For research use only. Not for therapeutic Use.
ISCK03 is a SCF/c-Kit and CD117-specific inhibitor. ISCK03 significantly inhibits c-Kit phosphorylation at 10 μM[1][2][3].
Pretreatment of 501mel cells with ISCK03 inhibits SCF-induced c-kit phosphorylation dose dependently. ISCK03 also inhibits p44/42 ERK mitogen-activated protein kinase (MAPK) phosphorylation, which is known to be involved in SCF/c-kit downstream signaling. However ISCK03 does not inhibit hepatocyte growth factor (HGF)-induced phosphorylation of p44/42 ERK proteins[1]. ISCK03, a tyrosine kinase inhibitor specific to KIT, prevents survival of CCDC26-KD cells under low-serum conditions. All treated cells exhibits sensitivity to ISCK03 in a dose-dependent manner. After ISCK03 treatment, the survival of KD cells is suppressed to the same level as that of non-KD cells. Conversely, ISCK03 treatment has limited effects on the growth of control K562 and KD clone 3–4 cells under high-serum concentration conditions[2].
Oral administration of ISCK03 induces the dose-dependent depigmentation of newly regrown hair, and this is reversed with cessation of ISCK03 treatment. The topical application of ISCK03 promotes the depigmentation of UV-induced hyperpigmented spots. Fontana-Masson staining analysis shows epidermal melanin is diminished in spots treated with ISCK03[1].
| Catalog Number | I007376 |
| CAS Number | 945526-43-2 |
| Synonyms | 4-tert-butyl-N-(4-imidazol-1-ylphenyl)benzenesulfonamide |
| Molecular Formula | C19H21N3O2S |
| Purity | ≥95% |
| InChI | 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 |
| InChIKey | XQABBHBFHWHMKF-UHFFFAOYSA-N |
| SMILES | CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=CC=C(C=C2)N3C=CN=C3 |
| Reference | [1]. Wintzell M, et al. Repeated cisplatin treatment can lead to a multiresistant tumor cell population with stem cell features and sensitivity to 3-bromopyruvate. Cancer Biol Ther. 2012 Dec;13(14):1454-62. [2]. Na YJ, 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. Biochem Pharmacol. 2007 Sep 1;74(5):780-6. [3]. Hirano T, et al. Long noncoding RNA, CCDC26, controls myeloid leukemia cell growth through regulation of KIT expression. Mol Cancer. 2015 Apr 19;14:90. doi: 10.1186/s12943-015-0364-7. |
