| DC47881 |
TMX-4116
|
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. |
| DC8146 |
PF-5006739
|
PF-5006739 is a potent inhibitor of casein kinases 1 delta (CK1δ) and 1 epsilon (CK1ε) |
| DC11250 |
Casein Kinase inhibitor A51
|
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. |
| DC74572 |
DEG-77
|
DEG-77 is a cereblon-dependent degrader of IKZF2 and casein kinase 1α (CK1α). It blocks cell growth and delays leukemia progression in murine and human acute myeloid leukemia (AML) mouse models. |
| DC74448 |
SR-4133
|
SR-4133 (SR4133) is a potent and highly selective CK1ε isoform inhibitor with IC50 of 58 nM, no significant acitivity agianst CK1δ (IC50>10,000 nM). |
| DC74447 |
SGC-CK2-1 analog 2h
|
SGC-CK2-1 analog 2h is potent, selective and in vivo active inhibitor of casein kinase 2α (CSNK2A, CK2α) with pIC50 of 7.5 and 7.7 against CSNK2A1 and CSNK2A2, respectively. |
| DC74445 |
FL-1607
|
FL-1607 is a novel Fam20C inhibitor with potent anti-proliferative effects on TNBC cells, induces apoptosis and inhibits migration in MDA-MB-468 cells. |
| DC74444 |
CKR-49-17
|
CKR-49-17 is a potent, allosteric small molecule activator of CK1γ2 with Kd value of 180 nM in MST assays. |
| DC74443 |
AB668
|
AB668 is a selective, bivalent Casein Kinase 2 (CK2) inhibitor targeting the ATP site and the αD pocket, AB668 inhibits the CK2 holoenzyme with Ki value of 41 nM (IC50=65 nM). |
| 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. |
