| S1116 |
PD-0332991 (Palbociclib) Hydrochloride
|
Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
|
-
Nature, 2025, 10.1038/s41586-025-09328-w
-
Cancer Discov, 2025, 10.1158/2159-8290.CD-24-1378
-
Nat Commun, 2025, 16(1):6677
|
|
| S5716 |
Abemaciclib (LY2835219)
|
Abemaciclib is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively.
|
-
Nat Genet, 2025, 57(6):1452-1462
-
Nat Commun, 2025, 16(1):4254
-
Mol Cell, 2025, S1097-2765(25)00042-5
|
|
| S8903 |
AS2863619
|
AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in Tconv cells.
|
-
Science, 2022, 378(6620):eabn5647
|
|
| S7440 |
LEE011 (Ribociclib)
|
Ribociclib is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.
|
-
Nat Commun, 2025, 16(1):2132
-
Cell Rep Med, 2025, S2666-3791(25)00231-9
-
EMBO J, 2025, 10.1038/s44318-025-00554-6
|
|
| S7747 |
Ro-3306
|
RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
|
-
Nat Commun, 2025, 16(1):7898
-
Nat Commun, 2025, 16(1):6439
-
Nucleic Acids Res, 2025, 53(21)gkaf1179
|
|
| S4482 |
Palbociclib (PD-0332991)
|
Palbociclib (PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively.This product has poor solubility, animal in vivo experiments are available, cell experiments please choose carefully!
|
-
Signal Transduct Target Ther, 2025, 10(1):363
-
Drug Resist Updat, 2025, 78:101161
-
Nat Commun, 2025, 16(1):7622
|
|
| S8840 |
SEL120 (SEL120-34A) hydrochloride
|
SEL120 (SEL120-34, SEL120-34A) is a novel inhibitor of Cyclin-dependent kinase 8 (CDK8) with IC50 values of 4.4 nM and 10.4 nM for CDK8/Cyclin C and CDK19/CyclinC respectively.
|
-
Cell Rep Med, 2025, S2666-3791(25)00231-9
-
Nature, 2024, 10.1038/s41586-024-08314-y
-
Endocrinology, 2024, 165(10)bqae114
|
|
| E1854 |
INX-315
|
INX-315 is an orally active and selective inhibitor of CDK2 that induces cell cycle arrest in the G1 phase. It exhibits an IC50 value of 2.3 nM in intracellular NanoBRET assay, respectively. It displays a 50-fold increased CDK2 selectivity compared to CDK1. INX-315 decreases the phosphorylation of CDK2 substrates and suppresses tumor growth in xenograft mouse models in a dose-dependent manner.
|
|
|
| S7158 |
LY2835219 (Abemaciclib) Mesylate
|
Abemaciclib mesylate is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.
|
-
Cell Rep Med, 2025, S2666-3791(25)00231-9
-
EBioMedicine, 2025, 118:105828
-
NPJ Breast Cancer, 2025, 11(1):39
|
|
| S9878 |
Tagtociclib (PF-07104091)
|
Tagtociclib (PF-07104091) inhibits CDK2, which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation.
|
-
JCI Insight, 2025, e189901
-
Nat Commun, 2024, 15(1):9181
|
|