NSC-23766 3HCl

Alias: NSC-23766 3HCl; NSC-23766 3Hydrochloride; NSC23766; NSC-23766; NSC 23766
Cat No.:V0012 Purity: ≥98%
NSC23766 3HCl, the salt form of NSC23766, is a novel and potent inhibitor of Rac GTPase that targets the activation of Rac by guanine nucleotide exchange factors (GEFs) with an IC50 of less than 50 μM in a test conducted without using cells; NSC23766 does not inhibit the closely related targets, Cdc42 or RhoA.
NSC-23766 3HCl Chemical Structure CAS No.: 1177865-17-6
Product category: Rho
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
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Other Forms of NSC-23766 3HCl:

  • NSC 23766
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description

NSC23766 3HCl, the salt form of NSC23766, is a novel and potent inhibitor of Rac GTPase that targets the activation of Rac by guanine nucleotide exchange factors (GEFs) with an IC50 of less than 50 μM in a test conducted without using cells; NSC23766 does not inhibit the closely related targets, Cdc42 or RhoA.

Biological Activity I Assay Protocols (From Reference)
Targets
Rac GTPase (IC50 = 50 μM)
ln Vitro
NSC 23766 (100 μM) NSC 23766 (100 μM) treatment effectively inhibits polar body emission in a dose-dependent manner. The percentage of oocyte spindles with abnormal morphology increases in response to NSC 23766 (200 μM). Oocytes treated with NSC 23766 exhibit a significant decrease in the expression of the p-MAPK protein[2]. Primordial follicles are increased and germLine cell cysts are decreased when NSC23766 (50 μM) is combined with 100 ng/mL Jagged1, GDF9, and BMP15[3]. In the spinal dorsal horn neurons, NSC23766 dramatically reduces GTP-Rac1 activity as well as the phosphorylation of Rac1-PAK, ERKs, and p38 MAPK[4].
ln Vivo
NSC23766 (2.5 mg/kg/day, i.p.) dramatically delays the onset of spontaneous diabetes in NOD mice while having no discernible effects on the mice's body weight or growth. In NOD mouse islets, NSC23766 dramatically upregulates the expression of Rac1 and CHOP, a marker for ER-stress[1].
Enzyme Assay
Protease and phosphatase inhibitors are used to homogenize fresh spinal cord tissue from the lumbar enlargement, and buffer is then used to lyse it. The beads are pelleted by centrifugation at 5000× g for 3 min at 4°C after being incubated with PAK-PBD beads at 4°C on a rotator for 1 hour following a centrifugation at 12,000× g for 5 min at 4°C. In the interim, the supernatants are collected. A second boiling period of two minutes is spent resuspending the resultant pellet in LaemmLi buffer. Analysis by Western blot is performed on the bead samples. By using a Western blot analysis, total Rac1 in every sample is also found.
Cell Assay
In 96-well tissue culture plates, 200 μL of medium is added to each well before seeding 1.5 × 104/mL of cells are grown. 200 μL of new medium containing NSC23766 at the specified concentrations is added to the medium after 24 hours of plating. Twenty microliters of MTS solution are added to each well at the conclusion of the treatment period, and they are incubated for two hours at 37 °C. We use a 96-well plate reader to measure absorbance at 490 nm.
Animal Protocol
At seven weeks of age, Balb/c control and NOD mice are split into four groups (n=8/group). At eight weeks of age, two experimental groups—Balb/c and NOD mice—receive NSC23766 (2.5 mg/kg/day, i.p./daily), while the other two groups—control Balb/c and NOD mice—receive an equivalent volume of saline. For 34 weeks, blood glucose and body weight are measured weekly.
References

[1]. NSC23766, a Known Inhibitor of Tiam1-Rac1 Signaling Module, Prevents the Onset of Type 1 Diabetes in the NOD Mouse Model. Cell Physiol Biochem. 2016;39(2):760-7.

[2]. Inhibition of Rac1 GTPase activity affects porcine oocyte maturation and early embryo development. Sci Rep. 2016 Oct 3;6:34415.

[3]. Rac1 modulates the formation of primordial follicles by facilitating STAT3-directed Jagged1, GDF9 and BMP15 transcription in mice. Sci Rep. 2016 Apr 6;6:23972.

[4]. Involvement of Rac1 signalling pathway in the development and maintenance of acute inflammatory pain induced by bee venom injection. Br J Pharmacol. 2016 Mar;173(5):937-50.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H35N7.3HCL
Molecular Weight
530.96
Exact Mass
529.225427
CAS #
1177865-17-6
Appearance
Solid powder
SMILES
CCN(CC)CCCC(C)NC1=NC(=CC(=N1)NC2=CC3=C(C=C(N=C3C=C2)C)N)C.Cl.Cl.Cl
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
Chemical Name
6-N-[2-[5-(diethylamino)pentan-2-ylamino]-6-methylpyrimidin-4-yl]-2-methylquinoline-4,6-diamine;trihydrochloride
Synonyms
NSC-23766 3HCl; NSC-23766 3Hydrochloride; NSC23766; NSC-23766; NSC 23766
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~100 mg/mL (~188.3 mM)
Water: <1 mg/mL
Ethanol: ~100 mg/mL (~188.3 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8834 mL 9.4169 mL 18.8338 mL
5 mM 0.3767 mL 1.8834 mL 3.7668 mL
10 mM 0.1883 mL 0.9417 mL 1.8834 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • 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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