An allosteric inhibitor of PAK1
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NVS-PAK1-1

Item No. 19964

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3S)-3-[[2-chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-yl]amino]-N-(1-methylethyl)-1-pyrrolidinecarboxamide
CAS Number
1783816-74-9
Molecular Formula
C23H25ClF3N5O
Formula Weight
479.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 50 mg/mlEthanol: 20 mg/ml
λmax
264 nm
SMILES
FC(F)CN1C2=C(C=C(Cl)C=C2)C(N[C@H]3CCN(C(NC(C)C)=O)C3)=NC4=C1C=CC(F)=C4
InChi Code
InChI=1S/C23H25ClF3N5O/c1-13(2)28-23(33)31-8-7-16(11-31)29-22-17-9-14(24)3-5-19(17)32(12-21(26)27)20-6-4-15(25)10-18(20)30-22/h3-6,9-10,13,16,21H,7-8,11-12H2,1-2H3,(H,28,33)(H,29,30)/t16-/m0/s1
InChi Key
OINGHOPGNMYCAB-INIZCTEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $134

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    10 mg

    $240

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    25 mg

    $530

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    Product Description

    NVS-PAK1-1 is an allosteric inhibitor of p21-activated kinase 1 (PAK1), a non-receptor serine/threonine kinase involved in tumorigenesis (Kd = 7 nM).1 It has an IC50 value of 5.2 nM in a PAK1 dephosphorylation assay. NVS-PAK1-1 is selective for PAK1 over PAK2 (Kd = 400 nM) and over a panel of 442 kinases, where it did not inhibit any other kinases by greater than 80%.1,2 It inhibits phosphorylation of MEK Ser289 when used at concentrations ranging from 6 to 20 µM but does not inhibit proliferation of Su86.86 cells at concentrations lower than 2 µM.1 See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Karpov, A.S., Amiri, P., Bellamacina, C., et al. Optimization of a dibenzodiazepine hit to a potent and selective allosteric PAK1 inhibitor. ACS Med. Chem. Lett. 6(7), 776-781 (2015).

    2. Semenova, G., and Chernoff, J. Targeting PAK1. Biochem. Soc. Trans. 45(1), 79-88 (2017).