| Identification | Back Directory | [Name]
NVS-PAK1-1 | [CAS]
1783816-74-9 | [Synonyms]
NVS-PAK1-1
NVS-PAK1-1 >=98% (HPLC)
NVS-PAK1-1;NVS-PAK11;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
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)- | [Molecular Formula]
C23H25ClF3N5O | [MDL Number]
MFCD30723183 | [MOL File]
1783816-74-9.mol | [Molecular Weight]
479.93 |
| Chemical Properties | Back Directory | [Boiling point ]
697.8±55.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMF: 50 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 50 mg/ml; Ethanol: 20 mg/ml | [form ]
powder | [pka]
14.02±0.40(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
NVS PAK1 1 is one of potent and selective allosteric PAK1 inhibitors. | [Biochem/physiol Actions]
NVS-PAK1-1 is a potent allosteric inhibitor of p21-activated kinase PAK1, a serine-threonine kinase that is upregulated in many cancers. 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. For full characterization details, please visit the NVS-PAK1-1 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc | [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)[1]. | [storage]
Store at -20°C |
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Sigma-Aldrich
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https://www.sigmaaldrich.cn |
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