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SIK2-3 inhibitor 7s

Chemical Structure : SIK2-3 inhibitor 7s

CAS No.: 3038862-86-8

SIK2-3 inhibitor 7s

货号: PC-25119Not For Human Use, Lab Use Only.

SIK2/3 inhibitor 7s is a potent, selective dual SIK2/3 inhibitor with IC50 of 1.1 nM for both, >30-fold selective over SIK1.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SIK2/3 inhibitor 7s is a potent, selective dual SIK2/3 inhibitor with IC50 of 1.1 nM for both, >30-fold selective over SIK1.
SIK2/3 inhibitor 7s demonstrated good potency in cells highly expressing MEF2C, such as MV-4-11 (Gi50=14 nM) and THP-1 cells, but not in cells with low MEF2C expression, reduced the ratio of phosphorylated HDAC4 to total HDAC (Figure 6A,B) and the mRNA levels of DUSP7.
SIK2/3 inhibitor 7s (10 mg/kg, PO, BID and 30 mg/kg, PO, BID) significantly suppressed tumor growth in MV4-11 subcutaneous xenograft model, reduced HDAC4 phosphorylation and suppresses tumor growth in vivo.

物理化学性质&存储条件

分子量 432.41
分子式 C20H19F3N6O2
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

6-(2-amino-5-(1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)-8-methoxy-2-(2,2,2-trifluoroethyl)-3,4-dihydro-2,7-naphthyridin-1(2H)-one

参考文献

1. Zhu W, et al. J Med Chem. 2025 Apr 10;68(7):7518-7538.

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