LDN-57444 is a reversible, competitive and site-directed inhibitor ofubiquitin C-terminal hydrolase L1 (UCH-L1), with anIC₅₀of 0.88 μM and aK_iof 0.40 μM; LDN-57444 also suppressesUCH-L3activity, with anIC₅₀of 25 μM.

IC50: 0.88 μM (UCH-L1), 25 μM (UCH-L3)^[1]
Ki: 0.40 μM (UCH-L1)^[1]

LDN-57444 is a reversible, competitive inhibitor of UCH-L1, with an IC₅₀of 0.88 μM, and also suppresses UCH-L3 activity, with an IC₅₀of 25 μM^[1]. 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^[2]. 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^[3].

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^[2].

397.64

Solid

C₁₇H₁₁Cl₃N₂O₃

668467-91-2

Room temperature in continental US; may vary elsewhere.

DMSO : 25 mg/mL(62.87 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.29 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。