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USP7/USP47 inhibitor is a novel, potent and selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor (EC50s = 0.42 μM and 1.0 μM) with anticancer activity.
| ln Vitro |
USP7/USP47 inhibitor (compound 14) has an EC50 of 0.42 μM and 1 μM, respectively, making it a selective inhibitor of USP7/USP47. The 20S proteasome, caspase 3, calpain 1, and a representative panel of USPs (USP2, USP5, USP8, USP21, and USP28; EC50 > 31.6 μM) were not inhibited by USP7/USP47 inhibitors. HCT-116 cell growth is inhibited by USP7/USP47 inhibitor, with an EC50 of 7.6 μM [1].
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| References |
| Molecular Formula |
C18H11CL2N3O3S3
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|---|---|
| Molecular Weight |
484.384
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| Exact Mass |
482.934
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| CAS # |
1247825-37-1
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| PubChem CID |
51031028
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| Appearance |
White to off-white solid powder
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| LogP |
6.593
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
736
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GUDJFFQZIISQJB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H11Cl2N3O3S3/c1-29(25,26)12-4-2-11(3-5-12)23-17(24)15-6-10(7-21)18(27-15)28-16-13(19)8-22-9-14(16)20/h2-6,8-9H,1H3,(H,23,24)
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| Chemical Name |
4-cyano-5-(3,5-dichloropyridin-4-yl)sulfanyl-N-(4-methylsulfonylphenyl)thiophene-2-carboxamide
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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 |
| 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 : ~50 mg/mL (~103.22 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.16 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0645 mL | 10.3225 mL | 20.6449 mL | |
| 5 mM | 0.4129 mL | 2.0645 mL | 4.1290 mL | |
| 10 mM | 0.2064 mL | 1.0322 mL | 2.0645 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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