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NVS-PAK1-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NVS-PAK1-1图片
CAS NO:1783816-74-9
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 479.93
Formula C23H25ClF3N5O
CAS No. 1783816-74-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥125 mg/mL
Water: <1 mg/mL
Ethanol:
SMILES Code O=C(N1C[C@@H](NC2=NC3=CC(F)=CC=C3N(CC(F)F)C4=CC=C(Cl)C=C42)CC1)NC(C)C
Synonyms NVS-PAK1-1; NVSPAK11; NVS PAK1 1
实验参考方法
In Vitro

In vitro activity: NVS-PAK1-1 is a a specific allosteric PAK1 inhibitor discovered in a fragment-based screen. The discovery of inhibitors targeting novel allosteric kinase sites is very challenging. Such compounds, however, once identified could offer exquisite levels of selectivity across the kinome. 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 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases.


Kinase Assay: 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 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases.


Cell Assay: 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.

In Vivo NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t1/2 in RLM 3.5 min)
Animal model
Formulation & Dosage
References ACS Med Chem Lett. 2015 May 22;6(7):776-81.