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Cat. No. Product Name CAS No. Information
PC-60582

(R)-DRF053 dihydrochloride

1241675-76-2

(R)-DRF053 dihydrochloride (DRF053) is a potent, cell-permeable, dual CK1/CDK inhibitor with IC50 of 14 nM, 220 nM and 80 nM for CK1, CDK5/p25 and CDK1/cyclin B, respectively; exhibits antiproliferative activity against human neuroblastoma SH-SY5Y cells with EC50 of 17.2 uM, prevents the CK1-dependent production of amyloid-beta in a cell model; specifically increases the number of duct-derived β-cells without affecting their proliferation.

PC-60387

SSTC3

1242422-09-8

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.

PC-60385

VU-WS113

1415921-09-3

VU-WS113 is a potent inhibitor of Wnt signaling with EC50 of 80 nM that selectively potentiates CK1α kinase activity.

PC-45870

CX-4945

1009820-21-6

CX-4945 (Silmitasertib, CX4945) is a potent, selective, orally bioavailable, ATP-competitive inhibitor of protein kinase Casein Kinase 2 (CK2) with Ki of 0.38 nM, CK2α IC50 of 1 nM; displays good selectivity profile against a panel of 238 kinases; attenuates PI3K/Akt signaling, blocks CK2-dependent HIF-1α transcription, caused cell cycle arrest and selectively induces apoptosis in cancer cells relative to normal cells; exhibits antitumor efficacy in murine xenograft models.

Blood Cancer

Phase 2 Clinical

PC-42523

D4476

301836-43-1

D4476 (Casein Kinase I Inhibitor, D 4476, D-4476) is a potent, selective ATP-competitive inhibitor of CK1 with IC50 of 0.3 uM in vitro; slightly weaker for ALK5 inhibition (IC50=0.5 uM); weak activity for p38α MAPK and no activity for PKB, SGK; specifically inhibits the phosphorylation of endogenous FOXO1a on Ser322 and Ser325; more potent and specific than IC261 or CKI-7.

PC-42026

SR-3029

1454585-06-8

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.

PC-36054

ON108110

1415599-79-9 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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