Induces p21 expression and S-phase arrest in cancer cells via ERK-mediated pathways. IC50 values are 0.89 and 12.6 μM for LoVo human colon cancer cell line and normal human fibroblasts respectively.
Pestalotin is a fungal metabolite originally isolated from P. cryptomeriaecola with diverse biological activities. It induces reducing sugar release in embryoless rice endosperms when used at concentrations ranging from 3 to 100 mg/L and enhances growth of rice seedlings (O. sativa) when used in combination with gibberellin A3 at concentrations ranging from 30 to 500 mg/L. Pestalotin has antifungal activity, reducing the growth of C. albicans, C. neoformans, T. rubrum, and A. fumigatus (MICs = 12.5, 50, 50, and 50 μg/ml, respectively). It is cytotoxic to HL-60, MKN45, LoVo, and A549 cells (IC50s = 64.87-182.92 μM). Pestalotin has been used as a standard for dereplication of natural products.
ATR-IN-16 (compound 46) is a highly effective ATR kinase inhibitor, exhibiting considerable anticancer activity in LoVo cells, as demonstrated by its IC 50 value of 410 nM [1].
ATR-IN-15 (compound 1) is a highly potent and orally active inhibitor of ATR kinase with an IC50 of 8 nM. Additionally, ATR-IN-15 demonstrates inhibitory activity against several targets, including human colon tumor cells LoVo, DNA-PK, and PI3K, with IC50 values of 47, 663, and 5131 nM, respectively [1].
ATR-IN-14 (compound 1) is a powerful ATR kinase inhibitor that significantly inhibits ATR signaling pathways following CHKI protein phosphorylation, demonstrating a remarkable inhibition rate of 98.03% at 25 nM. Moreover, ATR-IN-14 exhibits notable anticancer efficacy in LoVo cells, displaying an IC50 value of 64 nM [1].