2760404-50-8
Chemical Structure
SK-124
- CAS No.: 2760404-50-8
- Formula:C23H22N6O3
- Molecular Weight:430.46
InChIKey: VOYZWDQJVPQGCO-UHFFFAOYSA-N
SMILES: COC1=CC(C2=CN=C3C=C(C4=CN(C)N=C4)C=CN32)=CC(OC)=C1C5=NN=C(CC)O5
Biological Activity: SK-124 is an orally active salt-inducible kinase (SIK) inhibitor with an IC50 of 230 nM against SIK1, 4.1 nM against SIK2, and 21 nM against SIK3, exhibiting excellent kinome selectivity[1][2][4]. SK-124 blocks SIK-mediated CRTC2 phosphorylation, promotes CRTC2 nuclear translocation, and regulates vitamin D metabolism by upregulating renal Cyp27b1 and downregulating Cyp24a1[1][4]. SK-124 upregulates the expression of bone-related genes, increases serum Ca2+, 1,25-vitamin D and intact FGF23 levels, and suppresses endogenous PTH levels[1][2][3][4]. SK-124 can be used in studies related to osteoporosis, male osteoporosis, and chronic kidney disease-mineral and bone disorder[2][3][4].
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SK-124 | 95.0% | SK-124 is an orally active salt-inducible kinase (SIK) inhibitor with an IC50 of 230 nM against SIK1, 4.1 nM against SIK2, and 21 nM against SIK3, exhibiting excellent kinome selectivity. SK-124 blocks SIK-mediated CRTC2 phosphorylation, promotes CRTC2 nuclear translocation, and regulates vitamin D metabolism by upregulating renal Cyp27b1 and downregulating Cyp24a1. SK-124 upregulates the expression of bone-related genes, increases serum Ca2+, 1,25-vitamin D and intact FGF23 levels, and suppresses endogenous PTH levels. SK-124 can be used in studies related to osteoporosis, male osteoporosis, and chronic kidney disease-mineral and bone disorder. | ||||||||||||||||||||
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- [1]. Meyer MB, et al. Rapid genomic changes by mineralotropic hormones and kinase SIK inhibition drive coordinated renal Cyp27b1 and Cyp24a1 expression via CREB modules. The Journal of biological chemistry. 2022 Nov;298(11):102559. [Content Brief]
- [2]. Sato T, et al. Structure-based design of selective, orally available salt-inducible kinase inhibitors that stimulate bone formation in mice. Proceedings of the National Academy of Sciences of the United States of America. 2022 Dec 13;119(50):e2214396119. [Content Brief]
- [3]. Choi RB, et al. The orally available SIK2/SIK3 inhibitor SK-124 increases bone mass in hypogonadal male mice. JBMR plus. 2026 Apr;10(4):ziag032. [Content Brief]
- [4]. Yoon SH, et al. A parathyroid hormone/salt-inducible kinase signaling axis controls renal vitamin D activation and organismal calcium homeostasis. The Journal of clinical investigation. 2023 May 01;133(9):e163627. [Content Brief]
Keywords
