cdk5 in 1

CDK5-IN-1 is a highly potent inhibitor of CDK5, displaying an inhibitory activity of less than 10 nM. This potent compound is specifically employed in scientific investigations relating to kidney diseases.

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].

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].

5-HT6 inverse agonist 1 (Compound 33) is an antagonist of the 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. This compound can inhibit 5-HT6R-mediated Cdk5 and mTOR signaling pathways and reduce tactile allodynia induced by spinal nerve ligation (SNL) in rat models.

CP681301 is a potent inhibitor of CDK5 with antiproliferative activity. CP681301 exhibits anti-tumor activity in Drosophila. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in Glioma stem cells (GSCs). CP681301 reduces self-renewal in mouse glioma xenografts [1].

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.