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SJB2-043
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SJB2-043图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
SJB2-043 是一种天然 USP1/UAF1 复合物的抑制剂,IC50 为 544 nM。

Cell lines

K562 cells

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

0, 0.5, 1, 1.5, 2, 5 and 10 μM; 24 hrs

Applications

In K562 cells, SJB2-043 decreased USP1 levels in a dose-dependent way and caused degradation of the ID1 protein, which resulted from proteasomal degradation.

产品描述

SJB2-043 is a novel and potent inhibitor of USP1 with IC50 value of 0.544 μM [1].

Ubiquitin-specific protease 1 (USP1) is a deubiquitinating enzyme (DUB) and is a member of the ubiquitin-specific processing (UBP) family of proteases. It deubiquitinates a protein in the DNA repair pathway of the Fanconi anemia (FA) [1].

In the K562 cell line, SJB2-043 decreased USP1 levels in a dose-dependent way and caused degradation of the ID1 protein, which resulted from proteasomal degradation. Also, SJB2-043 decreased the levels of ID2 and ID3 proteins. Importantly, knockdown of USP1 inhibited cell growth and increased apoptosis. In primary AML cells, SJB2-043 inactivated USP1 and promoted ID 1 degradation. In primary human cord blood CD34+ cells, SJB2-043 in low micromolar levels inhibited cell growth. In HeLa cells, SJB2-043 increased the levels of Ub-FANCD2 and Ub-PCNA. And deubiquitination of FANCD2 is an important step in the BRCA/Fanconi anemia (FA) DNA repair pathway [1].

Reference:
[1].  Helena Mistry, Grace Hsieh, Sara S, et al. Buhrlage, et al. Small molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol Cancer Ther, 2013, 12(12): 2651-2662.