[(3S)-1-methyl-3-piperidinyl]-4-(1-oxopropyl)-

(-20℃)

With Ice Pack

≥ 2 years