CDK2-IN-3

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

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].

GSK-3 CDK5 CDK2-IN-1 is an imidazole derivative compound that inhibits cdk5, cdk2, and GSK-3.it has demonstrated applications in cancer research and the study of neurodegenerative diseases [1].

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.

CDK2-IN-36 (compound 1) is a CDK2 inhibitor with antitumor activity.

CDK2-IN-37 (COMPOUND 2) is an inhibitor of cyclin-dependent kinase 2 (CDK2) and exhibits anticancer properties.

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

SY-5609 (CDK7-IN-3) is a selective non-covalent CDK7 inhibitor (Kd value is 0.07 nM), with weak inhibitory activity against CDK2, CDK9 and CDK12 with IC50 values ​​of 5.5, 1.9 and 1.7 μM, respectively, and has anti-tumor activity and inhibits cell apoptosis.

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.

AG-024322 is a potent ATP-competitive inhibitor targeting pan-CDK, effectively inhibiting cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range (1-3 nM).

3-Methylthienyl-carbonyl-JNJ-7706621 is a highly potent and selective inhibitor of cyclin-dependent kinase (CDK), showing IC50 values of 6.4 nM for CDK1 cyclin B and 2 nM for CDK2 cyclin A. It also exhibits potent inhibition of GSK-3 (IC50 = 0.041 μM) and moderate inhibition of CDK4, VEGF-R2, and FGF-R2 (IC50 = 0.11 μM, 0.13 μM, and 0.22 μM, respectively), making it significant for cancer research.

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].

CDK5-IN-3 is a selective and potent CDK5 inhibitor that inhibits CDK5 p25 and CDK2 CycA and can be used in the study of cancer.

CDK1-IN-3 (8g) is a selective CDK1 inhibitor with IC50 values of 36.8 nM for CDK1, 305.17 nM for CDK2, and 369.37 nM for CDK5. CDK1-IN-3 can affect the cell cycle, inhibit cancer cell growth, and is suitable for use in cancer research.

1. Ginsenoside Rg5 could be a beneficial agent for the treatment of Alzheimer's disease. 2. Ginsenoside Rg5 suppresses LPS-induced nitric oxide (NO) production and proinflammatory TNF-α secretion. 3. Ginsenoside Rg5 can ameliorate lung inflammation possib

QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.

CDK2 degrader1 (Compound 3) is an orally active cyclin-dependent kinase 2 (CDK2) degrader based on PROTAC technology. It binds to cerebellum, inducing ubiquitination of CDK2 followed by proteasomal degradation pathway. CDK2 degrader1 is utilized in the research of multiple cancers.

PI3K AKT-IN-4 (compound 3), a diterpenoid extracted from the roots and rhizomes of Salvia castanea Dielsf., exhibits antitumor properties by inhibiting cell viability and proliferation (IC 50 =4.72 μM) and promoting apoptosis in Hep3B cells. This compound obstructs the G0 G1 phase of the cell cycle, triggers mitochondrial dysfunction, and induces oxidative stress. Moreover, PI3K AKT-IN-4 combats hepatocellular carcinoma through the inhibition of the PI3K-Akt signaling pathway and by interacting with PARP1 and CDK2 targets.