LDN-57444 是一种可逆的，竞争性的，定向位点的泛素 C 末端水解酶 L1 (UCH-L1) 抑制剂，IC₅₀ 和 K_i 值分别为 0.88 μM 和 0.40 μM；LDN-57444 同时可抑制 UCH-L3 的活性，IC₅₀ 值为 25 μM。

LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC 50 of 0.88 μM and a K i of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC 50 of 25 μM.

Solid

IC50: 0.88 μM (UCH-L1), 25 μM (UCH-L3)
Ki: 0.40 μM (UCH-L1)

LDN-57444 is a reversible, competitive inhibitor of UCH-L1, with an IC50 of 0.88 μM, and also suppresses UCH-L3 activity, with an IC50 of 25 μM. LDN-57444 (LDN, 5 μM for 1 hr) inhibits 70% of Uch activity in hippocampal slices of the mouse brain. LDN-57444 (5 μM for 2 hr) does not reduce potentiation further in APP/PS1 slices or in wt slices exposed to 200 nM Aβ. LDN-57444 (25-100 μM) inhibits ubiquitin-proteasome activity dose-dependently in SK-N-SH cells. LDN-57444 (50 μM) also induces apoptotic cell death, causes the endoplasmic reticulum stress and results in expression of spliced XBP-1(XBP-1s, 48KD) in SK-N-SH cells. has not independently confirmed the accuracy of these methods. They are for reference only.

LDN-57444 (0.4 mg/kg, i.p.) blocks the beneficial effect of V-Uch-L1, and worsens contextual conditioning performance as the mice are exposed to the context at 1, 7, 14, and 21 days after training. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Liu Y, et al. Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line. Chem Biol. 2003 Sep;10(9):837-46.
[2]. Gong B, et al. Ubiquitin hydrolase Uch-L1 rescues beta-amyloid-induced decreases in synaptic function and contextual memory. Cell. 2006 Aug 25;126(4):775-88.

In Vitro: DMSO : 25 mg/mL (62.87 mM; Need ultrasonic)配制储备液