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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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ISCK03 is a potent c-kit inhibitor. In mice and brownish guinea pigs, ISCK03 completely eliminates melanin synthesis and suppresses SCF/c-kit signaling in 501mel human melanoma cells. The phosphorylation of p44/42 ERK mitogen-activated protein kinase (MAPK), which is known to be involved in downstream signaling of SCF/c-kit, was also inhibited by ISCK03. It is possible to use ISCK03 as a skin-whitening agent.
| Targets |
SCF; c-Kit
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|---|---|
| ln Vitro |
Pretreatment of 501mel cells with ISCK03 inhibits SCF-induced c-kit phosphorylation dose dependently. Additionally, ISCK03 prevents the phosphorylation of p44/42 ERK mitogen-activated protein kinase (MAPK), which is known to be connected to downstream signaling of SCF/c-kit. Nevertheless, ISCK03 is not able to prevent the phosphorylation of p44/42 ERK proteins caused by hepatocyte growth factor (HGF)[1]. CCDC26-KD cells cannot survive in low-serum environments when ISCK03, a tyrosine kinase inhibitor specific to KIT, is present. A dose-dependent sensitivity to ISCK03 is seen in all treated cells. Following ISCK03 treatment, KD cells experience the same level of survival suppression as non-KD cells. On the other hand, under circumstances of high serum concentration, ISCK03 treatment has minimal effects on the growth of control K562 and KD clone 3-5 cells[2].
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| ln Vivo |
Oral ISCK03 treatment causes newly regrown hair to depigment in a dose-dependent manner, which is reversed when the treatment is stopped. UV-induced hyperpigmented spots can be made to become less pigmented by applying ISCK03 topically. Epidermal melanin in areas treated with ISCK03 is reduced, according to Fontana-Masson staining analysis[1].
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| Enzyme Assay |
Recombinant human c-kit protein is added for the kinase reaction, ATP is dispensed into 384-well plates, and chemical compounds (ISCK03: 2.5, 5, 10, 100 μM) are added by replicative plate. The development reaction is then allowed to run at room temperature for 40 minutes after a 45-minute incubation period at 37°C. The coumrain and fluorescein fluorescence-emission signals are detected after the reaction is stopped[1].
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| Cell Assay |
In order to ascertain whether ISCK03 has any cytotoxic effects on 501mel cells, MTT assays are conducted utilizing varying doses of ISCK03 (1, 5, 10 μM). 501mel cells are cultured for 48 hours either with SCF with ISCK03 or with SCF alone (50 ng/mL)[1].
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| Animal Protocol |
Mice: The female C57BL/6 mice's backs are depilated in order to initiate the hair cycle. Mice under anesthesia have their hair briefly removed. Intraperitoneal injection of 50 mg of the rat antimouse c-kit-neutralizing monoclonal antibody ACK2 is done daily. One oral dose of ISCK03 is given each day. Animals are sacrificed or examined for repigmentation of the newly regrown hair shaft on days 21–28. For immunohistochemical analyses, skin is removed, frozen, and fixed in paraffin[1].
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| References |
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| Molecular Formula |
C19H21N3O2S
|
|---|---|
| Molecular Weight |
355.4539
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| Exact Mass |
355.14
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| Elemental Analysis |
C, 64.20; H, 5.96; N, 11.82; O, 9.00; S, 9.02
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| CAS # |
945526-43-2
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| Related CAS # |
945526-43-2
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| Appearance |
Solid powder
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| SMILES |
CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=CC=C(C=C2)N3C=CN=C3
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| InChi Key |
XQABBHBFHWHMKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H21N3O2S/c1-19(2,3)15-4-10-18(11-5-15)25(23,24)21-16-6-8-17(9-7-16)22-13-12-20-14-22/h4-14,21H,1-3H3
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| Chemical Name |
4-tert-butyl-N-(4-imidazol-1-ylphenyl)benzenesulfonamide
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| Synonyms |
ISCK03; ISCK 03; ISCK-03
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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: ~71 mg/mL (~199.8 mM)
Ethanol: ~3 mg/mL (~8.4 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.03 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.03 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 | 2.8133 mL | 14.0667 mL | 28.1334 mL | |
| 5 mM | 0.5627 mL | 2.8133 mL | 5.6267 mL | |
| 10 mM | 0.2813 mL | 1.4067 mL | 2.8133 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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