Chemical Structure : SIK2-3 inhibitor 7s
CAS No.:
3038862-86-8
SIK2-3 inhibitor 7s
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
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 Apr 10;68(7):7518-7538.
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