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CAS No.: 856243-80-6

Degrasyn Catalog No. CSN16658

Synonyms: WP1130

WP1130 is a selective small molecular deubiquitinase (USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and a Bcr/Abl destruction pathway activator with an IC50 of 1.8 μM for K562 cells.

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生物活性

实验方案

技术信息

生物活性

描述WP1130 is a partly selective DUB inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37, which are known to regulate survival protein stability and 26S proteasome function. WP1130 at 5μM induced rapid accumulation of polyubiquitinated (K48/K63-linked) proteins into juxtanuclear aggresomes, without affecting 20S proteasome activity. WP1130-mediated inhibition of tumor-activated DUBs resulted in downregulation of antiapoptotic and upregulation of proapoptotic proteins, such as MCL-1 and p53, in BV173 cells treated by 5μM WP1130 for 4h^[3]. WP1130 at 5μM specifically and rapidly down-regulatef both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells, not requiring the participation of the proteasomal pathway. And this loss of Bcr/Abl protein correlated with the onset of apoptosis and reduced phosphorylation of Bcr/Abl substrates, including p-Stat5 and p-Hck. It was more effective in reducing leukemic versus normal hematopoietic colony formation and strongly inhibited colony formation of cells derived from patients with T315I mutant Bcr/Abl–expressing CML in blast crisis. WP1130 suppressed the growth of K562 heterotransplanted tumors of mice treated with WP1130 at 30mg/kg, i.p., every other day for 9 days^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human A375 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human A375 cells after 72 hrs by MTT assay, IC50=1.7 μM	24457091
human K562 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human K562 cells after 72 hrs by MTT assay, IC50=2.4 μM	24457091
human Mino cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human Mino cells after 72 hrs by MTT assay, IC50=0.8 μM	24457091

更多
动物研究
剂量
Mice: 20 mg/kg^[3] (i.p.), 40 mg/kg^[4] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 20 mg/kg^[3] (i.p.), 40 mg/kg^[4] (i.p.)
给药途径	i.p.

[1] Kapuria V, Peterson LF, et al. Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis. Cancer Res. 2010 Nov 15;70(22):9265-76.
[2] Bartholomeusz GA, Talpaz M, et al. Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. Blood. 2007 Apr 15;109(8):3470-8. Epub 2007 Jan 3.
[3] Kapuria V, Peterson LF, Fang D, Bornmann WG, Talpaz M, Donato NJ. Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis. Cancer Res. 2010 Nov 15;70(22):9265-76. doi: 10.1158/0008-5472.CAN-10-1530. Epub 2010 Nov 2. PMID: 21045142.
[4] Bartholomeusz GA, Talpaz M, Kapuria V, Kong LY, Wang S, Estrov Z, Priebe W, Wu J, Donato NJ. Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. Blood. 2007 Apr 15;109(8):3470-8. doi: 10.1182/blood-2006-02-005579. Epub 2007 Jan 3. PMID: 17202319; PMCID: PMC1852235.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6023 mL
- 13.0117 mL
- 26.0234 mL
- 5 mM
- 0.5205 mL
- 2.6023 mL
- 5.2047 mL
- 10 mM
- 0.2602 mL
- 1.3012 mL
- 2.6023 mL

技术信息

CAS号

856243-80-6

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H18BrN3O

运输

蓝冰

分子量

384.27

别名

WP1130

溶解度

DMSO	76.0 mg/mL (197.8 mM)
Water	Insoluble
Ethanol	18.0 mg/mL (46.8 mM)

动物实验配方

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human A375 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human A375 cells after 72 hrs by MTT assay, IC50=1.7 μM	24457091
human K562 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human K562 cells after 72 hrs by MTT assay, IC50=2.4 μM	24457091
human Mino cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human Mino cells after 72 hrs by MTT assay, IC50=0.8 μM	24457091
human MM1 cells	-	Function assay	24 to 72 hrs	Antitumor activity against human MM1 cells after 24 to 72 hrs by MTT assay, IC50=1 μM	22036213
human MM1S cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human MM1S cells after 72 hrs by MTT assay, IC50=1.2 μM	24457091
human OCI-My4 cells	-	Function assay	24 to 72 hrs	Antitumor activity against human OCI-My4 cells after 24 to 72 hrs by MTT assay, IC50=1.5 μM	22036213
human U266 cells	-	Function assay	24 to 72 hrs	Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay, IC50=1.3 μM	22036213
human Z138 cells	-	Function assay	1 h	Inhibition of UCH-L1 in human Z138 cells after 1 hr by immunoblotting analysis, IC50=3 μM	23791076
human Z138 cells	1.25 to 5 uM	Function assay	4 h	Inhibition of Usp9x in human Z138 cells using HA-Ub vinyl-sulfone as substrate at 1.25 to 5 uM after 4 hrs by immunoblotting analysis	24457091

Degrasyn Catalog No. CSN16658

靶点选择性

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