Casein Kinases (CKs) are serine/threonine-selective enzymes that function as regulators of signal transduction pathways in most eukaryotic cell types.
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IC261 (IC-261, SU-5607) is a potent, specific, ATP-competitive CK1delta/epsilon (CK1δ/CK1ε) with IC50 of 1 uM, does not block the activity of α, β and γ isoforms; specifically blocks phosphorylation in vivo of the CK1delta/epsilon phosphorylation sites in p53 in murine SV3T3 cells, inhibits cytokinesis causing a transient mitotic arrest; reduces pancreatic tumour cell growth in vitro and in vivo, decreases the expression levels of several anti-apoptotic proteins and sensitises cells to CD95-mediated apoptosis.
A potent inhibitor of Casein Kinase CK1ε, CK1δ and p38α with IC50 of 6.4, 6.8 and 6.7 nM, respectively; inhibits the phosphorylation of proteins downstream of p38α MAPK such as MAPKAPK2 and HSP27 during cardiogenesis, and increases ATF-2 and MEF2C during cardiac differentiation.
SR-3029 is a potent, highly selective, ATP-competitive and brain penetrating Casein Kinase 1δ/ε (CK1δ/ε) inhibitor with IC50 of 44/260 nM, respectively; inhibits melanoma A375 cell growth with IC50 of 86 nM; triggers apoptosis of CK1δ-expressing breast tumor cells ex vivo, tumor regression in orthotopic models of triple-negative breast cancer in mice model.
SR-653234 is a purine scaffold casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 160/540 nM, respectively.
SSTC3 is a novel small-molecule CK1α activator with EC50 of 30 nM (WNT-driven reporter gene assay), Kd of 32 nM; has better pharmacokinetic properties than pyrvinium, attenuates the growth of such Apc mutant organoids with EC50 of 2.9 uM; decreases the viability of the WNT-dependent cell lines (EC50 = 132, 63, and 123 nM for HT29, SW403, and HCT116 cells, respectively), inhibits the growth of CRC xenografts in mice; also attenuates the growth of patient-derived metastatic CRC xenograft, with minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
VU-WS113 is a potent inhibitor of Wnt signaling with EC50 of 80 nM that selectively potentiates CK1α kinase activity.
Pyrvinium Iodide is an anthelmintic effective for pinworms that shows to be a potent inhibitor of Wnt signaling with EC50 of 10 nM, binds to all CK1 family members in vitro at low nanomolar concentrations and selectively potentiates CK1α kinase activity; inhibits Wnt signaling downstream of β-catenin, and promotes Pygopus degradation; also is a potent inhibitor of HH signaling by reducing the stability of the Gli family of transcription factors.
Pyrvinium is an anthelmintic effective for pinworms that shows to be a potent inhibitor of Wnt signaling with EC50 of 10 nM, binds to all CK1 family members in vitro at low nanomolar concentrations and selectively potentiates CK1α kinase activity; inhibits Wnt signaling downstream of β-catenin, and promotes Pygopus degradation; also is a potent inhibitor of HH signaling by reducing the stability of the Gli family of transcription factors.
GO289 (GO-289, GO 289) is a potent and selective inhibitor of casein kinase 2 (CK2) with IC50 of 7 nM in in vitro kinase assays, shows minor effects on CKIδ and CKIα activity in vitro; GO289 showed only a moderate or minor effect on the activity of 59 kinases from a variety of classes, the second most affected kinase was PIM2 with an IC50 of 13 nM; caused dose-dependent lengthening of circadian period not only in Bmal1-dLuc reporter cells but also in Per2-dLuc reporter cells with a phase opposite to that of Bmal1-dLuc, inhibits phosphorylation of clock protein PER2 S693 in cells; strongly inhibits Caki-2, A498, and 769-P cancer cells, significantly reduces growth of mouse MLL-AF9 leukemia cells without effect on hematopoietic progenitor cells; shows effectivity on circadian period and reporter signal intensity in spleen explants of MLL-AF9 mice.
ON108110 (ON-108110, ON 108110) is a novel multi-kinase inhibitor of protein kinase CK2 (CK2α1/2, IC50=3/2 nM) as well as CDK4/6 (IC50=2-24 nM); reduces replication of influenza A virus in a dose-dependent manner by suppressing viral RNA synthesis, also inhibits other viruses including vesicular stomatitis virus and Newcastle disease virus; inhibits MCL and T-ALL cell growth (GI50 values of 0.2-3 uM), inhibits CK2 and CDK4/6 mediated oncogenic signaling.
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