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中文名称:

NULL

中文同义词:

PAK1变构抑制剂(NVS-PAK1-1)

英文名称:

NVS-PAK1-1

英文同义词:

NVS-PAK1-1;(3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide;NVS-PAK1-1;NVS-PAK11;NVS-PAK1 1;1-Pyrrolidinecarboxamide, 3-[[2-chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-yl]amino]-N-(1-methylethyl)-, (3S)-;NVS-PAK1-1 >=98% (HPLC)

CAS号:

1783816-74-9

分子式:

C23H25ClF3N5O

分子量:

479.93

EINECS号:

相关类别:

细胞生物学试剂;API

Mol文件:

1783816-74-9.mol

沸点 

697.8±55.0 °C(Predicted)

密度 

1.42±0.1 g/cm3(Predicted)

储存条件 

2-8°C

形态

powder

酸度系数(pKa)

14.02±0.40(Predicted)

颜色

white to beige

生物活性

NVS-PAK1-1是有效，选择性的 PAK1 变构抑制剂，IC50值为5 nM。

靶点

IC50: 5 nM (PAK1)

体外研究

NVS-PAK1-1 demonstrates high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 K d of 7 nM and a PAK2 K d of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved.

体内研究

NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t 1/2 in RLM 3.5 min).