cdk2 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.

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.

CDK2/4 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.

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

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

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.

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.

CDK2-IN-47 is a potent CDK2 inhibitor with an IC50 of 0.21 μM. It demonstrates strong anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. It is applicable for research on breast, colorectal, and gastric cancers.

CDK2-IN-48 (Compound 109) is an inhibitor specifically targeting CDK2, which is useful for research into cancers associated with CDK2.

GSK-3 inhibitor 4 is an orally active and brain-permeable compound that acts as a triple inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM (CDK2), and 0.68 μM (CDK5). It effectively reduces Tau protein levels and can be used in the study of Alzheimer's disease.

IMPDH2-IN-4 (compound 2d) is a Mycophenolic acid analog and a selective IMPDH2 inhibitor with a Ki of 1.8 μM. It exhibits potent cytotoxic activity against osteosarcoma cancer cell lines. Additionally, IMPDH2-IN-4 demonstrates high affinity for VEGFR-2, CDK2, and IMPDH.

CDK2-IN-39 (compound 4) is a CDK2 inhibitor.

NUAK1-IN-2 (Compound 24) is an inhibitor of NUAK1 with an IC50 of 3.162 nM, as well as an inhibitor of CDK2/4/6. It is applicable in research related to cancer, neurodevelopmental disorders, and Alzheimer's disease.

WAY-643018 (Compound 2) is an indolecarboxamide derivative that functions as an inhibitor of CDK1, CDK2, and CDK4. CDK1/2/4-IN-2 shows potential for use in cancer research.

Piperidine-4-carbaldehyde (Piperidine-4-carboxaldehyde) serves as a PROTAC linker. It is employed to enhance the binding affinity to target proteins, thereby increasing the degradation efficiency of PROTAC molecules. Additionally, Piperidine-4-carbaldehyde is utilized in the synthesis of CDK2 PROTACs.