Salt-inducible Kinase (SIK)
Salt-inducible kinases (SIKs) belong to AMP-activated protein kinase (AMPK) family, and functions mainly involve in regulating energy response-related physiological processes, such as gluconeogenesis and lipid metabolism. The SIK family comprises three isoforms, namely, SIK1, SIK2, and SIK3, all of which may act as metabolic transmitters. SIKs have shown self-phosphorylation, and play an important role in regulating adrenocortical function under the stimulation of high salt or adreno-cortico-tropic-hormone (ACTH).
All three SIK family kinases are expressed broadly. SIK1 mRNA expression is regulated by multiple stimuli, including high dietary salt intake, ACTH signaling, glucagon signaling, excitable cell depolarization, and circadian rhythms. In contrast, SIK2 and SIK3 expression is constitutive in tissues in which these kinases are expressed. In humans, SIK2 and SIK3 are expressed ubiquitously, with highest SIK2 levels in adipose tissue and highest SIK3 expression in brain. In addition, these SIK family members are dysregulated in various cancers, including ovarian, breast, prostate, and lung cancers, indicating that SIKs may execute crucial roles in tumor occurrence or progression.
Salt-inducible Kinase (SIK) Isoform Specific Products
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Salt-inducible Kinase (SIK) Related Products (39)
Related Products (39)
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Salt-inducible Kinase (SIK) Isoform Comparison
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MR22
0 ImagesMR22 is a potent pan-SIK (salt-inducible kinase) inhibitor. MR22 no longer exhibits activity on STE group kinases and displays excellent selectivity in a representative kinase panel. MR22-dependent SIK inhibition led to centrosome dissociation and subsequent cell-cycle arrest in ovarian cancer cells.
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SK-124
0 ImagesCat. No.: HY-173191CAS No.: 2760404-50-8SK-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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SIK2-IN-4
0 ImagesSIK2-IN-4 (Compound 4) is a highly selective SIK1/2 inhibitor (IC50s 0.143 and 0.076 μM, respectively). SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3) by targeting SIK1/2, thereby regulating cAMP response element binding protein (CREB)-dependent transcriptional activity. SIK2-IN-4 inhibits the production of pro-inflammatory cytokines such as TNF (IC50: 0.11 µM), IL-12/23 p40 (IC50: 0.25 µM), and IL-23 (IC50: 0.47 µM), while inducing the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 can be used to study intestinal inflammation and other chronic inflammatory diseases.
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SIK2/3-IN-2
0 ImagesCat. No.: HY-164534CAS No.: 1648864-21-4SIK2/3-IN-2 (compound 12, compound I-200) is a potent SIK2/3 inhibitor (SIK2 IC50 = 65 nM, SIK3 IC50 = 14 nM). SIK2/3-IN-2 is also a p21-activated protein kinase (PAK) 1 inhibitor with a Ki of 20.7 nM. SIK2/3-IN-2 can be used for hyperproliferative diseases and cancer research, such as Paclitaxel (HY-B0015)-resistant ovarian cancer.
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YKL-05-093
0 ImagesCat. No.: HY-101149CAS No.: 2172616-44-1YKL-05-093 is a salt-induced kinase (SIK) inhibitor (SIK2: Kd = 7.1 nM). YKL-05-093 reduces the phosphorylation level of HDAC4/5/CRTC2, inhibits SOST expression, and stimulates RANKL expression in vitro and in vivo. YKL-05-093 can be used in research on bone diseases.
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SIKs-IN-1
0 ImagesCat. No.: HY-149365CAS No.: 2927557-06-8SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, is a Salt-inducible kinases (SIKs) inhibitor. SIKs regulates the transformation of M1/M2 macrophages, involving in inflammation process. SIKs-IN-1 inhibits SIK activity, up-regulates anti-inflammatory cytokine IL-10, but down-regulates pro-inflammatory cytokine IL-12. SIKs-IN-1 shows excellent anti-inflammatory effects in a DSS-induced colitis model.
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SIK2-IN-3
0 ImagesCat. No.: HY-171590CAS No.: 2810809-10-8SIK2-IN-3 is an orally active SIK1/2 selective inhibitor (IC50: 0.128/0.084 μM). SIK2-IN-3 inhibits CRTC3 phosphorylation and myeloid cell pro-inflammatory cytokine production. SIK2-IN-3 ameliorates systemic and tissue inflammatory responses in a mouse anti-CD40 colitis model.
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SIK2/3-IN-1
0 ImagesCat. No.: HY-170237CAS No.: 3038863-24-7SIK2/3-IN-1 (Compound 7S) is a selectively inhibitory agent of SIK2/3 with oral activity. SIK2/3-IN-1 can significantly inhibit tumor growth (without any body weight loss) in the MV4-11 AML mice CDX model. SIK2/3-IN-1 can be used in the research of MEF2C-dependent acute myeloid leukemia.
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YKL-05-099 (Standard)
0 ImagesCat. No.: HY-101147RCAS No.: 1936529-65-5YKL-05-099 (Standard) is the analytical standard of YKL-05-099 (HY-101147). This product is intended for research and analytical applications. YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. YKL-05-099 binds to SIK1 and SIK3 with IC50s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM).
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SIK1-IN-1
0 ImagesCat. No.: HY-178014SIK1-IN-1 (Compound 27) is a selective Salt-inducible kinase 1 (SIK1) inhibitor with an IC50 of 0.7 nM for SIK1 over SIK2 and SIK3. SIK1-IN-1 has no cytotoxicity against HEK293 cells and PBMCs (maximum concentration of 30 μM). SIK1-IN-1 also has potent inhibitory activities for 392 kinases, in particular tyrosine kinases, such as FGR, HCK and LYN).
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Pterosin B (Standard)
0 ImagesCat. No.: HY-N1570RCAS No.: 34175-96-7Pterosin B (Standard) is the analytical standard of Pterosin B (HY-N1570). This product is intended for research and analytical applications. Pterosin B is an indanone. Pterosin B can be obtained from Pteridium aquilinum. Pterosin B is a Sik3 signaling inhibitor. Pterosin B inhibits Klf5 expression and reduces β-amyloid deposition. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice. Pterosin B inhibits cardiomyocyte hypertrophy, improves cognitive impairment, and lowers blood glucose. Pterosin B can be used in research on arthritis, Alzheimer's disease, pathological cardiac hypertrophy and diabetes.
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SIK2-IN-5
0 ImagesCat. No.: HY-184862CAS No.: 1613711-28-6
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