cdk-7-in-6

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.

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)

CDK HDAC-IN-2 是有效的 HDAC CDK 双重抑制剂，能够作用于 HDAC1 (IC50: 6.4 nM)、HDAC2 (IC50: 0.25 nM)、HDAC3 (IC50: 45 nM)、HDAC6,8 (IC50>1000 nM)、CDK1 (IC50: 8.63 nM)、CDK2 (IC50: 0.30 nM)、CDK4,6,7 (IC50>1000 nM)。CDK HDAC-IN-2 能够将细胞周期停滞在 G2 M 期，并诱导细胞凋亡 (apoptosis)。CDK HDAC-IN-2 具有优异的抗增殖效果，显示出显著的抗肿瘤作用。

CDK4 6-IN-14 是一种有效且高度选择性的 CDK4和 CDK6(CDK) 抑制剂，IC50分别为 10 nM 和 16 nM。CDK4 6-IN-14 的选择性是 CDK1、2、7 和 9 的 60 多倍，并且在其他 205 种激酶中表现出高选择性。