Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 44.00 | |
5 mg | In stock | $ 97.00 | |
10 mg | In stock | $ 177.00 | |
25 mg | In stock | $ 387.00 | |
50 mg | In stock | $ 579.00 | |
100 mg | In stock | $ 828.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 97.00 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (260.45 mM)
You can also refer to dose conversion for different animals. More
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