| 货号:AG-CR1-3551-M001 | 规格:1 mg | 目录价:¥360 |
| 货号:AG-CR1-3551-M005 | 规格:5 mg | 目录价:¥1080 |
产品详情
* 以下信息仅供参考,详情请以原厂网站为准
产品名称:
WP1130
别名:
WPI 130; Degrasyn; (2E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide
产品描述:
WP1130 is a second-generation tyrphostin derivative initially identified as a JAK2 signaling inhibitor through JAK2 ubiquitination that reduces STAT activation stimulated by cytokines (such as IL-6 and IL-3) through the rapid down-regulation of upstream JAK kinases. WP1130 has also been identified as a partially selective cell permeable deubiquitinating enzyme/deubiquitinase (DUB) inhibitor that directly inhibits DUB activity of USP9x, USP5, USP14, USP24, UCH37, UCHL1 and UCHL5, leading to rapid accumulation of polyubiquitinated (K48/K63-linked) proteins into juxtanuclear aggresomes and tumor cell apoptosis, accounting for its anti-cancer properties. Through this mechanism, WP1130 has been shown to downregulate the antiapoptotic proteins Bcr/Abl and Jak2 and to upregulate the proapoptotic proteins MCL-1 and p53. WP1130-induced apoptosis and anti-proliferation in tumor cells have been implicated in the treatment of chronic myelogenous leukemia (CML), melanoma, glioblastoma and myeloproliferative disorders. It has also been shown to inhibit autophagy. WP1130 exhibits antiviral activity through activation of the unfolded protein response (UPR) and is an antibacterial compound against S. aureus including clinically isolated MRSA strains. WP1130 inhibits the LPS/ATP-induced deubiquitination of NLRP3 and further increases NLRP3 ubiquitination. This leads to inhibition of NLRP3 activation, indicating that deubiquitination of NLRP3 by the priming and activation signals is critical for its activation.
保存温度:
+4°C
运输温度:
Ambient
预期分子量:
384.3
产品形式:
solid
产地:
瑞士
纯度:
>95%
CAS号:
856243-80-6
分子式:
C19H18BrN3O
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