perk-in-3

PERK-IN-3 is a potent inhibitor of PERK (IC50 of 7.4 nM).

FGFR-IN-25 (Compound 19E) is an FGFR inhibitor with IC50 values of 1.30 nM for FGFR1 and 0.85 nM for FGFR2, and also acts as a radiosensitizer. It effectively reduces the phosphorylation levels of FGFR1 and its downstream effectors, pAKT and pERK. FGFR-IN-25 exhibits broad-spectrum antitumor activity against gastric, colorectal, liver, breast, triple-negative breast cancers, and glioblastoma. When combined with radiation therapy, FGFR-IN-25 synergistically activates the ROS-Caspase-3-GSDME pathway, downregulates PD-L1 expression, and induces immunogenic cell death, thereby enhancing the antitumor effects.

8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland microsomes (IC50= 31 μM).4 1.Crombie, L., and Holloway, S.J.The biosynthesis of calendic acid, octadeca-(8E,10E, 12Z)-trienoic, acid, by developing marigold seeds: origins of (E,E,Z) and (Z,E,Z) conjugated triene acids in higher plantsJ. Chem. Soc. Perk. T. 12425-2434(1985) 2.Yasui, Y., Hosokawa, M., Kohno, H., et al.Growth inhibition and apoptosis induction by all-trans-conjugated linolenic acids on human colon cancer cellsAnticancer Res.26(3A)1855-1860(2006) 3.Shinohara, N., Ito, J., Tsuduki, T., et al.Jacaric acid, a linolenic acid isomer with a conjugated triene system, reduces stearoyl-CoA desaturase expression in liver of miceJ. Oleo Sci.61(8)433-441(2012) 4.Nugteren, D.H., and Christ-Hazelhof, E.Naturally occurring conjugated octadecatrienoic acids are strong inhibitors of prostaglandin biosynthesisProstaglandins33(3)403-417(1987)