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ISCK03

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Chemical Structure| 945526-43-2 同义名 : c-Kit Inhibitor II;N-(4-imidazol-1-yl phenyl)sulfonamide;ISCK03, ISCK-03, ISCK 03.;Stem-Cell Factor/c-Kit Inhibitor
CAS号 : 945526-43-2
货号 : A263965
分子式 : C19H21N3O2S
纯度 : 99%+
分子量 : 355.454
MDL号 : MFCD12031591
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(112.53 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 C-kit belongs to the platelet-derived growth factor (PDGF) family of receptor tyrosine kinases (RTKs). It has been reported that the SCF(stem-cell factor)/c-kit signaling is related to melanocyte development and pigmentation. ISCK03 is a potent c-kit inhibitor and may be useful for treating hyperpigmented spots caused by effects on c-kit expression. In 501mel human melanoma cells, pretreatment with ISCK03 inhibited SCF-induced c-kit phosphorylation dose dependently. Furthermore, ISCK03 inhibited c-kit phosphorylation in vitro and SCF-induced c-kit phosphorylation in 501mel human melanoma cells in a dose-dependent manner. Complete inhibition was observed with 1 and 5 μM ISCK03. It also inhibited SCF-induced p44/42 ERK phosphorylation dose dependently (5.0, 1.0, 0.5, and 0.1 μM ISCK03 for 2 h). In mice, once-daily oral administration of ISCK03 (500, 250, or 125 mg/kg) had a dramatic dose-dependent effect on hair depigmentation. Moreover, 0.1% ISCK03 treatment abolished UV-induced hyperpigmentation in brownish guinea pigs. And the epidermal melanin was found to be decreased in the ISCK03-treated pigment spots[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.07mL

2.81mL

1.41mL

28.13mL

5.63mL

2.81mL
参考文献

[1]Hirano T, Yoshikawa R, et al. Long noncoding RNA, CCDC26, controls myeloid leukemia cell growth through regulation of KIT expression. Mol Cancer. 2015 Apr 19;14:90.

[2]Na YJ, Baek HS, 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]Na YJ, Baek HS, Ahn SM, Shin HJ, Chang IS, Hwang JS. [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