2. Signaling Pathways
  3. Immunology/Inflammation
  4. Salt-inducible Kinase (SIK)

Salt-inducible Kinase (SIK)

Salt-inducible Kinase (SIK)

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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:

Salt-inducible Kinase (SIK) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-148063
    DB0614
    DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity.(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
    DB0614
  • HY-120877A
    (R)-MRT199665
    		Inhibitor 98.70%
    (R)-MRT199665 is an isomer of MRT199665 (HY-120877). MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
    (R)-MRT199665
  • HY-RS12917
    SIK3 Human Pre-designed siRNA Set A
    		Inhibitor

    SIK3 Human Pre-designed siRNA Set A contains three designed siRNAs for SIK3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SIK3 Human Pre-designed siRNA Set A
  • HY-173191
    SK-124
    		Inhibitor
    SK-124 is an orally active, selective SIK2/SIK3 inhibitor. SK-124 inhibits SIK2 and SIK3. SK-124 increases P1NP and CTX. SK-124 increases bone formation and bone mass.
    SK-124
  • HY-149075
    MR22
    		Inhibitor 99.76%
    MR22 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.
    MR22
  • HY-RS12918
    Sik3 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Sik3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sik3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sik3 Mouse Pre-designed siRNA Set A
  • HY-171591
    SIK2-IN-4
    		Inhibitor 99.06%
    SIK2-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.
    SIK2-IN-4
  • HY-RS12915
    Sik2 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Sik2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sik2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sik2 Mouse Pre-designed siRNA Set A
  • HY-149365
    SIKs-IN-1
    		Inhibitor
    SIKs-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.
    SIKs-IN-1
  • HY-RS12912
    Sik1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Sik1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sik1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sik1 Mouse Pre-designed siRNA Set A
  • HY-RS12914
    SIK2 Human Pre-designed siRNA Set A
    		Inhibitor

    SIK2 Human Pre-designed siRNA Set A contains three designed siRNAs for SIK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SIK2 Human Pre-designed siRNA Set A
  • HY-E70861
    SIK1 Recombinant Human Active Protein Kinase
    SIK1 is a MAP4 kinase. The SIK1 MAP4K regulates cell proliferation and cell expansion. SIK1 phosphorylates BIK1 and stabilizes it in a kinase activity-dependent manner. SIK1 Recombinant Human Active Protein Kinase is a recombinant SIK1 protein that can be used to study SIK1-related functions.
    SIK1 Recombinant Human Active Protein Kinase
  • HY-171590
    SIK2-IN-3
    		Inhibitor
    SIK2-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.
    SIK2-IN-3
  • HY-170237
    SIK2/3-IN-1
    		Inhibitor
    SIK2/3-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.
    SIK2/3-IN-1
  • HY-RS12913
    Sik1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Sik1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sik1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Sik1 Rat Pre-designed siRNA Set A
  • HY-P1576
    AMARA peptide
    AMARA peptide is a substrate for SIK and AMPK.
    AMARA peptide
  • HY-101147R
    YKL-05-099 (Standard)
    		Inhibitor
    YKL-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).
    YKL-05-099 (Standard)
  • HY-178014
    SIK1-IN-1
    		Inhibitor
    SIK1-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).
    SIK1-IN-1
  • HY-N1570R
    Pterosin B (Standard)
    		Inhibitor
    Pterosin 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.
    Pterosin B (Standard)
Salt-inducible Kinase (SIK) Isoform Comparison

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