DEGRASYN_化工百科

中文名	Degrasyn (WP1130)
英文名	Degrasyn (WP1130)
别名	化合物DEGRASYN BCR-ABL自身活化抑制剂(去泛素化酶抑制剂)(WP1130) (2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基丁基]-2-丙烯酰胺
英文别名	WP1130 CS-701 WP-1130 WP 1130 Degrasyn WP-1130 WP 1130 DEGRASYN Degrasyn (WP1130) WP1130 ( Degrasyn ) (2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide
CAS	856243-80-6
EINECS	604-604-1
化学式	C19H18BrN3O
分子量	384.27
密度	1.358
溶解度	溶于DMSO (高达45 mg/ml) 或乙醇 (高达25 mg/ml)。
存储条件	-20°
稳定性	从提供的购买之日起稳定2年。在DMSO中的溶液可以在-20 ° 储存长达3个月。
外观	固体
颜色	Yellow
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. 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	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. 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。

DEGRASYN - 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
5 mM	0.052 ml	0.26 ml	0.52 ml

最后更新：2024-01-02 23:10:35

北京索莱宝科技有限公司

现货供应

产品名: Degrasyn 去供应商网站查看询盘
CAS: 856243-80-6
产地: 北京
包装: 盒
规格: ID1270-D-1ml,10mM*1mlinDMSO,ID1270-10mg,10mg,ID1270-5mg,5mg
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上海吉至生化科技有限公司

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产品名: Degrasyn (WP1130) 去供应商网站查看询盘
CAS: 856243-80-6
产地: 中国上海
包装: 50mg
规格: 99%
价格: 6212.00
库存: 5个工作日
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上海麦克林生化科技股份有限公司

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产品名: Degrasyn (WP1130) 去供应商网站查看询盘
CAS: 856243-80-6
产地: 上海
规格: D872457
价格: 1mg-215,10mg-879,5mg-502,25mg-1494,1ml-599
库存: 7天内发货
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上海源叶生物科技有限公司

产品名: Degrasyn (WP1130) 去供应商网站查看询盘
CAS: 856243-80-6
产地: 上海
规格: 99%
价格: 5mg 550,10mg 1000,50mg 4000
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