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SJB2-043

现货
Catalog No.
A3823
USP1抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,560.00
Ship with 10-15 days
5mg
¥ 2,330.00
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10mg
¥ 3,550.00
Ship with 10-15 days
25mg
¥ 5,140.00
Ship with 10-15 days
50mg
¥ 8,410.00
Ship with 10-15 days

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt275.26
Cas No.63388-44-3
FormulaC17H9NO3
Solubility≥6.7 mg/mL in DMSO, <2.61 mg/mL in EtOH, <2.39 mg/mL in H2O
Chemical Name2-phenylbenzo[f][1,3]benzoxazole-4,9-dione
SDFDownload SDF
Canonical SMILESC1=CC=C(C=C1)C2=NC3=C(O2)C(=O)C4=CC=CC=C4C3=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

K562细胞

制备方法

可溶于DMSO。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

0、0.5、1、1.5、2、5和10 μM;24小时

实验结果

在K562细胞中,SJB2-043降解蛋白酶体,从而呈剂量依赖性地降低USP1水平并引起ID1蛋白降解。

References:

[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.

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