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(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺

(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺 更多供应商
公司名称:上海波以尔化工有限公司  
联系电话:86-15221043597
产品介绍:英文名称:WP1130
CAS:856243-80-6
公司名称:上海佰世凯化学科技有限公司  
联系电话:+86(0)21-20908456
产品介绍:英文名称:WP 1130
CAS:856243-80-6
备注:C14609
公司名称:济南精合医药科技有限公司  
联系电话:+86 (531) 88811783;
产品介绍:英文名称:WP1130
CAS:856243-80-6
纯度:99% 包装信息:5Mg, 10Mg, 20Mg, 50Mg
公司名称:BOC Sciences  
联系电话:
产品介绍:英文名称:Degrasyn
CAS:856243-80-6
纯度:>= 98.0% 包装信息:10mg, 100mg 备注:in stock, White solid powder, http://www.bocsci.com/degrasyn-cas-856243-80-6-item-307702.html
公司名称:T&W GROUP  
联系电话:+86-21-61551611, 61551462, 61551420, 61551610
产品介绍:英文名称:Degrasyn (WP1130)
CAS:856243-80-6
纯度:99% 包装信息:100g;500g;1kg;5kg;10kg
(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺
生物活性 体外研究 体内研究 特征
中文名称:(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺
中文同义词:(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺
英文名称:WP1130
英文同义词:WP1130;(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide;Degrasyn;Degrasyn (WP1130);WP1130 ( Degrasyn );(S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide;(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide Degrasyn (WP1130);Degrasyn, >=98%
CAS号:856243-80-6
分子式:C19H18BrN3O
分子量:384.28
EINECS号:
相关类别:Inhibitors;小分子抑制剂,天然产物;Inhibitor
Mol文件:856243-80-6.mol
(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺
(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺 性质
密度 1.358
(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺 用途与合成方法
生物活性Degrasyn (WP1130)是一种选择性的去泛素化酶(DUB: USP5, UCH-L1, USP9x, USP14, UCH37)抑制剂,也抑制Bcr/Abl,也是一种JAK2传感器(不影响20S蛋白酶体)和转录激活剂(STAT)。
体外研究In addition to inducing rapid down-regulation of Bcr/Abl without affecting Bcr or c-Abl, WP1130 also regulates the stability of Jak2 and c-Myc without affecting other kinases (HER1, HER2, c-Kit, FAK, ERK1, ERK2, Akt, Btk, Src and Src-related kinases) or transcription factors (wild-type p53, STAT1, STAT3, STAT5, c-Jun, NF-κB, and Max). Unlike adaphostin and Trisenox, WP1130 induces down-regulation of Bcr/Abl within 60 minutes. WP1130 is more effective in inducing apoptosis of myeloid and lymphoid tumor cells with IC50 of ~0.5-2.5 μM compared with normal CD34+ hematopoietic precursors, dermal fibroblasts, or endothelial cells with IC50 of ~5-10 μM. WP1130 (5 μM) specifically and rapidly down-regulates both wild-type and T315I mutant Bcr/Abl protein without affecting bcr/abl gene expression or engaging the proteasomal degradation pathway in chronic myelogenous leukemia (CML) cells, accompanied by induction of apoptosis. WP1130 is more effective in reducing leukemic cell colony formation compared with normal progenitor cells, and effective against primary leukemic cells harboring the T315I mutation. WP1130 induces rapid proteasomal-dependent degradation of c-Myc protein in MM-1 multiple myeloma and other tumor cell lines, correlated with tumor growth inhibition. Unlike AG490, WP1130 acts as a partly selective deubiquitinase (DUB) inhibitor to induce a rapid and marked accumulation of polyubiquitinated (K48/K63-linked) proteins into juxtanuclear aggresomes without affecting proteasome activity. WP1130 (5 μM) directly inhibits DUB activity of USP9x, USP5, USP14, UCH-L1, and UCH37, but not UCH-L3, resulting in downregulation of antiapoptotic and upregulation of proapoptotic proteins, such as MCL-1 and p53.
体内研究Administration of WP1130 inhibits the growth of K562 tumors as well as both wildtype Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells transplanted into nude mice. Consistent with the down-regulation of c-Myc, WP1130 displays potent inhibitory activity against A375 melanoma tumors established in nude mice.
特征WP1130 has an advantage over imatinib mesylate in that its activity is not inhibited by a variety of Abl kinase mutations, including T315I.
安全信息
"(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺" 相关产品信息
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