The AMP-activated protein kinase (AMPK) family includes salt-inducible kinases (SIKs), which are primarily involved in controlling physiological processes that are connected to the energy response, such as gluconeogenesis and lipid metabolism. Three isoforms of the SIK family—SIK1, SIK2, and SIK3—can all function as metabolic transmitters. SIKs have demonstrated self-phosphorylation and are crucial in controlling adrenocortical function in response to high salt or adreno-cortico-tropic hormone (ACTH) stimulation.
The expression of all three SIK family kinases is widespread. Numerous factors, such as high dietary salt intake, ACTH signaling, glucagon signaling, excitable cell depolarization, and circadian rhythms, affect SIK1 mRNA expression. When these kinases are expressed in tissues, however, SIK2 and SIK3 expression is constant. In humans, SIK2 and SIK3 are widely expressed, with the highest levels of SIK2 being found in adipose tissue and the highest levels of SIK3 being found in the brain. Additionally, the dysregulation of these SIK family members in various cancers, such as ovarian, breast, prostate, and lung cancers, suggests that SIKs may play important roles in the development or progression of tumors.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V3543 | ARN-3236 | 1613710-01-2 | ARN-3236 (ARN3236) is a novel, potent, oral bioavailable and selective inhibitor ofsalt-inducible kinase 2 (SIK2) with anticancer activity. |
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V85175 | GLPG3312 | 2340388-72-7 | |
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V74296 | GLPG3970 | 2403733-82-2 | GLPG3970 (compound 88) is a first-in-class SIK2/SIK3 inhibitor. |
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V3380 | HG-9-91-01 | 1456858-58-4 | HG-9-91-01 (HG9-91-01) is a novel, potent and highly selective inhibitor of salt-inducible kinase (SIKs) with antidiabetic effects. |
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V80835 | MR22 | 3027761-24-3 | MR22 is a potent pan-SIK (salt-induced kinase) inhibitor. |
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V74297 | Phanginin A | 1011528-58-7 | Phanginin A is a potent orally bioactive SIK1 activator. |
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V86998 | SIC-19 | 713112-69-7 | SIC-19 is a SIK2 inhibitor that promotes SIK2 protein degradation through the ubiquitination pathway. |
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V76513 | SIK2-IN-1 | SIK2-IN-1 (compound 8g) is a potent SIK2 inhibitor, more effective than other AMPK kinases. | |
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V74294 | SIKs-IN-1 | 2927557-06-8 | SIKs-IN-1 (compound 8h) is a salt-induced kinase (SIKs) inhibitor and is a pyrimidine-5-carboxamide analogue. |
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V74295 | WH-4-025 | 1876463-35-2 | WH-4-025 is an inhibitor (blocker/antagonist) of salt-induced kinase (SIK) (WO2016023014 A2). |
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V28380 | YKL-06-061 | 2172617-15-9 | YKL-06-061 (YKL06-061) is a novel and potent SIK (salt-inducible kinase) inhibitor (IC50: 6.56 nM/1.77 nM/20.5 nM (SIK1/2/3)) with the potentialto be used as a dermatologic drug impacting UV protection and skin cancer risk. |
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