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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.
Targets |
Rac GTPase (IC50 = 50 μM)
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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].
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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].
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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.
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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.
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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.
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References |
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Molecular Formula |
C24H35N7.3HCL
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Molecular Weight |
530.96
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Exact Mass |
529.225427
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CAS # |
1177865-17-6
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Related CAS # |
NSC 23766;733767-34-5
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Appearance |
Solid powder
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SMILES |
CCN(CC)CCCC(C)NC1=NC(=CC(=N1)NC2=CC3=C(C=C(N=C3C=C2)C)N)C.Cl.Cl.Cl
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InChi Key |
CPUHORIUXPQCHW-UHFFFAOYSA-N
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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
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Chemical Name |
6-N-[2-[5-(diethylamino)pentan-2-ylamino]-6-methylpyrimidin-4-yl]-2-methylquinoline-4,6-diamine;trihydrochloride
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. AO:AO ≥ 2.5 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 110 mg/mL (207.17 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.  (Please use freshly prepared in vivo formulations for optimal results.) |
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.
Calculation results
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.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.