1,4-DPCA is a potent inhibitor of prolyl-4-hydroxylase with an IC50 of 2.4 µM in human foreskin fibroblasts. 1,4-DPCA can inhibit the α isoenzyme of prolyl-4-hydroxylase and stabilize HIF-1α protein. 1,4-DPCA also inhibits factors that inhibit HIF with an IC50 of 60 µM[1][2].In mouse B6 cells, 1,4-DPCA specifically increases the expression of several target genes, including the pro-angiogenic targets Vegfa and Hmox1, and the proglycolytic targets Ldh-a, Pgk1, Pdk1, and Glut1, after 24 hours of treatment[1].1,4-DPCA significantly reduced cell colony size in T4-2 (10 μM) and ZR-75-1 cells (20 μM). T4-2 cells treated with 1,4-DPCA formed polarised spheroids in three-dimensional cultures. 1,4-DPCA treatment significantly reduced invasive branching in DA-MB-157 (20 μM) and MDA-MB-231 (10 μM) cells[3].
1,4-DPCA 动物研究
Animal study
1,4-DPCA inhibited the growth of connective tissue resulting from PLGA discs implanted in the abdominal cavity of mice 28 days after implantation. It was found that 1,4-DPCA was effective in inhibiting collagen deposition on the internal and external surfaces of the discs, as well as limiting connective tissue growth, but not to the same extent as glucocorticoids[2].
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