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NSC23766 | Rac1 GTPase inhibitor

CAS:
733767-34-5
Catalog Number:
10-2731
Activity:
Rac1 GTPase inhibitor
Chemical Names:
N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride
Molecular Weight:
530.98
Molecular Formula:
C24H35N7·3HCl
Solubility:
Soluble in DMSO (50 mg/ml); Water (50 mg/ml)
Physical Properties:
White solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
Room temperature
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

NSC23766 (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, 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.

References/Citations:

  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 endocytosis 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
NSC23766 | Rac1 GTPase inhibitor is also available in the Cellular Metabolism Library.
CAS:
733767-34-5
Catalog Number:
10-2731
Activity:
Rac1 GTPase inhibitor
Chemical Names:
N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride
Molecular Weight:
530.98
Molecular Formula:
C24H35N7·3HCl
Solubility:
Soluble in DMSO (50 mg/ml); Water (50 mg/ml)
Physical Properties:
White solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
Room temperature
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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