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首页-小分子抑制剂&激动剂-Autophagy-Salt Inducible Kinase (SIK)-GLPG3312
GLPG3312

Chemical Structure : GLPG3312

CAS No.: 2340388-72-7

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GLPG3312 (GLPG 3312, GLPG-3312)

货号: PC-21587Not For Human Use, Lab Use Only.

GLPG3312 is a potent and selective pan-SIK inhibitor with IC50 of 2.0/0.7/0.6 nM for SIK1/SIK2/SIK3, respectively.

规格 价格 库存 数量
2 mg ￥3580 In stock
5 mg ￥5480 In stock
10 mg ￥8980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GLPG3312 is a potent and selective pan-SIK inhibitor with IC50 of 2.0/0.7/0.6 nM for SIK1/SIK2/SIK3, respectively.
GLPG3312 displays high selectivity against a panel of 380 kinases, RIPK2 is the most potent off-target with IC50 of 19.7 nM, which is 10-fold less potent than that on SIK1 and 30-fold less potent than those on SIK2 and SIK3.
GLPG3312 dose-dependently inhibits TNFα release in vitro cell assays using primary human monocytes and monocyte-derived macrophages (MdM) stimulated with LPS, with IC50 of 17 nM and 34 nM, respectively, also enhances the release of IL-10 at higher concentrations.
GLPG3312 displays both anti-inflammatory and immunoregulatory activities in vitro, inhibits the production of TNFα and increased the release of IL-10 in mice stimulated with LPS.

物理化学性质&存储条件

分子量 453.45
分子式 C23H21F2N5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-Cyclopropyl-2-(difluoromethoxy)-6-methoxy-4-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)benzamide

参考文献

1. Temal-Laib T, et al. J Med Chem. 2023 Dec 26. doi: 10.1021/acs.jmedchem.3c01428.

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