cdk-2-in-4

CDK2-IN-4 is a potent and selective inhibitor of CDK2 with an IC50 of 44 nM for CDK2/cyclin A. It shows 2,000-fold selectivity over CDK1/cyclin B with IC50 of 86 uM.

EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor targeting EGFR and CDK-2, with IC50 values of 89.6 nM for EGFR and 165.4 nM for CDK-2. It induces apoptosis and S phase cell cycle arrest in MCF-7 cells, showing significant anti-cancer activity with an IC50 of 2.74 μM against MCF-7 cells [1].

CDK2-IN-41 (Compound 7a) is a CDK2 inhibitor that impedes the cell cycle by binding to CDK2, leading to cytotoxicity, increased ROS production, and apoptosis (Apoptosis). It exhibits anticancer activity with an IC50 of 10 µM against acute myeloid leukemia (AML) HL-60 cells. CDK2-IN-41 is applicable in research related to AML-associated cancers.

CDK9-IN-40 is an inhibitor of CDK2 (Cyclin-dependent kinase 2). It effectively inhibits CDK2/Cyclin E1, with an IC50 of ≤ 10 nM.

CDK2-IN-43 (Compound 3a) is a CDK2-cyclin E2 inhibitor with an IC50 value of 6.0 nM. It is applicable to cancer research.

CDK2-IN-42 (Compound H63) is a CDK12 inhibitor with an IC50 of 10 nM. It exhibits activity against ESCC cells by blocking transcription elongation, downregulating core G1 phase genes to induce cell cycle arrest, and altering the CDK12-ATM/ATR-CHEK1/CHEK2 signaling pathway, leading to DNA damage. Additionally, CDK2-IN-42 effectively inhibits tumor growth in human ESCC KYSE150 xenograft mouse models, holding promise for cancer research.

CDK2-IN-44 (Compound 46) is an inhibitor of cyclin-dependent kinase 2 (CDK2). It effectively suppresses the proliferation of cancer cells by arresting the cell cycle, promoting apoptosis (Apoptosis), and inducing cellular senescence. This compound shows potential in research related to ovarian and breast cancers.

CDK2-IN-45 is a CDK2 inhibitor with an IC50 value of 0.64 μM. It effectively inhibits the proliferation of DU-145 and PC-3 cell lines, with IC50 values of 2.20 μM and 4.17 μM, respectively. Additionally, CDK2-IN-45 induces G0/G1 phase cell cycle arrest and apoptosis. It is utilized in prostate cancer research.

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

VEGFR-2-IN-69 (Compound 5A) is an inhibitor of VEGFR-2 and telomerase (Telomerase) that enhances the expression of caspase 3, caspase 8, and caspase 9, while reducing the levels of CDK-2, CDK-4, and CDK-6. It has an IC50 of 15.46 µM against HCT116.

LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1]. [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non-Small Cell Lung Cancer: A Phase Ib Study. [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78, and 0.87 μM for CDK1, CDK2, and CDK4, respectively. It can be used in cancer research to arrest the cell cycle at the G2/M phase and induce apoptosis, elevating Bax, caspase-3, and P53 levels while decreasing Bcl-2 levels [1].

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.

CDK2-IN-18 (compound 8q) serves as a powerful inhibitor of CDK 2/E and CDK 4/D1, showing IC50 values of 8 nM and 46 nM, respectively. It effectively inhibits tumor cell proliferation [1].