Molecular Weight(MW): 530.96
NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.
Cited by 12 Publications
6 Customer Reviews
MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
Science, 2018, 11(528), doi: 10.1126/scisignal.aao6897. NSC 23766 purchased from Selleck.
IPEC-J2 cells were treated with PBS, 20 μg/ml CWA, 50 μM NSC 23766 (specific Rac1 inhibitor), or 20 μg/ml CWA with 50 μM NSC 23766 for 12 h. (C) Then, the IPEC-J2 cells were collected for Western blot analysis. (D) Alternatively, after washing with D-Hanks'solution, the IPEC-J2 cells were infected with 1 × 106 CFU of EHEC O157:H7 for 1 h and then washed with PBS. The cells were then collected for colony counting.
J Immunol, 2017, 198(4):1696-1705. NSC 23766 purchased from Selleck.
Effects of inhibitor of Rac1 on regulating NF-κB, PARP-1, p-AMPK andp-p70S6K in GFP-ART1 CT26 cells under starvation-induced conditions. The expressions of PARP-1 and p-AMPK reduce and the expression of p-p70S6K increase in the GFP-ART1 CT26 cells which treated with NSC23766.
Am J Cancer Res, 2015, 5(2): 498-513. NSC 23766 purchased from Selleck.
Effects of PMA and radiation on the subcellular distribution of Rac1 in CNE-1 cells. After different treatments, CNE-1 cells were immediately washed with PBS and fixed for immunofluorescence analysis under a confocal microscope. The red arrows indicate where Rac1 was recruited to the protruding edge of CNE-1 cells. The nuclei are stained blue by DAPI and the Rac1 protein are indicated in green. Original magnification 600×, scale bar=50 μm.
Radiat Res, 2016, 185(6):638-46. . NSC 23766 purchased from Selleck.
SH3BP1 activates Rac1 to promote Wave2 expression in cervical cancer cells (A) and (C) Rac1 activity in HeLa and Caski cells in response to co-processing SH3BP1 overexpression and Rac1 inhibitor NSC 23766 was determined using GST-pull down assays. (B) and (D) Wave2 protein levels in HeLa and Caski cells in response to co-processing SH3BP1 overexpression and Rac1 inhibitor NSC 23766 were determined using Western blot assays. The data are presented as mean ± SD of three independent experiments. *P<0.05, **P<0.01, compared to SH3BP1 (-) + NSC 23766 (-) group; ##P<0.01, compared to SH3BP1 (+) + NSC 23766 (-) group.
J Cell Biochem, 2018, 119(2):1733-1745. NSC 23766 purchased from Selleck.
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Choose Selective Rho Inhibitors
|Description||NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.|
NSC23766 is identified to fit into a surface groove of Rac1 known to be critical for GEF specification. NSC23766 effectively inhibits Rac1 binding and activation by the Rac-specific GEF Trio or Tiam1 in a dose-dependent manner without interfering with the closely related Cdc42 or RhoA binding or activation by their respective GEFs or with Rac1 interaction with BcrGAP or effector PAK1.  NSC 23766 is active in regulating Rac GTPase functions on cytoskeleton and many cell functions including cell cycle, cell growth, adhesion, migration and gene transcription. NSC 23766 (50 μM) potently blocks serum or platelet-derived growth factor-induced Rac1 activation and lamellipodia formation without affecting the activity of endogenous Cdc42 or RhoA in NIH 3T3 cells. NSC 23766 reduces Trio or Tiam1 but not Vav, Lbc, Intersectin, or a constitutively active Rac1 mutant-stimulated NIH 3T3 cells growth and suppresses Trio, Tiam1, or Ras-induced cell transformation. NSC23766 dose-dependently inhibits PC-3 cells proliferation and anchorage-independent growth. 25 μM NSC23766 inhibits the PC-3 cell invasion through Matrigel by 85%.  50 μM NSC 23766 inhibits thrombin-induced activation of Rac1 an d Rac2 in human platelets, as well as platelet aggregation.  NSC23766 prevents Aβ40 and Aβ42 production in swAPP-HEK293cells without affecting Notch and sAPPα. NSC23766 prevents γ-secretase activity in cell, but not act as a direct γ-secretase inhibitor. NSC23766 dose-dependently reduces levels of secreted and intracellular Aβ40 with IC50 of 48.94 μM. 50 μM NSC 23766 inhibits release of Aβ42 by 57.97%.  NSC23766 regulates endothelial nitric oxide synthase expression and endothelial function. 100 μM NSC23766 represses the eNOS promoter activity by 60% in bovine aortic ECs and by 30% to 35% in bEND.3 cells. Inhibition of Rac1 with NSC23766 destabilizes eNOS mRNA and shortens its half-life to 17 hours. NSC23766 dose-dependently attenuates ACh-induced relaxation of wild-type mice aortic rings.  NSC23766 inhibits cell growth and induces apoptosis. NSC23766 decreases MDA-MB-468 and MDA-MB-231 cells viability in a dose-dependent manner with IC50 of ~10 μM, which is not correlated with the status of estrogen receptor (ER), progesterone receptor (PR), Her2, and p53 mutation. NSC23766 has little effect on the survival of the MCF12A normal mammary epithelial cells. After 24 hours expose to NSC 23766, MDA-MB-231 cells showes an increase from 41% to 65% in G1 phase and a concomitant decrease in S and G2-M phases. 100 μM NSC23766 induces a six-fold increase of apoptotic MDA-MB-468. The inhibition of NSC23766 on cell cycle arrest or apoptosis in breast cancer cells is mediated by downregulation of cyclin D1, survivin, and X-linked inhibitor of protein apoptosis. 
|In vivo||NSC23766 induces mobilization of hematopoietic stem cells/progenitors. Intraperitoneal administration of NSC23766 (2.5 mg/kg) into the ‘‘poorly mobilizing ’’ C57Bl/6 mouse strain leads to a two-fold increase in circulating hematopoietic stem cells/progenitors 6 hr after injection.  NSC23766 alleviates lipopolysaccharide-induced acute pulmonary injury in mice. Treatment with NSC23766 at 1 or 3mg/kg not only reduces the inflammatory cells infiltration and MPO activities, but also inhibits pro-inflammatory mediators, tumor necrosis factor-α and interleukin-1β, mRNA expression. NSC23766 also reduces Evans Blue and albumin accumulation in LPS-challenged lungs. |
Rho GTPase activity assay:Cells are grown in log phase in a 10-cm dish, and are starved in 0.5% serum medium or indicated otherwise for 24 h before lysis in a buffer containing 20 mM Tris HCl (pH 7.6), 100 mM NaCl, 10 mM MgCl2, 1% Nonidet P-40, 10% glycerol, and 1× protease inhibitor mixture. Lysates are clarified, the protein concentrations are normalized, and the GTP-bound Rac1 in the lysates is measured by an effector domain pull-down assay. For the His6-PAK1 PBD pull-down assay, cell lysates are incubated with Ni2+-agarose-immobilized His6-PAK1 PBD domain (∼1 μg each) purified from E. coli for 30 min. The Ni2+-agarose co-precipitates are washed twice in the wash buffer and analyzed by immunoblotting with anti-Rac1 monoclonal antibody.
-  Gao Y, et al. Proc Natl Acad Sci U S A, 2004, 101(20), 7618-7623.
-  Akbar H, et al. Methods Enzymol, 2006, 406, 554-565.
-  Désiré L, et al. J Biol Chem, 2005, 280(45), 37516-3
|In vitro||DMSO||100 mg/mL warmed (188.33 mM)|
|Water||100 mg/mL warmed (188.33 mM)|
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