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Purity: ≥98%
NSC 23766 (NSC-23766; NSC23766) is a novel, selective and potent inhibitor of Rac GTPase with anti-influenza virus activity. It does not inhibit closely related proteins like Cdc42 or RhoA. Instead, it targets Rac activation via guanine nucleotide exchange factors (GEFs) with an IC50 of ~50 μM in a cell-free assay.
| Targets |
Rac GTPase (IC50 = 50 μM)
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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 the tissue. The supernatants are collected and incubated with PAK-PBD beads at 4°C on a rotator for 1 hour after being centrifuged at 12,000× g for 5 min at 4°C.The beads are then pelleted by centrifugation at 5000× g for 3 min at 4°C. After being resuspended in LaemmLi buffer, the resultant pellet is boiled for two minutes. Western blot analysis is applied to the bead samples. Western blot analysis is also used to determine the total Rac1 in each sample.
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| Cell Assay |
Each well of 96-well tissue culture plates is seeded with 1.5 × 104/mL of cells and 200 μL of medium. Following a 24-hour plating period, the medium is substituted with 200 μL of new medium that contains NSC23766 at the specified concentrations. Upon completion of the treatment period, 20 μL of MTS solution are introduced into each well and incubated for two hours at 37 °C. Using a 96-well plate reader, absorbance at 490 nm is measured.
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| Animal Protocol |
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| References |
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| Molecular Formula |
C24H35N7
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| Molecular Weight |
421.58
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| Exact Mass |
421.29539415
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| CAS # |
733767-34-5
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| Related CAS # |
NSC 23766 trihydrochloride;1177865-17-6
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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 |
DEFBCZWQLILOJF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H35N7/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)
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| Chemical Name |
6-N-[2-[5-(diethylamino)pentan-2-ylamino]-6-methylpyrimidin-4-yl]-2-methylquinoline-4,6-diamine
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3720 mL | 11.8601 mL | 23.7203 mL | |
| 5 mM | 0.4744 mL | 2.3720 mL | 4.7441 mL | |
| 10 mM | 0.2372 mL | 1.1860 mL | 2.3720 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.
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