cdk2/a

CDK2 acetate is a member of the eukaryotic S/T protein kinase family and its function is to catalyze the phosphoryl transfer of ATP γ-phosphate to serine or threonine hydroxyl (denoted as S0/T0) in a protein substrate.

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

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

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 degrader4 (compound 104) is a potent degrader of CDK2, showing promise for cancer research applications.

CDK2 Degrader 5 (compound 12) is a degrader targeting cyclin-dependent kinase 2 (CDK2). In a HiBiT assay system, CDK2 Degrader 5 (compound 12) exhibits a moderate level of degradation efficiency, with a maximum degradation (Dmax) of approximately 50–80%.

CDK2/FLT4/PDGFRA-IN-1 (Compound 4a) is a potent inhibitor of CDK2/cyclin A, FLT4 (VEGFR3), and PDGFRA, with IC50 values of 1.672, 0.554, and 0.629 μM respectively. This compound demonstrates significant antiproliferative effects on cancer cells, including lung cancer EBC-1, pancreatic ductal adenocarcinoma AsPC-1, and colorectal cancer HT-29 cells. Additionally, CDK2/FLT4/PDGFRA-IN-1 can induce apoptosis in these cancer cells.

CDK2 degrader6 (compound 6) is an orally active CDK2 degrader with a DC50 of 46.5 nM, and is applicable in breast cancer research.

CDK2ligand-2 is a PROTAC target protein ligand (Ligands for Target Protein for PROTAC). It can be used in conjunction with E3Ligase Ligand-linker Conjugate 184 to synthesize a PROTAC degrader (CDK2 degrader2).

CDK2/MDM2-IN-1 (III-13) is a dual inhibitor targeting both CDK2 and MDM2, exhibiting an IC50 value of 2.60 nM against CDK2, and demonstrating antitumor activity.

(R)-CDK2 degrader 6 (Compound 7) is the R enantiomer of CDK2 degrader 6. It functions as a selective molecular glue degrader for CDK2, with a DC50 of 27.0 nM within 24 hours. This compound can be utilized in breast cancer research.

(S)-CDK2 degrader 6 (Compound 8) is the S-enantiomer of CDK2 degrader 6. This selective CDK2 molecular glue degrader has a DC50 of 166.7 nM within 24 hours and is applicable in breast cancer research.

CDK2 degrader 8 is a novel bifunctional protein degrader (PROTAC) developed based on patent WO 2025/181261, featuring Cyclopropyl and 1,3,4-Oxadiazole scaffolds. This compound facilitates the formation of a ternary complex between CDK2 and an E3 ubiquitin ligase, mediating the selective ubiquitination and subsequent proteasomal degradation of the target protein. In experimental models, it effectively blocks tumor cell cycle progression by depleting CDK2 levels, thereby demonstrating potent anti-proliferative activity.

CDK2-IN-55 is a potent and highly selective cyclin-dependent kinase 2 (CDK2) inhibitor (IC50 = 15 nM). It disrupts the cell cycle machinery to specifically induce G1/S phase arrest in cancer cells, showing excellent anti-clonogenic and anti-proliferative activities in various gastrointestinal tumor models.

CDK2/4 ligand 1 is a ligand for the target proteins in PROTACs, specifically targeting CDK2/4. It is utilized in the synthesis of PROTAC CDK2/4 Degrader-1.

PROTACCDK2/4 Degrader-1 (Compound 5) is a potent CDK2/4 PROTAC degrader with a DC50 of ≤ 10 nM for both CDK2 and CDK4. It demonstrates excellent activity in inhibiting cell proliferation in OVCAR3 and T47D cell lines. This compound is applicable for breast cancer and ovarian cancer research.

PROTACCDK2/4/6 Degrader-1 is an orally active CDK2/CDK4/CDK6 PROTAC degrader. It is a prodrug created through a one-step reaction from PROTACCDK2/4/6 Degrader-2 using chloromethylnorvaline ester. This compound is applicable in research related to malignant melanoma.

PROTACCDK2/4/6 Degrader-2 is a PROTAC degrader specifically targeting CDK2/4/6. It can react in a single step with pivaloyl chloride to convert into the prodrug PROTACCDK2/4/6 Degrader-1. In malignant melanoma cells, this compound effectively degrades CDK2/4/6 proteins and their complexes, leading to cell cycle arrest and apoptosis, with a pronounced effect on melanoma cells. PROTACCDK2/4/6 Degrader-2 is valuable for related malignant melanoma research.

Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL), a CDK2 inhibitor, exhibits dose-dependent cytotoxic effects on U2OS osteosarcoma cells [1].

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].

CDK2 degrader2 is a PROTAC class CDK2 degrader that targets the CDK2 protein for ubiquitination, facilitating its degradation via the ubiquitin-proteasome pathway (UPP). It effectively degrades CDK2 in MKN1 cells, with a DC50 value of less than 100 nM and an average Dmax greater than 75%.

CDK2/4-IN-1 (compound B-4a) serves as both a CDK2/4 inhibitor and a microtubule polymerization inhibitor, making it useful in cancer research.

CDK2, a eukaryotic S/T protein kinase family member, catalyzes the phosphoryl transfer from ATP γ-phosphate to the hydroxyl of serine or threonine (denoted as S0/T0) in a protein substrate.