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LDN-57444

目录号: PL04818 纯度: ≥99%

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 Ki 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。

CAS No. :668467-91-2

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中文名称	LDN-57444
中文别名	LDN-57444 抑制剂
英文名称	LDN-57444
英文别名	1H-Indole-2,3-dione, 5-chloro-1-[(2,5-dichlorophenyl)methyl]-,3-(O-acetyloxime);LDN 57444;LDN-57444;1H-Indole-2,3-dione, 5-chloro-1-[(2,5-dichlorophenyl)methyl]-, 3-(O-acetyloxime);LDN-57444 ( LDN 57444, Compound 30);3-(O-acetyloxime), 5-chloro-1-[(2,5-dichlorophenyl)methyl]-1H-Indole-2,3-dione;C30;UCH-L1 Inhibitor;HMS3653K09;IN1021;AK547911;[(Z)-[5-chloro-1-[(2,5-dichlorophenyl)methyl]-2-oxoindol-3-ylidene]amino] acetate
Cas No.	668467-91-2
分子式	C₁₇H₁₁Cl₃N₂O₃
分子量	397.64
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	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 Ki 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。

产品详情	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。
生物活性	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.
性状	Solid
IC50 & Target[1][2]	IC50: 0.88 μM (UCH-L1), 25 μM (UCH-L3) Ki: 0.40 μM (UCH-L1)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

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

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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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

LDN-57444

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