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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
668467-91-2
- 规格:
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥627.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥554.0 |
| 规格: | 10 mg | 产品价格: | ¥950.0 |
| 规格: | 25 mg | 产品价格: | ¥1900.0 |
| 规格: | 50 mg | 产品价格: | ¥3040.0 |
| 规格: | 100 mg | 产品价格: | ¥4788.0 |
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LDN-57444
CAS No. : 668467-91-2
MCE 国际站: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 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。
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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