| ISCK03inhibitor of SCF-mediated c-kit activation |
Sample solution is provided at 25 µL, 10mM.
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| Cas No. | 945526-43-2 | SDF | Download SDF |
| Synonyms | c-Kit Inhibitor II,Stem-Cell Factor/c-Kit Inhibitor | ||
| Chemical Name | 4-(1,1-dimethylethyl)-N-[4-(1H-imidazol-1-yl)phenyl]-benzenesulfonamide | ||
| Canonical SMILES | O=S(NC1=CC=C(N2C=NC=C2)C=C1)(C3=CC=C(C(C)(C)C)C=C3)=O | ||
| Formula | C19H21N3O2S | M.Wt | 355.5 |
| Solubility | ≤2mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
ISCK03 is an inhibitor of SCF-mediated c-kit activation.
The signaling downstream of SCF/c-kit plays a key role in the development of various mammalian cells, such as mast cells, melanocytes, primordial germ cells, and hematopoietic progenitor cells.
In vitro: Previous study showed that the pretreatment of 501mel cells with ISCK03 could dose-dependently inhibit SCF-induced c-kit phosphorylation. ISCK03 could also inhibit the phosphorylation of p44/42 ERK mitogen-activated protein kinase that was known to be involved in SCF/c-kit downstream signaling. However, ISCK03 was not able to inhibit hepatocyte growth factor-induced phosphorylation of p44/42 ERK proteins [1].
In vivo: To determine the in vivo efficacy, ISCK03was orally administered to depilated C57BL/6 mice. Results showed that the oral administration of ISCK03 could induce the dose-dependent depigmentation of newly regrown hair, and this was reversed with cessation of ISCK03 treatment. In addition, the topical application of ISCK03 could promote the depigmentation of UV-induced hyperpigmented spots on n brownish guinea pig skin. Moreover, the Fontana–Masson staining analyses showed epidermal melanin was diminished in spots treated with ISCK03 [1].
Clinical trial: Up to now, ISCK03 is still in the preclinical development stage.
References:[1] Y. J. Na, H. S. Baek, S. M. Ahn, et al. [4-t-Butylphenyl]-N-(4-imidazol-1-yl phenyl)sulfonamide (ISCK03) inhibits SCF/c-kit signaling in 501mel human melanoma cells and abolishes melanin production in mice and brownish guinea pigs. Biochemical Pharmacology 74(5), 780-786 (2007).
