IACS-9571(Synonyms: ASIS-P040)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

IACS-9571 (Synonyms: ASIS-P040)

IACS-9571 是溴结构域蛋白 TRIM24 和 BRPF1 的抑制剂，对 TRIM24 的 IC50 和 Kd 值分别为 8 nM 和 31 nM，对 BRPF1 的 Kd 值为 14 nM。

IACS-9571(Synonyms: ASIS-P040)

IACS-9571 Chemical Structure

CAS No. : 1800477-30-8

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IACS-9571 的其他形式现货产品:

IACS-9571 hydrochloride

生物活性

IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.

IC50 & Target

IC50: 8 nM (TRIM24)[1]
Kd: 31 nM (TRIM24), 14 nM (BRPF1)[1]
体外研究
(In Vitro)

IACS-9571 shows excellent cellular potency with EC50 of 50 nM. IACS-9571 (1 μM) has potent activities against a panel of 32 bromodomains. IACS-9571 is a selective dual TRIM24/BRPF1 inhibitor (Kd = 1.3/2.1 nM) with 9- and 21-fold selectivity against BRPF2 and BRPF3, respectively. IACS-9571 does not interact with the BET sub-family of bromodomains, displaying greater than 7,700-fold selectivity versus BRD4(1, 2) relative to TRIM24[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

642.76

Formula

C32H42N4O8S
CAS 号

1800477-30-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Palmer WS, et al. Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J Med Chem. 2016 Feb 25;59(4):1440-54.

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