NVS-PAK1-1

产品编号: DC10473 Featured
NVS-PAK1-1
结构式
1783816-74-9
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中国地区超过5000个高品质化合物库存
应用领域
NVS-PAK1-1是有效,选择性的 PAK1 变构抑制剂,IC50值为5 nM。
Cas No.: 1783816-74-9
名称:
别名: NVS-PAK1-1,NVS-PAK11,NVS-PAK1 1
SMILES: CC(C)NC(=O)N1CC[C@@H](C1)NC2=NC3=C(C=CC(=C3)F)N(C4=C2C=C(C=C4)Cl)CC(F)F
分子式: C23H25ClF3N5O
分子量: 479.93
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: NVS-PAK1-1 is a potent, allosteric PAK1 inhibitor. It is about 60-fold selective over PAK2. It is highly selective over other kinases in the kinome. It has a submicromolar IC50 in a PAK1 autophosphorylation assay. These features make it a useful tool to assess the impact of PAK1 inhibition in a cellular context. More data would need to be collected, but poor microsomal stability (rat) suggests the compound may not be suitable for use in model organisms (in vivo applications).NVS-PAK1-1 has an IC50 value of 5 nM for dephoshorylated PAK1 and 6 nM for phosphorylated PAK1 in an in vitro dephosphorylation assay. NVS-PAK1-1 showed good selectivity against 442 other kinases including PAK2. NVS-PAK1-1 has generally good physicochemical properties, but was metabolized by rat liver microsomes, so may not be useful for in vivo work.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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