NSC23766
Rac1 GTPase inhibitor / NSC-23766 is a selective inhibitor of Rac1-GEF interaction. Prevents Rac1 activation by Rac-specific guanine nucleotide exchange factors (GEFs) Trio and Tiam1 (IC50 ca. 50 μM) with no effect on the closely related Cdc42 or RhoA. In cells, it blocks serum or PDGF-induced Rac-1 activation and lamellipodia formation. NSC-23766 suppressed the growth of wild-type NIH 3T3 cells but was inactive in cells expressing the constitutively active Rac1 mutant, L61Rac1.1 It is a useful tool to probe the involvement of Rac1 in cell signalling.2 Off target effect: antagonist at muscarinic acetylcholine receptors.3 Cell permeable.
Biochemicals & reagents
733767-34-5
1) Gao et al. (2004), Rational design and characterization of a RAc GTPase-specific small molecule inhibitor; Proc. Natl. Acad. Sci. USA, 101 7618 2) Shankar et al. (2013), Raft endocytisus of AMF regulates mitochondrial dynamics through Rac1 signaling and the Gp78 ubiquitin ligase; J. Cell Sci., 126 3295 3) Levay et al. (2013), NSC23766, a widely used inhibitor of Rac1 activation, additionally acts as a competitive antagonist at muscarinic acetylcholine receptors; J. Pharmacol. Exp. Ther., 347 69
RT
TARGET: GTPase; GPCR -- PATHWAY: ACh (Acetylcholine) signaling -- RESEARCH AREA: Stem cells; Angiogenesis -- DISEASE AREA: Cancer