NSC 23766

Short Summary : Selective inhibitor of Rac1-GEF interaction.

Category : Cell Cycle/Checkpoint|Rho

Purity : 0.9857

CAS Number : 1177865-17-6

Formula : C24H35N7.3HCl

Molecular Weight : 530.96

SMILE : CCN(CC)CCCC(C)NC1=NC(=CC(=N1)NC2=CC3=C(C=C2)N=C(C=C3N)C)C

Solubility : >26.6mg/mL in DMSO

Storage : Store at -20°C

Description : NSC-23766 is a specific inhibitor of Rac with IC50 of 50M.NSC-23766 blocks the activation of Rac 1 through binding the GEFs including Trio and Tiam 1 [1]. In human dermal microvascular endothelial cells, NSC-23766 decreased trans-endothelial electrical resistance and caused the intercellular gap formation. Inhibition of Rac 1 by NSC-23766 shortly reduced endothelial barrier functions as revealed by measurement of TER and the appearance of intracellular gaps [2]. In the mucous cell of the intestine, inhibition of Rac1 either by NSC-23766 protected cells from TNF–induced apoptosis by inhibiting caspase-3, -8 and -9 activities. Inhibition of Rac1 significantly prevented TNF–induced activation of JNK1/2, but did not modulate TNF–induced ERK1/2, Akt and p38 MAPK activity [3].References:[1]. Gao Y, Dickerson JB, Guo F, Zheng J, Zheng Y. Rational design and characterization of a Rac GTPase-specific small molecule inhibitor. Proc Natl Acad Sci U S A. 2004 May 18;101(20):7618-23. [2]. Baumer Y, Spindler V, Werthmann RC, Bnemann M, Waschke J. Role of Rac 1 and cAMP in endothelial barrier stabilization and thrombin-induced barrier breakdown. J Cell Physiol. 2009 Sep;220(3):716-26. [3]. Jin S1, Ray RM, Johnson LR. Rac1 mediates intestinal epithelial cell apoptosis via JNK. Am J Physiol Gastrointest Liver Physiol. 2006 Dec;291(6):G1137-47.

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