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LDN-57444

Catalog No. T1924   CAS 668467-91-2
Synonyms: LDN57444

LDN-57444 is a reversible, competitive proteasome Uch-L1 inhibitor(IC50=0.88 μM) .

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
LDN-57444 Chemical Structure
LDN-57444, CAS 668467-91-2
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 51.00
10 mg In stock $ 92.00
25 mg In stock $ 176.00
50 mg In stock $ 313.00
100 mg In stock $ 486.00
1 mL * 10 mM (in DMSO) In stock $ 51.00
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Purity: 99.87%
Purity: 97.8%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LDN-57444 is a reversible, competitive proteasome Uch-L1 inhibitor(IC50=0.88 μM) .
Targets&IC50 UCH-L1:0.88 μM
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)
Synonyms LDN57444
Molecular Weight 397.64
Formula C17H11Cl3N2O3
CAS No. 668467-91-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 19.9 mg/mL (50 mM)

TargetMolReferences and Literature

1. Liu Y, et al. Chem Biol, 2003, 10(9), 837-846. 2. Cartier AE, et al. PLoS One, 2012, 7(4), e34713. 3. Gong B, et al. Cell, 2006, 126(4), 775-788. 4. Tan YY, et al. Mol Cell Biochem, 2008, 318(1-2), 109-115.

TargetMolCitations

1. 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 2. 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 3. 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

Related compound libraries

This product is contained In the following compound libraries:
Endoplasmic Reticulum Stress Compound Library Autophagy Compound Library Apoptosis Compound Library HIF-1 Signaling Pathway Compound Library Bioactive Compounds Library Max Ubiquitination Compound Library DNA Damage & Repair Compound Library Bioactive Compound Library Cell Cycle Compound Library NO PAINS Compound Library

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Keywords

LDN-57444 668467-91-2 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB Inhibitor inhibit Deubiquitinase LDN 57444 LDN57444 DUBs inhibitor

 

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