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LDN-57444

CAS No. : 668467-91-2

MCE 站：LDN-57444

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：Deubiquitinase  |  Apoptosis

In Vitro: 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.

In Vivo: 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.

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