cdk 4

CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectively.

CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM). CDK4/6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.

CDK4/6-IN-2 is a potent inhibitor of CDK4 and CDK6 [IC50s: 2.7 and 16 nM].

CDK4/6-IN-3, a brain-penetrant CDK4/CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM), is used for the treatment of glioblastoma and inhibits CDK1 with a Ki of 110 nM.

CDK4/6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 nM for CDK4/Cyclin D1 and 4.4 nM for CDK6/Cyclin D3 (WO2019207463A1, example A93).

CDK4/6-IN-14 is a potent, highly selective inhibitor of Cyclin-Dependent Kinases 4 and 6 (CDK4/6), with inhibition concentrations (IC50s) of 10 nM and 16 nM, respectively. It shows over 60-fold selectivity for CDK4/6 compared to CDKs 1, 2, 7, and 9, and exhibits significant selectivity against 205 other kinases.

CDK4/6-IN-23 (Compound 42) is a potent and selective inhibitor of CDK4/6, displaying an IC50 of 11 nM for CDK6. This compound significantly activates immune cells and enhances IL-3 production. In mice undergoing 5-FU chemotherapy, CDK4/6-IN-23 demonstrates dual bone marrow protection and immunomodulatory effects.

CDK4/6/HDAC-IN-1 (Compound N14) is a dual-target inhibitor of CDK4/6 and HDAC, with IC50 values of 7.23 nM for CDK4, 13.20 nM for CDK6, 55.66 nM for HDAC1, and 48.38 nM for HDAC6. It induces apoptosis and G0/G1 phase arrest through the HDAC-p21-CDK signaling pathway and can inhibit hepatocellular carcinoma.

CDK4/9-IN-1 (Compound 29) is a selective dual inhibitor of CDK4 and CDK9, exhibiting IC50 values of 23 nM and 12 nM, respectively. It holds potential for use in cancer research.

CDK4/6-IN-24 (Compound A) is an inhibitor of CDK4/6 with broad-spectrum antitumor activity. It can effectively inhibit various cancer cells, exhibiting an IC50 in the submicromolar range.

CDK4/6/BRD4-IN-1 (B15) is an inhibitor targeting CDK4, CDK6, and BRD4, with IC50 values of 220 nM for BRD4-BD2, 146 nM for BRD4-BD1, 106 nM for CDK6, and 85 nM for CDK4. This compound is applicable for research in non-small cell lung cancer (NSCLC) and can induce cell cycle arrest and apoptosis.

CDK4 degrader1 (ML 1–71) is a molecular glue degrader specifically targeting CDK4.

CDK4/6-IN-15 hydrochloride is an orally active selective inhibitor of CDK4/6. It effectively restrains the growth of cancer cells by arresting the cell cycle at the G1 phase. Additionally, CDK4/6-IN-15 hydrochloride inhibits phosphorylation of the retinoblastoma tumor suppressor protein (Rb) at site S780 and suppresses E2 factor (E2F)-regulated gene expression.

CDK4-IN-3 (Compound 389) is a highly selective irreversible inhibitor of cyclin-dependent kinase 4 (CDK4) with an IC50 of 25 nM and exhibits more than 10-fold selectivity over CDK6. It arrests the cell cycle at the G1 phase and induces apoptosis in tumor cells. CDK4-IN-3 holds potential for research in solid tumors such as breast and lung cancer.

CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor with enzymatic inhibitory activity against CDK4 and CDK6, having IC50 values of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used in cancer research[1].

CDK4/6-IN-7, a highly potent and selective orally active inhibitor of CDK4/6, demonstrates impressive inhibition activity with IC50 values of 1.58 nM and 4.09 nM respectively. This compound is particularly valuable for breast cancer research [1].

CDK4/6-IN-8 (Compound 7p) is a selective inhibitor of CDK4 with an IC50 of 5.01 nM and CDK6 with an IC50 of 3.97 nM.

CDK4/6-IN-9 (compound 10) is a selective inhibitor of CDK4/6, demonstrating activity on CDK6/cyclin D1 (IC50: 905 nM), and holds potential research value in multiple myeloma (MM).

Compounds 10B and 10C, functioning as cdk4/6 inhibitors, demonstrated low nanomolar activity, optimal antiproliferative effects, excellent metabolic properties, and acceptable pharmacokinetics targeting cdk4/6.

FLT3/CDK4-IN-1 is a highly selective, potent, orally active dual inhibitor of FLT3 (IC50: 7 nM) and CDK4 (IC50: 11 nM), demonstrating significant anti-tumor effects in vivo and anti-proliferative effects on certain cancer cells.

CDK4/6-IN-10 is a selective, potent, orally active inhibitor of CDK4 (IC50: 22 nM) and CDK6 (IC50: 10 nM) with antitumour effects, showing potential for studies in multiple myeloma (MM).

SHP2/CDK4-IN-1 (compound 10) is a dual inhibitor targeting SHP2 and CDK4, with oral activity and high potency, showing IC50 values of 4.3 nM for SHP2 and 18.2 nM for CDK4. It induces G0/G1 arrest, inhibits proliferation of TNBC cell lines, and demonstrates significant antitumor efficacy in the EMT6 syngeneic mouse model. This compound is valuable for research into triple-negative breast cancer (TNBC) [1].

CDK4/6-IN-15, an orally active and selective inhibitor of CDK4/6, effectively halts the growth of cancer cells by arresting the cell cycle at the G1 phase and inhibiting the phosphorylation of the retinoblastoma tumor suppressor protein (Rb) at S780, as well as suppressing E2 factor (E2F)-regulated gene expression.

CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader.