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NVS-PAK1-1

Catalog No. T16367 CAS 1783816-74-9

NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).

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NVS-PAK1-1, CAS 1783816-74-9

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).
Targets&IC50	PAK1:5 nM
In vitro	NVS-PAK1-1 inhibits the proliferation of the Su86.86 cell line only above a concentration of 2 μM, consistent with the observation. NVS-PAK1-1 (6-20 μM) inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Inhibition of downstream signaling, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, and cell proliferation at a significantly lower 0.21 μM concentration is achieved. NVS-PAK1-1 shows 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 displays excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases .
In vivo	NVS-PAK1-1 displays relatively poor stability in rat liver microsomes (RLM). This would limit its application for in vivo studies (t1/2 in RLM 3.5 min).

Molecular Weight	479.93
Formula	C23H25ClF3N5O
CAS No.	1783816-74-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 125 mg/mL (260.45 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Karpov AS, et al. Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett. 2015 May 22;6(7):776-81.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Bioactive Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

NVS-PAK1-1 1783816-74-9 细胞骨架 PAK Inhibitor p21 activated kinases NVS PAK1 1 inhibit NVS-PAK-1-1 NVSPAK11 inhibitor

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