JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA with an IC value of 0.57 µM. JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC = 8.5 µM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA and LYPLA JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysates and intact cells.
JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC50 values of 0.50 μM and 0.57 μM, respectively.
IC50&Target
0.50 μM (AIG1) and 0.57 μM (FAHFA) in HEK293T cells
体外研究
JJH260 (30 min) inhibited the hydrolysis activity of ADTRP, FP Rh labeled hAIG1, and 9-PAHSA in HEK293T cells, with IC50 values of 8.5, 0.5, and 0.57 μM, respectively. JJH260 (5 μM, 4 h) inhibits FAHFA hydrolysis in LNCaP cells and human T cells.
分子式
C29H34ClN5O5
分子量
568.06
CAS号
1831135-30-8
运输条件
Room temperature in continental US; may vary elsewhere.