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You are here:Home-Inhibitors & Agonists-Autophagy-Salt Inducible Kinase (SIK)

Request The Product List ofSalt Inducible Kinase (SIK) Salt Inducible Kinase (SIK)

    Salt-inducible Kinases (SIK) are a family of related serine-threonine kinases. In cultured adrenocortical cells, SIK1 is rapidly but transiently induced by adrenocorticotropin (ACTH) treatment, suggesting that it contributes to ACTH-mediated induction of steroidogenic enzymes. SIK2 is found in adipocytes and phosphorylates a specific serine residue. Members of the SIK family are emerging as important modulators of key processes such as steroid hormone biosynthesis by the adrenal cortex in adipocytes.



Cat. No. Product Name CAS No. Information
GY06693

MRT 199665

1456858-57-3

MRT 199665 is a potent salt-inducible kinases (SIKs) inhibitor with IC50 of 110, 12, 43 nM for SIK1,2,3 respectively; also inhibits AMPKα1/α2 (both IC50=10 nM), MARK1/2/3/4 (both IC50=2 nM), NUAK1/2 (IC50=3/120 nM), and MELK (IC50=29 nM); elevates IL-10 production by inducing the dephosphorylation of CREB-regulated transcriptional coactivator 3 (CRTC3), increases LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine secretion (IL-6, IL-12, and TNF) in macrophages.

GY06692

ARN-3236

1613710-01-2

ARN-3236 is a novel potent, selective, and orally active SIK2 inhibitor with IC50 of <1 nM; does not significantly inhibit SIK1 and SIK3, as well as other AMPK family members; inhibits the growth of 10 ovarian cancer cell lines with IC50 of 0.8-2.6 uM; increasess centrosome uncoupling from nucleus, and inhibits centrosome splitting in mitotic cells; induces cell cycle arrest, apoptosis and tetraploidy, also inhibits AKT phosphorylation and attenuates survivin expression; sensitizes ovarian cancer to paclitaxel in SKOv3ip xenograft model.

GY06690

YKL-05-099

1936529-65-5

YKL-05-099 (YKL 05-099) is a novel potent, selective pan-SIK inhibitor with IC50 of 10, 40 and 30 nM for SIK1, 2 and 3, respectively; displays increased SIK selectivity and enhanced pharmacokinetic properties compared with HG-9-91-01; reduces LPS stimulated phosphorylation of HDAC5 at the SIK-specific phosphorylation site Ser259, increases expression of the CREB target genes Il10 and Nurr77, suppresses production of TNFα, IL-6 and IL-12p40 in BMDMs; a useful probe to investigate SIK function in vivo.

GY06687

Pterosin B

34175-96-7

Pterosin B is a potent and specific SIK3 signaling inhibitor that suppresses SIK3 downstream cascades by up-regulating the phosphorylation levels in the SIK3 C-terminal regulatory domain; shows no effect on up-regulation of MEF2 and down-regulation of CRTC2 activities by SIK1 or SIK2; promotes glucose production by up-regulating gluconeogenic gene expression in mouse hepatoma AML-12 cells, decreases the glycogen content and stimulates an association between PHKG2 and SIK3.

GY06685

rac Pterosin B

60657-37-6

rac Pterosin B is a potent and specific SIK3 signaling inhibitor that suppresses SIK3 downstream cascades by up-regulating the phosphorylation levels in the SIK3 C-terminal regulatory domain; shows no effect on up-regulation of MEF2 and down-regulation of CRTC2 activities by SIK1 or SIK2; promotes glucose production by up-regulating gluconeogenic gene expression in mouse hepatoma AML-12 cells, decreases the glycogen content and stimulates an association between PHKG2 and SIK3.

GY04727

YKL-06-061

2172617-15-9

YKL 06-061 is a potent, selective, second-generation salt-inducible kinase (SIK) inhibitor with IC50 of 6.56/1.77/20.5 nM for SIK1/2/3, respectively; inhibits only one kinase FRK (IC50=1.1 nM), more strongly than SIKs, in a panel of 468 human kinases; dose-dependently increases MITF mRNA expression in human melanoma cells; induces significant pigmentation in Mc1r-deficient mice and normal human skin.

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