cdk-7-in-1

THZ2 (CDK7-IN-1), an analog of THZ1, is a potent and selective CDK7 inhibitor(IC50:13.9 nM),with the potential to treat Triple-negative breast cancer (TNBC).

CDK7-IN-1 is an analog derived from YKL-5-124 and functions as an inhibitor of cyclin-dependent kinase 7 (cdk7). It exhibits strong inhibitory activity, with an IC50 value of less than 100 nM (WO 2016105528 A2, Compound 215).

Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.1,2 It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 μg/ml for both).1 Roccellic acid (100 μg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.2 |1. Sweidan, A., Chollet-Krugler, M., Sauvager, A., et al. Antibacterial activities of natural lichen compounds against Streptococcus gordonii and Porphyromonas gingivalis. Fitoterapia 121, 164-169 (2017).|2. Mishra, T., Shukla, S., Meena, S., et al. Isolation and identification of cytotoxic compounds from a fruticose lichen Roccella montagnei, and it's in silico docking study against CDK-10. Rev. Bras. Farmacogn. 27(6), 724-728 (2017).

6-Chloro-2-fluoropurine is a heterocyclic building block.1,2It has been used in the synthesis of purine nucleosides that inhibit cyclin-dependent kinases (CDKs)in vitro.16-Chloro-2-fluoropurine has also been used in the synthesis of purine nucleosides that are active against HIV-1 and hepatitis B virus (HBV)in vitro.2 1.Wilson, S.C., Atrash, B., Barlow, C., et al.Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitorsBioorg. Med. Chem.19(22)6949-6965(2011) 2.Lee, K., Choi, Y., Gullen, E., et al.Synthesis and anti-HIV and anti-HBV activities of 2'-fluoro-2',3'-unsaturated L-nucleosidesJ. Med. Chem.42(7)1320-1328(1999)

CDK7 9-IN-1 is a specific inhibitor of cyclin-dependent kinases 7 9 (CDK7 9), targeting CDK7 with IC50 values of 0.0656 μM without pre-incubation and 0.00574 μM after 3 hours pre-incubation, and displaying inhibitory activity against CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation, making it valuable for cancer research.

CDK7-IN-16 (Compound 9) is a potent inhibitor of CDK 7 (IC50: 1-10 nM). CDK7-IN-16 can be used in research against cancer, particularly cancers with transcriptional abnormalities.

CDK4 6-IN-14 is a potent, highly selective inhibitor of Cyclin-Dependent Kinases 4 and 6 (CDK4 6), with inhibition concentrations (IC50s) of 10 nM and 16 nM, respectively. It shows over 60-fold selectivity for CDK4 6 compared to CDKs 1, 2, 7, and 9, and exhibits significant selectivity against 205 other kinases.

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].

CDK7-IN-25 (CY-16-1) is a highly potent CDK7 inhibitor with an IC50 of less than 1nM, used in cancer research [1].