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-15776
    HG-9-91-01
    		Inhibitor 99.77%
    HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIK) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively.
    HG-9-91-01
  • HY-101147
    YKL-05-099
    		Inhibitor 99.76%
    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
  • HY-120877
    MRT199665
    		Inhibitor 99.74%
    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.
    MRT199665
  • HY-120856
    ARN-3236
    		Inhibitor 98.60%
    ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity.
    ARN-3236
  • HY-150203
    GLPG3970
    		Inhibitor 99.64%
    GLPG3970 (compound 88) is a first-in-class SIK2/SIK3 inhibitor. GLPG3970 can be used for the research of inflammation and autoimmune disease.
    GLPG3970
  • 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-159657
    SIK-IN-4
    		Inhibitor
    SIK-IN-4 (compound 34) is a SIK inhibitor, with IC50 values of 1.2 nM, 0.9 nM and 1.8 nM for SIK1, SIK2 and SIK3, respectively.
    SIK-IN-4
  • HY-N1570R
    Pterosin B (Standard)
    		Inhibitor
    Pterosin B (Standard) is the analytical standard of Pterosin B. This product is intended for research and analytical applications. Pterosin B, a indanone found in bracken fern (Pteridium aquilinum), is an inhibitor of salt-inducible kinase 3 (Sik3) signaling. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice by inhibiting Sik3.
    Pterosin B (Standard)
  • HY-129141
    YKL-06-062
    		Inhibitor 99.40%
    YKL-06-062 is a second-generation salt-inducible kinase (SIK) inhibitor with an IC50 of 2.12 nM/1.40 nM/2.86 nM for SIK1, SIK2 and SIK3, respectively.
    YKL-06-062
  • HY-N1570
    Pterosin B
    		Inhibitor 99.92%
    Pterosin B, a indanone found in bracken fern (Pteridium aquilinum), is an inhibitor of salt-inducible kinase 3 (Sik3) signaling. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice by inhibiting Sik3.
    Pterosin B
  • HY-157442
    GLPG3312
    		Inhibitor 98.25%
    GLPG3312 (Compound 28) is a selective pan-SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases.
    GLPG3312
  • HY-120056
    YKL-06-061
    		Inhibitor 99.21%
    YKL-06-061 is a potent, selective, second-generation salt-inducible kinase (SIK) inhibitor with IC50 values of 6.56 nM/1.77 nM/20.5 nM for SIK1/2/3, respectively.
    YKL-06-061
  • HY-148062
    RSS0680
    		98.03%
    RSS0680 (Example 22) is a bifunctional compound targeted protein degradation of kinases. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used for research of disease or disorder mediated by aberrant kinase activity.
    RSS0680
  • HY-P1576A
    AMARA peptide TFA
    		99.29%
    AMARA peptide (TFA) is a substrate for salt-inducible kinase (SIK) and adenosine monophosphate activated protein kinase (AMPK).
    AMARA peptide TFA
  • HY-148063
    DB0614
    		98.80%
    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-138001
    WH-4-025
    		Inhibitor 99.31%
    WH-4-025 is a Salt-inducible kinase (SIK) inhibitor (WO2016023014 A2).
    WH-4-025
  • HY-139253
    MRIA9
    		Inhibitor 98.80%
    MRIA9 is an ATP-competitive, pan Salt-Inducible kinase (SIK) and PAK2/3 inhibitor, with IC50 values of 516 nM, 180 nM and 127 nM for SIK1, SIK2 and SIK3, respectively.
    MRIA9
  • HY-148061
    DB1113
    		99.28%
    DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades 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. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity.
    DB1113
  • 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-149075
    MR22
    		Inhibitor
    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
Salt-inducible Kinase (SIK) Isoform Comparison

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