|4-(1,1-二甲基乙基)-N-(4-(1H-咪唑-1-基)苯基)苯磺酰胺|CsnPharm

CAS No.: 945526-43-2

ISCK03 Catalog No. CSN20497

Synonyms: N-(4-imidazol-1-yl phenyl)sulfonamide;c-Kit Inhibitor II;Stem-Cell Factor/c-Kit Inhibitor

ISCK03 is a cell-permeable c-Kit inhibitor with IC50 < < 2.5 μM in cell-free kinase assays and blocks SCF-induced c-kit and Erk phosphorylation (1 μM causes > 90% inhibition) without any effect on HGF-induced Erk phosphorylation in 501mel melanoma cells, it's a phenyl-imidazolosulfonamide compound.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 SCF/c-kit

IC50:2.5μM
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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8133 mL
- 14.0665 mL
- 28.1330 mL
- 5 mM
- 0.5627 mL
- 2.8133 mL
- 5.6266 mL
- 10 mM
- 0.2813 mL
- 1.4067 mL
- 2.8133 mL

技术信息

CAS号

945526-43-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21N3O2S

运输

蓝冰

分子量

355.45

别名

N-(4-imidazol-1-yl phenyl)sulfonamide;c-Kit Inhibitor II;Stem-Cell Factor/c-Kit Inhibitor

溶解度

DMSO	71.0 mg/mL (199.7 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (8.4 mM)

动物实验配方

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