货号	规格	价格	上海	北京	珠海	重庆	武汉
S81013-5mg	≥98%	￥410.00 S81013-5mg ￥410.00 现货	7 7	-	-	-	-
S81013-10mg	≥98%	￥730.00 S81013-10mg ￥730.00 现货	8 8	-	-	-	-
S81013-25mg	≥98%	￥1480.00 S81013-25mg ￥1480.00 现货	8 0 8	-	-	-	-
S81013-50mg	≥98%	￥2410.00 S81013-50mg ￥2410.00 现货	6 6	-	-	-	-
S81013-100mg	≥98%	￥3890.00 S81013-100mg ￥3890.00 现货	5 5	-	-	-	-

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产品描述：

Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.

靶点：

IC50: 1.8 μM (Bcr-Abl, in K562, BV-173 cells):Deubiquitinase;Apoptosis; JAK; Bcr-Abl; DUB; Autophagy

体内研究：

Degrasyn suppresses the growth of K562 heterotransplanted tumors as well as both wild-type Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells transplanted into nude mice. To assess the possible therapeutic activity of Degrasyn against CML, nude mice received a subcutaneous transplant with K562 cells and are treated with 30 mg/kg Degrasyn every other day for 9 days after palpable tumor formation (10 days). This dose and schedule are well tolerated and effective in other tumor models. Antitumor activity is compared with that after daily Imatinib mesylate treatment (50 mg/kg). Nineteen days after tumor inoculation, tumors in the control group reached maximum allowable dimension, and the effect of therapy is assessed. Degrasyn treatment suppresses K562 tumor growth to an extent comparable to that observed in imatinib mesylate-treated animals, suggesting that Degrasyn is active in reducing the growth of established K562 tumors

参考文献：

1. Bartholomeusz GA, 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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.602 ml	13.012 ml	26.023 ml
5 mM	0.52 ml	2.602 ml	5.205 ml
10 mM	0.26 ml	1.301 ml	2.602 ml
50 mM	0.052 ml	0.26 ml	0.52 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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