1-NM-PP1

• CAT Number: I002695
• CAS Number: 221244-14-0
• Molecular Formula: C20H21N5
• Molecular Weight: 331.4
• Purity: ≥95%
• Synonyms: 1-tert-butyl-3-(naphthalen-1-ylmethyl)pyrazolo[3,4-d]pyrimidin-4-amine
• Target: Src
• Solubility: DMSO: ≤ 27.5 mg/mL
• Storage: Store at -20C
• IC50: 4.2 nM (v-Src-as1 I338G) [1]
• InChI: InChI=1S/C20H21N5/c1-20(2,3)25-19-17(18(21)22-12-23-19)16(24-25)11-14-9-6-8-13-7-4-5-10-15(13)14/h4-10,12H,11H2,1-3H3,(H2,21,22,23)
• InChIKey: GDQXJQSQYMMKRA-UHFFFAOYSA-N
• SMILES: NC1=NC=NC2=C1C(CC3=CC=CC4=C3C=CC=C4)=NN2C(C)(C)C

1-NM-PP1 (CAT: I002695), also known as PP1 Analog II, is a cell-permeable compound with significant implications in kinase inhibition. It serves as a potent and selective inhibitor of mutant kinases compared to their wild-type counterparts. Notably, 1-NM-PP1 effectively targets and inhibits the activity of mutant kinases, such as v-Src (IC50 = 28 μM) and v-Src-as1 I338G (IC50 = 4.2 nM). This inhibitor’s selectivity for mutant kinases over wild-type forms underscores its potential importance in cancer research and personalized medicine, where targeting specific kinase mutations can offer innovative therapeutic strategies for disease treatment and intervention.

Reference

[1]. Papa FR, et al. Bypassing a kinase activity with an ATP-competitive drug. Science. 2003 Nov 28;302(5650):1533-7.
[2]. Larochelle S, et al. Requirements for Cdk7 in the assembly of Cdk1/cyclin B and activation of Cdk2 revealed by chemical genetics in human cells. Mol Cell. 2007 Mar 23;25(6):839-50.