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NSC-23766 | Rac1 GTPase inhibitor

NSC-23766 (733767-34-5) 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, L61Rac11. It is a useful tool to probe the involvement of Rac1 in cell signalling2. Off target effect: antagonist at muscarinic acetylcholine receptors3. Cell permeable.

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

Focus Biomolecules cell signaling supplier, chemical structure of NSC-23766 | Rac1 GTPase inhibitor | CAS 733767-34-5

Catalog#  10-2731

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Catalog Number:
Rac1 GTPase inhibitor
Chemical Name:
N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrocholoride
Molecular Weight:
Molecular Formula:
C24H,sub>35N7 3HCl
Soluble in DMSO (up to 50 mg/ml) or in Water (up to 50 mg/ml).
Physical Properties:
White solid
98% by TLC
NMR (Conforms)
Storage Temperature:
Stable for 1 year as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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