The ubiquitous Ser/Thr kinases known as casein kinases (CKs) control a variety of cellular processes in eukaryotes, including the phosphorylation of proteins that are targets for degradation by the ubiquitin-proteasome system (UPS). Casein kinase-1 (CK-1) and casein kinase-2 (CK-2) have both been extensively characterized.
Mammals have at least seven different isoforms of CK1 kinases (,, 1-3,, and ), and these enzymes phosphorylate different substrates to participate in a variety of physiological processes including DNA repair, cell cycle progression, cytokinesis, differentiation, and apoptosis.A highly pleiotropic serine-threonine kinase called casein kinase 2 (CK2) phosphorylated more than 300 proteins, many of which are involved in the regulation of cellular processes like signal transduction, transcriptional control, apoptosis, and the cell cycle.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V52838 | (E/Z)-GO289 | 694522-87-7 | (E/Z)-GO289 is a potent and specific inhibitor of casein kinase 2 (CK2) (IC50=7 nM). |
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V9819 | Quinalizarin | 81-61-8 | Quinalizarin is a potent, ATP-competitive, and highly selective (IC50 >1μM against CK1 and 72 other kinases) casein Kinase II (CK2) inhibitor (IC50= 110nM),superior to the first-in-class CK2 inhibitor, CX-4945. |
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V55064 | Ac-ESMD-CHO | 191338-87-1 | Ac-ESMD-CHO is an inhibitor (blocker/antagonist) of caspase-3 and caspase-7. |
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V55062 | Ac-VDVAD-CHO | 194022-51-0 | Ac-VDVAD-CHO is a caspase-2/3 inhibitor (IC50= 46 and 15 nM). |
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V119348 | AH081 | AH081 (compound 38) is a CK1δ/ε PROTAC degrader. | |
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V52425 | AMG-548 dihydrochloride | 2518299-32-4 | AMG-548 di-HCl is an orally bioactive, selective p38α inhibitor (Ki=0.5 nM), slightly selective for p38β (Ki=36 nM) and >1000-fold selective for p38γ and p38δ. |
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V52424 | AMG-548 hydrochloride | 2437438-16-7 | AMG-548 HCl is an orally bioactive, selective p38α inhibitor (Ki=0.5 nM), slightly selective for p38β (Ki=36 nM) and >1000-fold selective for p38γ and p38δ. |
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V85448 | Antiproliferative agent-46 | ||
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V115346 | APL-5125 | 2830619-57-1 | APL-5125 (compound 61f) is a highly effective, selective, and orally available ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. |
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V108996 | BMS-135 | 1541248-36-5 | BMS-135 is a highly potent and selective ATP-competitive casein kinase 2 (CK2) inhibitor with IC50 values of 0.8 nM and 0.3 nM for the CK2α and CK2α' isoforms, respectively. |
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V109120 | BMS-159 | 1541248-45-6 | BMS-159 is an orally effective direct phosphate prodrug of BMS-135. |
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V99683 | BMS-986397 | 2564486-44-6 | BMS-986397 is a cereblon-based CK1α (casein kinase 1α) molecular glue degrader that causes rapid apoptosis and cell cycle arrest in TP53 wild-type AML (acute myeloid leukemia) cells. |
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V52313 | BTX161 | 2052301-24-1 | BTX161, a Thalidomide analogue, is a potent CKIα degrader. |
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V116126 | CAM4066 | 2101206-81-7 | CAM4066 is a potent CK2α inhibitor with an IC50 value of 300 nM. |
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V69794 | Casein kinase 1δ-IN-1 | 851871-94-8 | Casein kinase 1δ-IN-1 (compound 822) is an inhibitor (blocker/antagonist) of casein kinase 1δ (CK1δ) with an inhibitory effect of greater than 5%. |
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V69793 | Casein kinase 1δ-IN-10 | 332074-85-8 | Casein kinase 1δ-IN-10 is a casein kinase 1δ (CK1δ) inhibitor (WO2012080729A2; compound 685). |
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V69789 | Casein kinase 1δ-IN-14 | 793722-88-0 | Casein kinase 1δ-IN-14 (compound 481) is a casein kinase inhibitor that may be utilized to study neurodegenerative diseases such as AD/Alzheimer's disease. |
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V88599 | Casein kinase 1δ-IN-15 | 2765264-27-3 | Casein kinase 1δ-IN-15 is an inhibitor of casein kinase 1 (CK1δ) with IC50 of 0.045 μM. |
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V69792 | Casein kinase 1δ-IN-3 | 349438-77-3 | Casein kinase 1δ-IN-3 (Compound 23a) is a casein kinase 1δ (CK1d) inhibitor (antagonist) with pIC50 of 6.5376 M. |
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V69791 | Casein kinase 1δ-IN-4 | 851168-98-4 | Casein kinase 1δ-IN-4 (compound 567) is a potent inhibitor of casein kinase 1δ. |