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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-WP1130
WP1130

Chemical Structure : WP1130

CAS No.: 856243-80-6

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WP1130 (Degrasyn, WP-1130)

货号: PC-43444Not For Human Use, Lab Use Only.

WP1130 (Degrasyn) is a small molecule that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression (IC50=1.8 uM), also inhibits deubiquitinases and blocks autophagy.

规格 价格 库存 数量
5 mg ￥580 In stock
10 mg ￥880 In stock
25 mg ￥1380 In stock
50 mg ￥2180 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

WP1130 (Degrasyn) is a small molecule that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression (IC50=1.8 uM), inhibits deubiquitinases USP9x, USP5, USP14, and UCH37 and blocks autophagy.
WP1130 reduces leukemic versus normal hematopoietic colony formation and strongly inhibits colony formation of cells derived from patients with T315I mutant Bcr/Abl-expressing CML in blast crisis.
WP1130 suppresses the growth of K562 heterotransplanted tumors as well as both wild-type Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells in vivo.
WP1130 acts as a partly selective DUB inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37, triggers aggresome formation and tumor cell apoptosis.

物理化学性质&存储条件

分子量 384.27
分子式 C19H18BrN3O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 33 mg/mL
Chemical Name/SMILES

2-Propenamide, 3-(6-bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-, (2E)-

参考文献

1. Bartholomeusz GA, et al. Blood. 2007 Apr 15;109(8):3470-8.

2. Bartholomeusz G, et al. Cancer Res. 2007 Apr 15;67(8):3912-8.

3. Kapuria V, et al. Cancer Res. 2010 Nov 15;70(22):9265-76.

4. Drießen S, et al. Autophagy. 2015;11(9):1458-70.

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