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Cat. No. Product Name CAS No. Information
PC-63122

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.

PC-61766

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.

PC-42327

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.

PC-63124

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.
PC-63123

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.
PC-61952

ARN-3261

ARN-3261 is a potent, selective, orally available salt inducible kinase SIK2 and SIK3 inhibitor with IC50 of 11 nM and 19 nM, respectively; specifically inhibits SIK2-expressed SKOv3 cells with IC50 of 92 nM; demonstrates effectivity against ovarian, breast cancer cell lines alone and in combination with Paclitaxel and Cisplatin; also inhibits ovarian tumor growth significantly in SKOv3 human ovarian cancer xenografts in mice.
PC-61765

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.

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