LDN-57444 [T1924][CAS no. 668467-91-2]_TargetMol - 코아사이언스

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LDN-57444

Cat.# T1924 / Size: 2mg, 5mg, 10mg, 25mg, 50mg, 100mg, 1 mL * 10 mM (in DMSO)

​Biological Description

Description	LDN-57444 is a reversible, competitive proteasome Uch-L1 inhibitor(IC50=0.88 μM) .
In vitro	In vivo, LDN-57444 significantly alters the distribution of synaptic proteins and the morphology of dendritic spines. It leads to a reduction in UCH-L1 activity but does not affect the protease inhibition of cAMP levels.
In vivo	LDN-57444 (25-50 μM) reduces cell viability in a dose-dependent manner by inhibiting the activity of the ubiquitin-proteasome system and increasing the levels of highly ubiquitinated proteins, thereby inducing apoptosis.
Kinase Assay	HTS screen: To start an assay, 0.5 μL of 5 mg/mL test compound (about 50 μM final reaction concentration) or DMSO control is aliquoted into each well. Both enzyme and substrate are prepared in UCH reaction buffer (50 mM Tris-HCl [pH 7.6], 0.5 mM EDTA, 5 mM DTT, and 0.5 mg/mL ovalbumin). 25 μL of 0.6 nM UCH-L1 is then added to each well except substrate control wells, followed by plate shaking for 45–60 s on an automatic shaker. The enzyme/compound mixture is incubated at room temperature for 30 min before 25 μL of 200 nM Ub-AMC is added to initiate the enzyme reaction. The reaction mixture (300 pM UCH-L1, 100 nM Ubiquitin-AMC with 2.5 μg test compound) is incubated at room temperature for 30 additional minutes prior to quenching the reaction by the addition of 10 μL 500 mM acetic acid per well. The fluorescence emission intensity is measured on a LJL Analyst using a coumarin filter set (ex = 365 nm, em = 450 nm) and is subtracted by the intrinsic compound fluorescence to reveal the enzyme activity. A DMSO control (0.5 μL of DMSO, 25 μL of UCH-L1, 25 μL of ubiquitin-AMC, 10 μL of acetic acid), enzyme control (25 μL of UCH-L1, 25 μL of buffer, 10 μL of acetic acid), substrate control (25 μL of buffer, 25 μL of ubiquitin-AMC, 10 μL of acetic acid), and inhibitor control (0.5 μL of ubiquitin aldehyde [100 nM stock], 25 μL of UCH-L1, 25 μL of ubiquitin-AMC, 10 μL of acetic acid) are also performed in each assay plate to ensure quality and reproducibility. Potential UCH-L1 inhibitors are selected if the compounds demonstrated greater than 60% inhibition compared to the controls. The UCH-L1 enzymatic reactions are manually repeated twice using the same protocol to confirm the results for the hit compounds from the primary robot-assisted screen.
Cell Research	MTT assay(Only for Reference)
Alias	LDN57444

Chemical Properties

Molecular Weight	397.64
Formula	C17H11Cl3N2O3
Cas No.	668467-91-2

Storage & Solubility Information​

Storage	Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information	DMSO: 19.9 mg/mL (50 mM)

Citations

1.Liu S, Chai T, Garcia-Marques F, et al.UCHL1 is a potential molecular indicator and therapeutic target for neuroendocrine carcinomas.Cell Reports Medicine.2024

2.Wu W, Xu H, Liao C, et al. Blockade of USP14 potentiates type I interferon signaling and radiation-induced antitumor immunity via preventing IRF3 deubiquitination. Cellular Oncology. 2022: 1-15

3.Yue X, Liu T, Wang X, et al.Pharmacological inhibition of BAP1 recruits HERC2 to competitively dissociate BRCA1–BARD1, suppresses DNA repair and sensitizes CRC to radiotherapy.Acta Pharmaceutica Sinica B.2023

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