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MLS-573151 is a novel, specific, cell permeable inhibitor of Cdc42 (IC50 = 2 μM). Other GTPases, such as the related members of the Rho family RhoA, Rac1, and Rac2, are unaffected by it. It functions by preventing GTP from binding to Cdc42.
| Targets |
Cdc42 (EC50 = 2 μM)
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|---|---|
| ln Vitro |
MLS-573151 can effectively capture the phagocytic ability of granulosa cells. The fluorescence intensity of slicing beads or slices in hemocytes (as a slicing criterion for slicing efficiency) was considerably reduced in granule cells treated with MLS-573151 (50 μM; 15 min) compared to trays [1].
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| References |
[1]. Zurab Surviladze, et al. Identification of a small GTPase inhibitor using a high-throughput flow cytometry bead-based multiplex assay. J Biomol Screen. 2010 Jan;15(1):10-20.
[2]. Fan Mao, et al. Transcriptomic Evidence Reveals the Molecular Basis for Functional Differentiation of Hemocytes in a Marine Invertebrate, Crassostrea gigas. Front Immunol. 2020 May 27;11:911. |
| Molecular Formula |
C21H19N3O2S
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|---|---|
| Molecular Weight |
377.45946
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| Exact Mass |
377.11979803
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| CAS # |
10179-57-4
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| Related CAS # |
10179-57-4
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| Appearance |
solid
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| SMILES |
C1C(N(N=C1C2=CC=CC=C2)C3=CC=C(C=C3)S(=O)(=O)N)C4=CC=CC=C4
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| InChi Key |
OPPCVEVPKHRJNY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19N3O2S/c22-27(25,26)19-13-11-18(12-14-19)24-21(17-9-5-2-6-10-17)15-20(23-24)16-7-3-1-4-8-16/h1-14,21H,15H2,(H2,22,25,26)
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| Chemical Name |
4-(3,5-diphenyl-3,4-dihydropyrazol-2-yl)benzenesulfonamide
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| Synonyms |
MLS-573151; MLS000573151
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| 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)
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| Solubility (In Vitro) |
DMSO: 75~100 mg/mL (198.7~264.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.62 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6493 mL | 13.2464 mL | 26.4929 mL | |
| 5 mM | 0.5299 mL | 2.6493 mL | 5.2986 mL | |
| 10 mM | 0.2649 mL | 1.3246 mL | 2.6493 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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