|(R)-N-((S)-3,3-二甲基-1-(甲胺基)-1-氧代丁烷-2-基)-2-((S)-1-(N-羟基甲酰胺基)乙基)-5-苯基戊酰胺|CsnPharm

CAS No.: 260264-93-5

GI254023X Catalog No. CSN19851

Synonyms: GI4023;SRI028594

GI 254023X is a potent and selective ADAM10 metalloproteinase inhibitor.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述GI254023X is a selective ADAM10 inhibitor with IC50 value of 5.3nM, more than 100-fold higher potency than ADAM17. Also, it exhibits inhibition of MMP9 and MMP13 with IC50 values of 2.5nM and 1.1nM, respectively. GI254023X inhibited constitutive shedding of IL6R (in IL6R expressing THP-1 cells), CX3CL1 and CXCL16 (in COS-7 cells transfected to express either CX3CL1 or CXCL16) with IC50 values of 1.5μM, 0.4μM and 1.8μM, respectively, but with much less potency to the inducible shedding of these chemokines. Addition of GI254023X at 5μM significantly decreased invasion of BT20, MDA-MB-453 and MDA-MB-231 cells post 5 days. Pre-treatment of A549 cells with GI254023X at 20μM abrogated E-cadherin cleavage caused by toxin-induced ADAM10 metalloprotease hyperactivity, as well as impaired toxin binding and oligomerization on A549 cells. And this effect on E-cadherin could also be observed in vivo through administration of GI254023X at ~200mg/kg, i.p., daily, in mice.
作用机制GI254023X has an improved fit to the specificity pocket of ADAM10 as compared to that of ADAM17.
参考文献

[1] Inoshima et al (2011) A Staphylococcus aureus pore-forming toxin subverts the activity of ADAM10 to cause lethal infection in mice. Nat.Med. 17 1310.
[2] Moss et al (2007) The ADAM10 prodomain is a specific inhibitor of ADAM10 proteolytic activity and inhibits cellular shedding events. J.Biol.Chem. 282 35712.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5542 mL
- 12.7712 mL
- 25.5425 mL
- 5 mM
- 0.5108 mL
- 2.5542 mL
- 5.1085 mL
- 10 mM
- 0.2554 mL
- 1.2771 mL
- 2.5542 mL

技术信息

CAS号

260264-93-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H33N3O4

运输

蓝冰

分子量

391.50

别名

GI4023;SRI028594

溶解度

DMSO	375.0 mg/mL (957.8 mM)
Water	insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

GI254023X Catalog No. CSN19851

靶点选择性

请登录您的专属账户

确认信息