$ 294.30
Details:
The e-isomer of a cell-permeable pyridine hydrazone compound that acts as a selective inhibitor against jumonji family histone demethylases (ic50 = 230, 290-320, 340, 435, 445, 855, and 1,100 nm, respectively, against jarid1a/kdm5a, jmjd2d/kdm4d, jmjd2e/kdm4e, jmjd2b/kdm4b, jmjd2a/kmd4a, jmjd3/kdm6b, and jmjd2c/kdm4c, respectively), presumably via catalytic site iron interaction, displaying little toward 5mc dna hydroxylase tet1, aurora kinases, hdacs, hif prolyl hydroxylase phd2, histone methyltransferases, protein arginine methyltransferases, sirtuins, or the non-jumonji family histone demethylase lsd1/kdm1a. Shown to exhibit anticancer activity against h358 and a549 lunger cancer cells both in cultures in vitro (ic50 in 4 d = 100 and 250 nm, respectively) and in mice in vivo (via i.P. At 100mg/kg and p.O. At 55mg/kg, respectively; 2-3 times per week).
