CDK IN 2

CDK-IN-2 (CDK inhibitor II) is a potent and specific CDK9 inhibitor (IC50: <8 nM).

CDK9-IN-2 is a specific CDK9 inhibitor with an IC50 of 5 nM in the A2058 skin cell line (72 hours) and 7 nM in the H929 multiple myeloma cell line (72 hours).

Cdk1/2 Inhibitor III is a selective inhibitor of Cdk1/2 with an IC50 value of 2.1 μM against CDK1/cyclin B.

Cdk2 Inhibitor II is a selective and potent CDK2 inhibitor50 at 60 nM.

CDK2-IN-13 is a potent Cyclin-dependent kinase 2 (CDK2) inhibitor (IC50 value: 12 µM).CDK2-IN-13 is involved in cell cycle regulation and can arrest the cell cycle. CDK2-IN-13 prevents cell division and proliferation, induces apoptosis, and can be used in cancer research.

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

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.

CDK7-IN-2 hydrochloride hydrate (Example 6) is a potent and specific inhibitor of the CDK7 enzyme, exhibiting significant anti-cancer properties.

CDK2-IN-7 is a CDK2 inhibitor for treating cancer (IC50 < 50 nM).

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].

CDK/HDAC-IN-2 is a potent dual HDAC/CDK inhibitor that acts on HDAC1 (IC50: 6.4 nM), HDAC2 (IC50: 0.25 nM), HDAC3 (IC50: 45 nM), HDAC6 and 8 (IC50 > 1000 nM), CDK1 (IC50: 8.63 nM), CDK2 (IC50: 0.30 nM), and CDK4, 6, and 7 (IC50 > 1000 nM). CDK/HDAC-IN-2 can arrest the cell cycle in the G2/M phase and induce apoptosis, demonstrating excellent anti-proliferative and significant anti-tumor effects.

CDK2/Bcl2-IN-1 (compound 1) is a saponin-based inhibitor of CDK-2 (IC50=117.6 nM) with potent cytotoxic effects on cancer cells, also inhibiting Bcl-2 and promoting apoptosis in A549 lung cancer cells [1].

EGFR/CDK2-IN-2 (compound 6a) is a dual inhibitor targeting EGFR and CDK-2, with IC50 values of 19.6 nM and 87.9 nM, respectively. It induces apoptosis in MCF-7 cells and arrests cell cycle progression in the S phase, demonstrating notable anticancer activity with an IC50 of 0.39 μM [1].

EGFR/CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC50 values of 71.7 nM and 113.7 nM, respectively. It induces apoptosis in MCF-7 cells, arrests the cell cycle in the S phase, and exhibits significant anti-cancer cell toxicity, inhibiting MCF-7 cells with an IC50 of 3.16 μM [1].

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-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].

CDK2-IN-26, also known as compound 9, effectively inhibits CDK 2 [1].

PROTAC CDK2/9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1].

PROTAC CDK2 Degrader-1 (Compound 41) is a PROTAC degrader targeting cyclin-dependent kinase 2 (CDK2). It inhibits the phosphorylation of the RB protein in the CDK2-dependent cell line OVCAR3, with an IC50 ranging from 100-500 nM.

CDK2/4-IN-2 (compound 56) serves as a dual inhibitor for CDK2 and CDK4, exhibiting an IC50 of less than 100 nM. It is applicable in cancer research.

CDK2-IN-30 (Formula (I)) is a CDK2 inhibitor with an IC50 of ≤20 nM, utilized primarily in tumor research.

CDK2-IN-32 (Compound 5g) is a selective CDK2 inhibitor with an IC50 of 0.21 μM. It exhibits cytotoxicity towards Vero cells with an IC50 of 28.52 μM.

CDK2-IN-31 (compound I-125A) is an inhibitor of CDK2 and is utilized in cancer research.