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    NSC-23766 3HCl
    NSC-23766 3HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0012
    CAS #: 1177865-17-6Purity ≥98%

    Description: NSC23766 3HCl, the salt form of NSC23766, is a novel and potent inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; it does not inhibit the closely related targets, Cdc42 or RhoA. NSC23766 disrupted polar secretion of adhesive, polarization of endomembranes, and tip-focused growth in the rhizoid. NSC 23766 (100 μM) treatment effectively inhibits polar body emission in a dose-dependent manner. NSC 23766 (200 μM) increases the percentage of morphologically abnormal spindles of oocytes. In NSC 23766-treated oocytes, the p-MAPK protein expression is significantly decreased.

    References: Proc Natl Acad Sci U S A. 2004 May 18;101(20):7618-23; J Biol Chem. 2005 Nov 11;280(45):37516-25.

    Related CAS: 733767-34-5 (free base)

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    Molecular Weight (MW)530.96
    FormulaC24H35N7.3HCl
    CAS No.1177865-17-6 (HCl)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO:  100 mg/mL (188.3 mM)
    Water: <1 mg/mL
    Ethanol: 100 mg/mL (188.3 mM)
    Other infoChemical Name: N6-(2-((5-(diethylamino)pentan-2-yl)amino)-6-methylpyrimidin-4-yl)-2-methylquinoline-4,6-diamine trihydrochloride
    InChi Key: CPUHORIUXPQCHW-UHFFFAOYSA-N
    InChi Code: InChI=1S/C24H35N7.3ClH/c1-6-31(7-2)12-8-9-16(3)27-24-28-18(5)14-23(30-24)29-19-10-11-22-20(15-19)21(25)13-17(4)26-22;;;/h10-11,13-16H,6-9,12H2,1-5H3,(H2,25,26)(H2,27,28,29,30);3*1H
    SMILES Code: NC1=CC(C)=NC2=CC=C(NC3=NC(NC(CCCN(CC)CC)C)=NC(C)=C3)C=C12.[H]Cl.[H]Cl.[H]Cl
    SynonymsNSC23766; NSC23766; NSC 23766


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    In Vitro

    In vitro activity: 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%. [1] 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.


    Kinase 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.


    Cell Assay: Cells (1.5 × 104/mL Human breast cancer cells MDA-MB-468) are seeded in each well of 96-well tissue culture plates with 200 μL of medium. After 24 hours of plating, the medium is replaced with 200 μL of fresh medium containing NSC23766 at the indicated concentrations. At the end of the treatment period 20 μL of MTS solution are added to each well and incubated at 37 ℃ for 2 hours. Absorbance at 490 nm is read on a 96-well plate reader.

    In VivoNSC23766 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. 
    Animal modelBalb/c control and NOD mice are at 7 weeks of age and are divided into four groups (n=8/group). At 8 weeks of age two groups of experimental animals (Balb/c and NOD) receive NSC23766 (2.5 mg/kg/day, i.p./daily) and other two groups, which serve as control Balb/c and NOD mice and receive equal volume of saline. The body weights and blood glucose are monitored every week for 34 weeks.
    Formulation & Dosage2.5 mg/kg/day, i.p.
    ReferencesProc Natl Acad Sci U S A. 2004 May 18;101(20):7618-23; Methods Enzymol. 2006;406:554-65; J Biol Chem. 2005 Nov 11;280(45):37516-25. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    NSC-23766 3HCl

    Identification of NSC23766 as an inhibitor of Rac1–Trio interaction. Proc Natl Acad Sci U S A. 2004 May 18;101(20):7618-23.
     

    NSC-23766 3HCl

    Dose-dependent specific inhibition of GEF interaction with Rac1 by NSC23766. Proc Natl Acad Sci U S A. 2004 May 18;101(20):7618-23.
     

    NSC-23766 3HCl

    NSC23766 was effective in specifically inhibiting Rac1 activation in cells. Proc Natl Acad Sci U S A. 2004 May 18;101(20):7618-23.


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