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NSC 23766 (hydrochloride)

Cayman Chemical Item Number 13196

(CAS 1177865-17-6)

NSC 23766 (hydrochloride) (CAS 1177865-17-6)

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Description

Rac1 is a GTPase that is involved in the regulation of the cell cycle, cell-cell adhesion, motility, and differentiation.1 Rac1 is activated by its interaction with specific guanine nucleotide exchange factors (GEFs). NSC23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 μM).2 It has no effect on the closely related GTPases, Cdc42, and RhoA. NSC 23766 has been used to investigate the role of Rac1 in such diverse cellular functions as stem cell mobilization, epithelial cell migration, angiogenesis, leukemia cell migration and growth, and gene expression.3,4,5,6,7

1 Bosco, E.E., Mulloy, J.C., and Zheng, Y. Rac1 GTPase: A “Rac” of all trades. Cell Mol Life Sci 66 370-374 (2009).

2 Gao, Y., Dickerson, J.B., Guo, F., et al. Rational design and characterization of a Rac GTPase-specific small molecule inhibitor. Proc Natl Acad Sci USA 101(20) 7618-7623 (2004).

3 Cancelas, J.A., Lee, A.W., Prabhakar, R., et al. Rac GTPases differentially integrate signals regulating hematopoietic stem cell localization. Nat Med 11(8) 886-891 (2005).

4 Rao, J.N., Liu, S.V., Zou, T., et al. Rac1 promotes intestinal epithelial restitution by increasing Ca2+ influx through interaction with phospholipase C-γ1 after wounding. Am J Physiol Cell Physiol 295 C1499-C1509 (2008).

5 Sawada, N., Salomone, S., Kim, H., et al. Regulation of endothelial nitric oxide synthase and postnatal angiogenesis by Rac1. Circ Res 103 360-368 (2008).

6 Wang, J., Rao, Q., Wang, M., et al. Overexpression of Rac1 in leukemia patients and its role in leukemia cell migration and growth. Biochem Biophys Res Commun 386 769-774 (2009).

7 Vallon, M., Rohde, F., Janssen, K., et al. Tumor endothelial marker 5 expression in endothelial cells during capillary morphogenesis is induced by the small GTPase Rac and mediates contact inhibition of cell proliferation. Exp Cell Res 316 412-421 (2010).

Formal Name N6-​[2-​[[4-​(diethylamino)-​1-​methylbutyl]amino]-​6-​methyl-​4-​pyrimidinyl]-​2-​methyl-​4,​6-​quinolinediamine,​ trihydrochloride
CAS Number 1177865-17-6
Molecular Formula C24H35N7 · 3HCl
Formula Weight 531.0
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CC1=NC2=C(C(N)​=C1)​C=C(NC3=NC(NC(C)​CCCN(CC)​CC)​=NC(C)​=C3)​C=C2

Background Reading

Bosco, E.E., Mulloy, J.C., and Zheng, Y. Rac1 GTPase: A “Rac” of all trades. Cell Mol Life Sci 66 370-374 (2009).

Cancelas, J.A., Lee, A.W., Prabhakar, R., et al. Rac GTPases differentially integrate signals regulating hematopoietic stem cell localization. Nat Med 11(8) 886-891 (2005).

Rao, J.N., Liu, S.V., Zou, T., et al. Rac1 promotes intestinal epithelial restitution by increasing Ca2+ influx through interaction with phospholipase C-γ1 after wounding. Am J Physiol Cell Physiol 295 C1499-C1509 (2008).

Wang, J., Rao, Q., Wang, M., et al. Overexpression of Rac1 in leukemia patients and its role in leukemia cell migration and growth. Biochem Biophys Res Commun 386 769-774 (2009).

Vallon, M., Rohde, F., Janssen, K., et al. Tumor endothelial marker 5 expression in endothelial cells during capillary morphogenesis is induced by the small GTPase Rac and mediates contact inhibition of cell proliferation. Exp Cell Res 316 412-421 (2010).

Gao, Y., Dickerson, J.B., Guo, F., et al. Rational design and characterization of a Rac GTPase-specific small molecule inhibitor. Proc Natl Acad Sci USA 101(20) 7618-7623 (2004).

Sawada, N., Salomone, S., Kim, H., et al. Regulation of endothelial nitric oxide synthase and postnatal angiogenesis by Rac1. Circ Res 103 360-368 (2008).

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Size Price Quantity Subtotal
1 mg $53.00 $0.00
5 mg $239.00 $0.00
10 mg $424.00 $0.00
25 mg $928.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-05-26. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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