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WP1130

WP1130 更多供应商
公司名称: 上海波以尔化工有限公司  
联系电话:
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: 021-20908456
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: 16314854226
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:Degrasyn, also known as WP1130, is a small molecule that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogen
公司名称: Wuhan NCE Biomedical Co.,Ltd.  
联系电话: 4000-027-021 |24 hour enquiry :+86-13986109188 |English:+86-15623472865 |Japanese:+81-08033611988
产品介绍: 英文名称:WP1130
CAS:856243-80-6
纯度:99% HPLC 包装信息:50Mg,100Mg,500Mg,1g,5g,10g,50g,100g,500g,1kg 备注:XYA0004
最新发布供应信息
Bcr-Abl自身活化抑制剂(去泛素化酶抑制剂)(WP1130)_上海泽叶生物科技有限公司
2021/8/3 13:22:00
WP1130 (Degrasyn)_南京百鑫德诺生物科技有限公司
2020/3/30 13:12:37
WP1130
生物活性体外研究体内研究特征生物活性靶点体外研究体内研究 MSDS 用途与合成方法 WP1130价格(试剂级) 上下游产品信息
中文名称:WP1130
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;BCR-ABL自身活化抑制剂(去泛素化酶抑制剂)(WP1130);化合物DEGRASYN
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;WP1130;WP 1130;WP-1130;CS-701;DEGRASYN; WP 1130; WP-1130;Degrasyn;Degrasyn (WP1130);WP1130 ( Degrasyn )
CAS号:856243-80-6
分子式:C19H18BrN3O
分子量:384.27
EINECS号:604-604-1
相关类别:细胞生物学试剂;小分子抑制剂,天然产物;Inhibitor;Inhibitors
Mol文件:856243-80-6.mol
WP1130
WP1130 性质
密度 1.358
WP1130 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.
生物活性Degrasyn (WP1130)是一种选择性deubiquitinase (DUB: USP5,UCH-L1,USP9x,USP14,和 UCH37)抑制剂,对Bcr/Abl也有抑制作用,也是一种JAK2传感器(不影响20S蛋白酶体)和转录激活剂(STAT)。Degrasyn (WP1130)可诱导凋亡而阻滞自噬。
靶点
TargetValue
DUB
(Cell-free assay)
Bcr-Abl
(Cell-free assay)
1.8 μM
体外研究

除了诱导快速的Bcr/Abl下调而不影响Bcr或c-Abl,WP1130也会调节Jak2和c-Myc的稳定性,而不影响其他激酶(HER1,HER2,c-Kit,FAK,ERK1,ERK2,Akt,Btk,Src 和Src相关的激酶)或转录因子(野生型p53,STAT1,STAT3,STAT5,c-Jun,NF-κB,和Max)。不同于adaphostin 和Trisenox,WP1130在60分钟内诱导Bcr/Abl下调。与正常CD34在MM-1多发性骨髓瘤和其他肿瘤细胞系中,WP1130诱导快速的蛋白酶体依赖性c-Myc蛋白降解,与肿瘤生长的抑制相关。不同于AG490,WP1130作为一种部分选择性去泛素化酶(DUB)抑制剂,诱导快速显著的多泛素化(K48/K63连接)蛋白聚集到似核状聚集体,而不影响蛋白酶体活性。WP1130 (5 μM)直接抑制除UCH-L3外的USP9x,USP5,USP14,UCH-L1,和UCH37的DUB活性,导致抗细胞凋亡的下调和促细胞凋亡蛋白质,比如MCL-1和p53的增加。

体内研究WP1130给药抑制移植到裸鼠体内的K562肿瘤,以及野生型Bcr/Abl 和T315I突变体Bcr/Abl表达的BaF/3细胞的生长。与c-Myc的下调一致,WP1130对裸鼠体内已建立的A375黑色素瘤表现出有效的抑制作用。
安全信息
WP1130 价格(试剂级)
更新日期产品编号产品名称CAS编号包装价格
2021/06/02S2243Degrasyn (WP1130)856243-80-65mg1379.43元
2021/06/02S2243Degrasyn (WP1130)856243-80-610mM (1mL in DMSO)2121.61元
"WP1130" 相关产品信息()
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