cdk2 in 7

CDK2-IN-7 is a CDK2 inhibitor for treating cancer (IC50 < 50 nM).

CDK7-IN-6 is a highly effective and specific inhibitor (IC50 ≤100 nM) of cyclin-dependent kinase 7 (CDK7). It showcases remarkable selectivity, with more than a 200-fold preference for CDK7 over CDK1, CDK2, and CDK5. This compound holds significant potential for cancer research purposes.

CDK HDAC-IN-2 is a potent dual HDAC CDK inhibitor that acts on HDAC1 (IC50: 6.4 nM), HDAC2 (IC50: 0.25 nM), HDAC3 (IC50: 45 nM), HDAC6 and 8 (IC50 > 1000 nM), CDK1 (IC50: 8.63 nM), CDK2 (IC50: 0.30 nM), and CDK4, 6, and 7 (IC50 > 1000 nM). CDK HDAC-IN-2 can arrest the cell cycle in the G2 M phase and induce apoptosis, demonstrating excellent anti-proliferative and significant anti-tumor effects.

CDK7-IN-20 is a potent, selective, and irreversible inhibitor of Cyclin-Dependent Kinase 7 (CDK7) with an IC50 value of 4 nM, exhibiting over 206-fold selectivity against related kinases [CDK1, CDK2, CDK3, CDK5, CDK6, CDK9, and CDK12]. It holds potential for research into autosomal dominant polycystic kidney disease (ADPKD).

Multi-kinase-IN-4 (compound 5d) is a multi-targeted kinase inhibitor effective against VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18, and 2.09 μM, respectively. It shows broad-spectrum anti-cancer activity in HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50: 1.94–7.1 µM) and exhibits lower toxicity in WI-38 cells (IC50 = 40.85 µM). Additionally, it induces apoptosis, causes S-phase cell cycle arrest in HepG2 cells, and holds potential for cancer research [1].

FD2056 is a potent, orally active PI3K inhibitor, with IC50 values of 0.30, 0.80, 1.10, and 0.42 nM against PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. Additionally, it exhibits inhibitory effects on CDK2-CyclinA2 and CDK4-CyclinD3 with IC50s of 115.95 nM and 2782.15 nM. FD2056 effectively inhibits the proliferation of various breast cancer cell lines, such as MDA-MB-231, MDA-MB-468, and MCF-7, with IC50s of 1.06 μM, 0.04 μM, and 1.40 μM, respectively. The compound also promotes apoptosis in cancerous cells and has been shown to suppress tumor growth [1].

EGFR CDK2-IN-2 (compound 6a) is a dual inhibitor targeting EGFR and CDK-2, with IC50 values of 19.6 nM and 87.9 nM, respectively. It induces apoptosis in MCF-7 cells and arrests cell cycle progression in the S phase, demonstrating notable anticancer activity with an IC50 of 0.39 μM [1].

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].

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].

Compound 5K (Multi-target kinase inhibitor 2) is a multi-targeted kinase inhibitor demonstrating activity against EGFR, Her2, VEGFR2, and CDK2 with IC50 values between 40 to 204 nM. It exhibits cytotoxic effects on HepG2, HeLa, MDA-MB-231, and MCF-7 cell lines, with IC50 values of 41, 57, 51, and 59 μM, respectively. Additionally, it induces cell cycle arrest and apoptosis specifically in HepG2 cells.

CDK2-IN-20 (compound 3b), a CDK2 inhibitor, exhibits cytotoxic effects on tumor cells with an IC50 ranging from 5.52-17.09 µM. It arrests the MCF-7 cell cycle at the S phase and induces apoptosis [1].