YKL-06-061

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Chemical Structure| 2172617-15-9 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

溶解度 :

DMSO: 16 mg/mL(30.32 mM),配合低频超声助溶,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 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

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

[1]Lombardi MS, Gilliéron C, Berkelaar M, Gabay C. Salt-inducible kinases (SIK) inhibition reduces RANKL-induced osteoclastogenesis. PLoS One. 2017 Oct 3;12(10):e0185426. doi: 10.1371/journal.pone.0185426. PMID: 28973003; PMCID: PMC5626034.

[2]Mujahid N, Liang Y, Murakami R, Choi HG, Dobry AS, Wang J, Suita Y, Weng QY, Allouche J, Kemeny LV, Hermann AL, Roider EM, Gray NS, Fisher DE. A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin. Cell Rep. 2017 Jun 13;19(11):2177-2184. doi: 10.1016/j.celrep.2017.05.042. PMID: 28614705; PMCID: PMC5549921.