IACS-9571

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

IACS-9571 是一种有效的、选择性的双重 TRIM24-BRPF1 bromodomain 抑制剂，Kd 分别为 31 和 14 nM。

IACS-9571 is a potent, selective dual TRIM24-BRPF1 bromodomain inhibitor with Kd of 31 and 14 nM, respectively; displays 9- and 21-fold selectivity against BRPF2 and BRPF3, weaker affinities with BAZ2B (Kd= 400 nM) and the second domain of TAF1 (Kd=1,800 nM), and >7,700-fold selectivity versus BRD4 BD1 and BD2; demonstrates excellent cellular potency (EC50= 50 nM) and favorable pharmacokinetic properties; IACS-9571 is a chemical probe to investigate biological and pharmacological role of TRIM24 and/or BRPF1 bromodomain inhibition in vitro and in vivo.

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.

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IACS9571

Chromatin/Epigenetic

Bromodomain

Bromodomain

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1800477-30-8

642.768

C32H42N4O8S

>98% (HPLC)

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CCCOC1=CC(=CC(=C1)OC2=CC3=C(C=C2NS(=O)(=O)C4=CC(=C(C=C4)OC)OC)N(C(=O)N3C)C)OCCCCN(C)C

Benzenesulfonamide, N-[6-[3-[4-(dimethylamino)butoxy]-5-propoxyphenoxy]-2,3-dihydro-1,3-dimethyl-2-oxo-1H-benzimidazol-5-yl]-3,4-dimethoxy-

(-20℃)

With Ice Pack

≥ 2 years