| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
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| Other Sizes |
| Targets |
Tyrosinase-IN-22 targets tyrosinase, a copper-containing enzyme that catalyzes the rate-limiting steps in melanin biosynthesis. It inhibits tyrosinase's monophenolase activity on L-tyrosine with an IC50 of 60 nM and its diphenolase activity on L-dopa with an IC50 of 30 nM. By inhibiting tyrosinase, the compound reduces melanin production, making it useful for studying pigmentation disorders and skin-whitening applications. It also exhibits antioxidant properties that may contribute to its anti-melanogenic effects.
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|---|---|
| ln Vitro |
In vitro studies demonstrate that Tyrosinase-IN-22 is a potent inhibitor of tyrosinase with IC50 values of 60 nM for L-tyrosine and 30 nM for L-dopa. These values indicate high potency against both the monophenolase and diphenolase activities of the enzyme. The compound also exhibits significant antioxidant activity, which may contribute to its anti-melanogenic properties. Detailed cellular assay data, including effects on melanin production in melanocytes, are not extensively documented in the available literature.
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| ln Vivo |
In vivo activity of Tyrosinase-IN-22 is inferred from its potent tyrosinase inhibition and anti-melanogenic properties. As an inhibitor of melanin biosynthesis, it may have potential applications in treating hyperpigmentation disorders. The compound's antioxidant properties may provide additional benefits in reducing oxidative stress in skin tissues. Detailed in vivo efficacy data from animal models, including skin pigmentation studies, are not extensively documented in the available literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for Tyrosinase-IN-22 involves measuring its inhibitory activity against tyrosinase using L-tyrosine and L-dopa as substrates. The assay typically uses mushroom tyrosinase incubated with the compound at varying concentrations and the substrate. Enzyme activity is measured by spectrophotometric monitoring of dopachrome formation at 475 nm. IC50 values are determined by plotting percentage inhibition against compound concentration. Standard protocols include appropriate positive controls such as kojic acid.
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| Cell Assay |
In vitro cell-based assays for Tyrosinase-IN-22 are conducted using melanocyte cell lines such as B16 melanoma cells. Cells are treated with the compound at various concentrations, and melanin content is measured spectrophotometrically after cell lysis. Tyrosinase activity in cell lysates is assessed using L-dopa as a substrate. Cytotoxicity is evaluated using MTT or CCK-8 assays to determine the therapeutic window. Standard protocols include appropriate positive controls such as arbutin or kojic acid.
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| Animal Protocol |
In vivo animal studies for Tyrosinase-IN-22 would typically be conducted using mouse models of hyperpigmentation, such as UV-induced pigmentation or melanin synthesis models. Animals would be administered the compound via topical application or systemic routes, and skin pigmentation would be assessed by visual scoring, chromametry, or histology. However, detailed in vivo protocols and efficacy data are not available from the search results. The compound is intended for research use only.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tyrosinase-IN-22 include a molecular weight of 184.64 and a molecular formula of C7H5ClN2S. Storage recommendations include powder at -20°C for 3 years and in solvent at -80°C for 1 year. Detailed pharmacokinetic parameters such as solubility, half-life, and bioavailability are not extensively documented in the available literature. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
Toxicity information for Tyrosinase-IN-22 is limited. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. Cytotoxicity should be evaluated in cell-based assays to determine appropriate concentrations for experimental use. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
Tyrosinase-IN-22 (5-Chloro-2-mercaptobenzimidazole, compound 4) is a potent tyrosinase inhibitor with IC50 values of 60 nM for L-tyrosine and 30 nM for L-dopa. It exhibits significant antioxidant and anti-melanogenic properties. The compound has a molecular weight of 184.64 and formula C7H5ClN2S. It is a 2-mercaptobenzimidazole derivative that inhibits both monophenolase and diphenolase activities of tyrosinase. It is intended for research use only.
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| Molecular Formula |
C7H5CLN2S
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|---|---|
| Molecular Weight |
184.65
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| Exact Mass |
183.986
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| CAS # |
25369-78-2
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| PubChem CID |
2056429
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| Appearance |
Solid powder
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| Density |
1.54g/cm3
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| Boiling Point |
300.7ºC at 760mmHg
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| Melting Point |
290-292 °C
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| Flash Point |
135.6ºC
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| Vapour Pressure |
0.0011mmHg at 25°C
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| Index of Refraction |
1.75
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| LogP |
2.505
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
11
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| Complexity |
185
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C([H])C2=C(C=1[H])N([H])C(N2[H])=S
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| InChi Key |
ZZIHEYOZBRPWMB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H5ClN2S/c8-4-1-2-5-6(3-4)10-7(11)9-5/h1-3H,(H2,9,10,11)
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| Chemical Name |
5-chloro-1,3-dihydrobenzimidazole-2-thione
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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) |
Typically soluble in DMSO (e.g. 10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (27.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (50.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 5 mg/mL (27.08 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 DMSO stock solution (50.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.4157 mL | 27.0783 mL | 54.1565 mL | |
| 5 mM | 1.0831 mL | 5.4157 mL | 10.8313 mL | |
| 10 mM | 0.5416 mL | 2.7078 mL | 5.4157 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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