CDK4/6-IN-6

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-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 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 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-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).

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).

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-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-11 is a potent PROTAC CDK4 6 degrader.

CDK4 6-IN-17 (compound 12) is an orally bioavailable inhibitor of CDK4 6, exhibiting potent activity with IC50 values between 10-100 nM in BE(2) cells, and has demonstrated efficacy in inhibiting tumor growth in the COLO205 xenograft model [1].

CDK4 6-IN-21 (compound I-52) is a CDK4 6 inhibitor with IC50 values of 3.88 nM for CDK4 and 3.31 nM for CDK6, exhibiting antitumor activity.

CDK4 6-IN-21 maleate (compound I-52) is a potent inhibitor of CDK4 and CDK6, with IC50 values of 3.88 nM and 3.31 nM, respectively. This compound exhibits antitumor activity.

CDK4 6-IN-22 (Compound 1-A) is a dual inhibitor of CDK4 and CDK6.

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.

CDK4 6-IN-19 (Compound II-7) serves as an inhibitor of CDK4 and CDK6, exhibiting IC 50 values of 0.2 nM and 5.0 nM, respectively. Additionally, it suppresses cell proliferation and is applicable in cancer research.

CDK4 6-IN-20 (Compound II-5) is an inhibitor targeting CDK4 and CDK6, exhibiting IC 50 values of 1.9 and 14.2 nM, respectively. Additionally, it suppresses cell proliferation and is applicable in cancer research.

Abemaciclib metabolite M20 (CDK4 6-IN-4) is an active metabolite of Abemaciclib. Abemaciclib metabolite M20 is a selective CDK4 6 inhibitor and can be used for researches on the treatment of cancer.

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].