NVS-PAK1-1

Synonym(s):(S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide

CAS NO.：1783816-74-9
Empirical Formula: C23H25ClF3N5O
Molecular Weight: 479.93
MDL number: MFCD30723183
Update Date: 2024-11-19 23:02:33

What is NVS-PAK1-1?

The Uses of NVS-PAK1-1

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

storage

Store at -20°C

Properties of NVS-PAK1-1

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

Safety information for NVS-PAK1-1

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P271:Use only outdoors or in a well-ventilated area. P280:Wear protective gloves/protective clothing/eye protection/face protection. P312:Call a POISON CENTER or doctor/physician if you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P304+P340:IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P332+P313:IF SKIN irritation occurs: Get medical advice/attention.