YKL-06-061

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 macrophages¹. 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) activity². 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, respectively². 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, respectively².

溶解方案(细胞实验)

DMSO 中的溶解度 : 16.67 mg/mL (31.59 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 1.25 mg/mL (2.37 mM); 澄清溶液 此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案 二": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 1.25 mg/mL (2.37 mM); 澄清溶液 此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"