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HG-9-91-01

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Chemical Structure| 1456858-58-4 同义名 : SIK inhibitor 1
CAS号 : 1456858-58-4
货号 : A333717
分子式 : C32H37N7O3
纯度 : 95%
分子量 : 567.681
MDL号 : MFCD28167714
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 145 mg/mL(255.43 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 HG-9-91-01 is effective against a range of protein tyrosine kinases featuring a threonine residue at the gatekeeper position, including Src family kinases (Src, Lck, Yes), BTK, and receptors for FGF and Ephrin[1]. HG-9-91-01 can potentiate IL-10 production in bone marrow-derived dendritic cells (BMDCs) when pre-treated with zymosan, showing an EC50 of ~200 nM, an effect comparable to that induced by PGE2, suggesting a strong link between SIK2 inhibition and enhanced IL-10 production[2]. HG-9-91-01 exhibits significant selectivity for SIKs over AMPK in cell-free assays, with an over 100-fold higher potency against SIKs (IC50 against AMPK = 4.5 μM). Treatment with HG-9-91-01 dose-dependently increases mRNA expression of Pck1 and G6pc and glucose production[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.81mL

1.76mL

0.88mL

17.62mL

3.52mL

1.76mL
参考文献

[1]Clark K, et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated andregulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91.

[2]Sundberg TB, et al. Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells. Proc Natl Acad Sci U S A. 2014 Aug 26;111(34):12468-73.

[3]Patel K, et al.The LKB1-salt-inducible kinase pathway functions as a key gluconeogenic suppressor in the liver. Nat Commun. 2014 Aug 4;5:4535.