| DC11952 |
(R)-DRF053 dihydrochloride |
(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. |
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| DC11790 |
VU-WS211 |
A negative control of VU-WS113, which is a potent inhibitor of Wnt signaling with EC50 of 80 nM that selectively potentiates CK1α kinase activity.. |
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| DC11950 |
SR-2890
Featured
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A potent, highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 4 nM for CK1δ. |
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| DC11948 |
CK2 inhibitor D11 |
A potent, selective, cell permeab anti-apoptotic protein kinase CK2 with Ki of 5 nM. |
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| DC11951 |
Bischof-5 |
A potent, specfic casein kinase 1δ (CK1δ) inhibitor with IC50 of 40 nM. |
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| DC11949 |
SR-653234 |
A purine scaffold casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 160/540 nM, respectively.. |
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| DC11788 |
Pyrvinium Iodide |
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. |
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| DC11787 |
Pyrvinium |
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. |
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| DC11252 |
BTX161 |
BTX161 is a thalidomide analog that mediates degradation of CKIα better than lenalidomide in human AML cells and activates DDR and p53, while stabilizing the p53 antagonist MDM2. |
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| DC11250 |
Casein Kinase inhibitor A51
Featured
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Casein Kinase inhibitor A51 (CKIα inhibitor A51) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=0.5-20 nM, CKIα Kd=5.3 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19; target both CDK7 and CDK9 with low nM Kd values; induces leukemia cell apoptosis at <160 nM, in correlation to the capacity to stabilize p53; shows high and selective sensitivity against leukemic CFUs in colony-forming unit (CFU) assay, without effect on normal hematopoietic CFUs; blocking CKIα together with CDK7 and/or CDK9 synergistically stabilize p53, deprive leukemia cells of survival and proliferation-maintaining SE-driven oncogenes, induce apoptosis, abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1; demonstrates therapeutic efficacy with preserved hematopoiesis and leukemia cure potential in AML mouse models. |
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| DC11251 |
Casein Kinase inhibitor A86 |
Casein Kinase inhibitor A86 (CKIα inhibitor A86) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=1-10 nM, CKIα Kd=9.8 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19. |
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| DC7111 |
CX-4945 (Silmitasertib)
Featured
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CX-4945 (Silmitasertib) is a potent and selective ATP-competitive small molecule protein kinase CK2 inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively. |
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| DC7011 |
D4476 (D-4476)
Featured
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D4476, a cell-permeant inhibitor of CK1δ (IC90 <10 uM), suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a, D4476 originally identified as inhibitors of activin receptor-like kinase ALK5. |
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| DC9730 |
IC-261(SU-5607)
Featured
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IC261 is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM. |
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| DC8146 |
PF-5006739
Featured
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PF-5006739 is a potent inhibitor of casein kinases 1 delta (CK1δ) and 1 epsilon (CK1ε) |
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| DC9782 |
SR-3029
Featured
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SR 3029 is a potent and highly specific CK1δ/CK1ε inhibitor with the IC50 of 97 nM. |
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| DC11791 |
SSTC3 |
SSTC3 is a novel small-molecule CK1α activator with EC50 of 30 nM (WNT-driven reporter gene assay), Kd of 32 nM. |
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| DC9301 |
TA-01
Featured
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TA-01 induces cardiomyocyte differentiation from human embryonic stem cells following mesoderm induction at 1 μM. Inhibits cardiomyocyte differentiation at 5 μM. Potently inhibits CK1ε, p38α, and CK1δ (IC50 values are 6.4, 6.7 and 6.8 nM respectively). |
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| DC11789 |
VU-WS113 |
VU-WS113 is a potent inhibitor of Wnt signaling with EC50 of 80 nM that selectively potentiates CK1α kinase activity.. |
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| DC28717 |
CKI-7 |
CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases. |
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| DC40122 |
TBCA |
TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases. |
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| DC44833 |
CK2/PIM1-IN-1 |
CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1, with IC50s of 3.787 μM and 4.327 μM for CK2 and PIM1, respectively. CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders. |
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| DC46935 |
SR-1277 |
SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer. |
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| DC47881 |
TMX-4116
Featured
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TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC50s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma. |
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| DC47903 |
SGC-CK2-1 |
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases. |
|
| DC70196 |
Pyrvinium pamoate |
An anthelmintic effective agent 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. |
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| DC70308 |
CIGB-300 |
CIGB-300 (P15-Tat) is a cell-permeable cyclic peptide that modulates CK2 (CSNK2) activity by binding to the phosphoacceptor site on CK2 targets, abrogates the CK2 phosphorylation by blocking recombinant substrates in vitro.CIGB-300 (P15-Tat) induced apoptosis as evidenced by rapid caspase activation and cellular cytotoxicity in a variety of tumor cell lines (HSCLC H-82 cell IC50=20 uM).CIGB-300 (P15-Tat) demonstrated substantial regression of the tumor mass C57BL6 mice bearing day 7-established solid tumors.CIGB-300 (P15-Tat) reduced breast cancer cell growth in MDA-MB-231, MCF-7 and F3II cells, exerting a pro-apoptotic action and cell cycle arrest. CIGB-300 decreased cell adhesion, migration and clonogenic capacity of malignant cells.CIGB-300 may interfere with the SARS-CoV-2 life cycle within infected human cells. |
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| DC70311 |
CK2 inhibitor KN2 |
CK2 inhibitor KN2 is a potent, highly selective, cell-permeable, bivalent CK2 inhibitor, binds to CK2α- and CK2α′-based CK2 holoenzymes with Ki of 6.1 nM (CK2α2β2) and 4.0 nM (CK2α′2β2).KN2 inhibits CK2α- and CK2α′-based CK2 holoenzymes with IC50 of 19.3 nM (CK2α2β2) and 15.6 nM (CK2α′2β2) at 100 uM ATP.KN2 downregulated the CK2-dependent phosphorylation level of Akt phosphorylation at Ser129 (p-Akt S129). |
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| DC72497 |
MU1742 |
MU1742 is a probe for CK1δ and CK1ε protein kinases. |
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| DC72498 |
JNJ-6204 |
JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure. |
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