YKL-06-061
产品说明书
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同义名 : | - |
| CAS号 : | 2172617-15-9 | |
| 货号 : | A1164822 | |
| 分子式 : | C30H37N7O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 527.66 | |
| MDL号 : | MFCD32173438 | |
| 存储条件： |
Pure form Keep in dark place, sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Salt-inducible kinases (SIK) constitute a subfamily of kinases comprising three members (SIK1, -2, and -3). Inhibition of SIK kinase activity induces an anti-inflammatory phenotype in macrophages[1]. SIK has also been demonstrated to regulate MITF (microphthalmia-associated transcription factor), the master regulator of pigment gene expression, through its effects on CRTC (cAMP-regulated transcriptional co-activators) and CREB (cAMP-responsive element-binding protein) activity[2]. YKL-06-061 is a potent, selective, second-generation SIK inhibitor with IC50 values of 6.56 nM/1.77 nM/20.5 nM for SIK1/2/3, respectively[2]. Both in UACC62 human melanoma cells and UACC257 human melanoma cells, YKL 06-061 yields a dose-dependent increase in MITF mRNA expression after continuous 3 hours exposure to drug concentrations of 0-4 μM and 0-16 μM, respectively[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.90mL 0.38mL 0.19mL |
9.48mL 1.90mL 0.95mL |
18.95mL 3.79mL 1.90mL |
| 参考文献 |
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