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经验配方 C₁₉H₁₈BrN₃O 描述 概述 A cell-permeable tyrphostin compound that acts as a partially selective deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway. Reported to cause accumulation of polyubiquitinated p53, JAK2 and Bcr-Abl, and reduce c-Myc and MCL-1 protein levels in several tumor cells and downregulate Stat3 and NF-κB activities (IC50 < 1 µM in MCL cells) leading to tumor cell apoptosis (IC50 ~1.2 µM in Z138 cells). Suggested to modify active site cysteine of DUB and inhibit USP5, UCH-L1, USP9x, USP14, and UCH37 activities (≥80% inhibition at 5 µM) without affecting 20S proteasome. Reported to exert stronger antiproliferative and antitumor properties than STAT3 Inhibitor III, WP1066 (Cat. No. 573097) in xenograft mouse models of CML and melanoma. 产品目录编号 681685 品牌系列 Calbiochem®
同义词 Degrasyn 参考 参考 Kapuria, V., et al. 2010. Cancer Res. 70, 9265.
Pham, L.V., et al. 2010. Mol. Cancer Ther. 9, 2026.
Bartholomeusz, G.A, et al. 2007. Cancer Res. 67, 3912.
Bartholomeusz, G.A, et al. 2007. Blood 109, 3470.产品信息 形式 Light yellow solid Hill配方 C₁₉H₁₈BrN₃O 化学配方 C₁₉H₁₈BrN₃O Molar Mass 384.3 结构配方图像 生物信息 纯度 ≥97% by HPLC 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
毒性 Standard Handling
储存 +2°C to +8°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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