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-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.

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.

Olomoucine II is a potent cyclin-dependent kinase inhibitor with IC50 values of 7.6, 0.1, 19.8, 0.45, and 0.06 μM for CDK1, CDK2, CDK4, CDK7, and CDK9, respectively. Olomoucine II demonstrates high selectivity over numerous other kinases while retaining measurable activity against ERK2 and ABCB1, allowing it to modulate multidrug resistance pathways. Olomoucine II suppresses proliferation across cancer cell lines regardless of p53 status and exhibits synergistic action with daunorubicin in ABCB1-expressing HCT-8 cells.Olomoucine II additionally inhibits replication of HSV-1, HSV-2, vaccinia virus, adenovirus 4, and human CMV, making Olomoucine II an important antiviral and anticancer research tool.

CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1).

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-1 exhibits potent inhibitory activity towards CDK2/4/6 and HDAC6, with IC50 values of 60.9 ± 2.9 nM, 276 ± 22.3 nM, 27.2 ± 4.2 nM, and 128.6 ± 0.4 nM, respectively.

CDK-IN-9 (compound 24) is a potent inhibitor of CDK and acts on CDK2/E (IC50: 4 nM). It functions as a molecular gel that induces interaction between CDK12 and DDB1, and can dephosphorylate retinoblastoma protein and RNA polymerase II, thereby inducing apoptosis.

CDK1-IN-4 (10d) is a selective CDK1 inhibitor that acts on CDK1 (IC50: 44.52 nM), CDK2 (IC50: 624.93 nM), and CDK5 (IC50: 135.22 nM). It affects the cell cycle, inhibiting the growth of cancer cells, and can be used in cancer research.