UCH-L1 inhibitor,reversible competitve
CAS：668467-91-2
分子式：C17H11Cl3N2O3
分子量：397.64
纯度：98%
存储：Store at -20°C

Background:

LDN 57444 is a reversible competitive inhibitor of ubiquitin C-terminal hydrolase L1 (Uch-L1) with IC50 value of 0.88μM [1].

Besides Uch-L1, LDN 57444 also inhibits Uch-L3 with a higher IC50 value of 25μM. The inhibition of Uch enzymes subsequently causes the reduction of long-term potentiation and basal synaptic transmission, which is similar to the alterations induced by Aβ [1].

In rat insulinoma cell line INS 832/13, treatment of LDN 57444 leads to the cell apoptosis. The increased activity of caspase-3 can be seen when the concentration of LDN 57444 is above 30μM. LDN 57444 also induces nuclear CHOP, suggesting that the apoptosis induced by the inhibition of Uch-L1 is related to ER stress [2].

参考文献:
[1] Gong B, Cao Z, Zheng P, Vitolo OV, Liu S, Staniszewski A, Moolman D, Zhang H, Shelanski M, Arancio O. Ubiquitin hydrolase Uch-L1 rescues beta-amyloid-induced decreases in synaptic function and contextual memory. Cell. 2006 Aug 25;126(4):775-88.
[2] Gong B, Cao Z, Zheng P, Vitolo OV, Liu S, Staniszewski A, Moolman D, Zhang H, Shelanski M, Arancio O. Ubiquitin hydrolase Uch-L1 rescues beta-amyloid-induced decreases in synaptic function and contextual memory. Cell. 2006 Aug 25;126(4):775-88.