| DC74445 |
FL-1607
|
FL-1607, a novel Fam20C inhibitor, has shown remarkable anti-proliferative effects in triple-negative breast cancer (TNBC) cells. This compound induces apoptosis and significantly reduces the migration ability of MDA-MB-468 cells, underscoring its potential as a promising therapeutic agent for TNBC treatment. |
| DC11791 |
SSTC3
|
SSTC3 is a novel small-molecule CK1α activator with EC50 of 30 nM (WNT-driven reporter gene assay), Kd of 32 nM. |
| DC8146 |
PF-5006739
|
PF-5006739 is a potent inhibitor of casein kinases 1 delta (CK1δ) and 1 epsilon (CK1ε) |
| DC11251 |
Casein Kinase inhibitor A86
|
CKIα inhibitor A86 is a groundbreaking pan-specific inhibitor targeting Casein Kinase I (CSNK1), with a remarkable binding affinity (Kd=1-10 nM) and a specific Kd of 9.8 nM for CKIα. Beyond its primary activity, this compound also demonstrates dual inhibitory effects on the transcriptional kinases CDK7 and CDK9. Notably, it exhibits minimal to no inhibition against CDK8, CDK13, CDK11a, CDK11b, and CDK19, highlighting its selective pharmacological profile. |
| 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. |
| DC11950 |
SR-2890
|
A potent, highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 4 nM for CK1δ. |
| DC81781 |
ZD-2767P
|
ZD-2767P (Compound 1) is a reversible and competitive inhibitor of IDH1, with its IC50 value being 410 nM. |
| DC81440 |
RB-105
|
RB-105 is an inhibitor of angiotensin-converting enzyme (ACE) (Ki = 4.2 nM) and neutral endopeptidase (NEP) (Ki = 1.7 nM). RB-105 after inhibiting ACE reduces the production of Ang II and increase the level of bradykinin. RB-105 after inhibiting NEP increases the level of natriuretic peptide and further increases the level of bradykinin, thereby generating a powerful synergistic effect. RB-105 has significant antihypertensive and natriuretic effects in both spontaneously hypertensive rats and normal blood pressure rats. RB-105 can be used for research on hypertension. |
| DC80688 |
G9a-IN-4
|
G9a-IN-4 is a G9a inhibitor with high selectivity (IC50 = 32 nM). G9a-IN-4 shows high selectivity against the other tested lysine/arginine methyltransferases. G9a-IN-4 exhibits high enzymatic activity against G9a and more potent antiproliferative effects against all tested cancer cells. G9a-IN-4 significantly suppresses the H3K9me2 level. G9a-IN-4 triggers autophagy by inducing the production of ROS, thus leading to cell apoptosis and cell cycle arrest at G0/G1 in CT26 colon cells. G9a-IN-4 can be used for the study of colon cancer. |
| DC80450 |
CK1-IN-5
|
CK1-IN-5 (compound B-AZ) is an inhibitor of CK1. CK1-IN-5 lengthened the circadian period by inhibits AtCKL3/AtCKL4 activity. |
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