Chemical Structure : SIK inhibitor 7s
CAS No.:
3038863-24-7
SIK inhibitor 7s
Catalog No.: PC-24280Not For Human Use, Lab Use Only.
SIK inhibitor 7s is a potent, selective inhibitor of SIK2/SIK3 with IC50 of 1.1 nM for both, inhibits SIK1 with IC50 of 34.5 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
SIK inhibitor 7s is a potent, selective inhibitor of SIK2/SIK3 with IC50 of 1.1 nM for both, inhibits SIK1 with IC50 of 34.5 nM.
SIK inhibitor 7s demonstrates over 30-fold selectivity for SIK2/3 over other kinases by KINOMEscan in the presence of 1 mM ATP, except for MKNK2 (14-fold) and PDGFRα (28-fold).
SIK inhibitor 7s exhibits antiproliferative effects on various AML cancer lines, demonstrates good potency in cells highly expressing MEF2C, such as MV-4-11 (IC50=14 nM) and THP-1 cells (IC50=144 nM), but not in cells with low MEF2C expression.
SIK inhibitor 7s reduced the ratio of phosphorylated HDAC4 to total HDAC and the mRNA levels of DUSP7, both in a dose-dependent manner, in MV-4-11 and THP-1 cells.
SIK inhibitor 7s (10 mg/kg, PO, BID and 30 mg/kg, PO, BID) reduces HDAC4 phosphorylation and suppresses tumor growth in MV4-11 CDX model.
Physicochemical Properties
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M.Wt
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432.41
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Formula
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C20H19F3N6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Zhu W, et al. J Med Chem. 2025 Mar 20. doi: 10.1021/acs.jmedchem.4c03225.
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