CA-074 methyl ester

SKU: orb1304217

Description

CA-074 methyl ester

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 147859-80-1
• MW: 397.47
• Purity: 97.26% (May vary between batches)
• Formula: C₁₉H₃₁N₃O₆
• SMILES: C(N[C@H](C(=O)N1[C@H](C(OC)=O)CCC1)[C@H](CC)C)(=O)[C@@H]2[C@@H](C(NCCC)=O)O2
• Target: Cysteine Protease
• Solubility: Ethanol:73 mg/mL (183.66 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (12.58 mM);DMSO:257.5 mg/mL (647.85 mM)

Bioactivity

• Target IC50:
  Cathepsin B (pH 7.2):7.6 μM|Cathepsin B (pH 4.6):8.9 μM|Cathepsin B (pH 5.5):13.7 μM
• In Vivo:
  METHODS: To study the neuroprotective effect of CA-074 methyl ester, CA-074 methyl ester (1 μg, 10 μg) was administered to the hippocampus induced by global cerebral I/R injury. RESULTS: CA-074 methyl ester prevented necroptosis in hippocampal CA1 neurons induced by global cerebral I/R injury. CA-074 methyl ester pretreatment strongly inhibited lysosomal membrane disruption and cathepsin-B leakage. CA-074 methyl ester inhibited the overexpression and nuclear translocation of RIP3 and the reduction of NAD+ levels after I/R injury. Pretreatment with CA-074 methyl ester enhanced the upregulation of Hsp70. METHODS: To study the effect of CA-074 methyl ester on osteoclastogenesis, CA-074 methyl ester (10, 30 mg/kg) was injected into the skull of mice. RESULTS: CA-074 methyl ester inhibited osteoclastogenesis in vivo. METHODS: To study the anti-inflammatory activity of CA-074 methyl ester, CVB+CA-074 methyl ester (4 mg/kg) was injected intramuscuarly into guinea pigs. RESULTS: Inflammation scores were significantly lower in the CVB+None group than in the CVB+ NONE group. The number of CD8+T cells was reduced in the CVB+CA-074 methyl ester group compared with the sham-operated group.
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• In Vitro:
  METHODS: C57BL/6J BMM cells were treated with CA-074 methyl ester (50 μM) for 24, 48 and 72 hours, and the target protein expression was detected by Western Blot. RESULTS: CA-074 methyl ester inhibited RANKL-stimulated c-FOS upregulation and subsequent NFATc1 self-amplification.
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• Cell Research:
  HL-60 cells are pre-treated for 24 h with 200 μM BSO followed by 60 min with 1 mM DEM. Thereafter, the cells(1×106/ml) are incubated with 100 μM CA-074 or CA-074Me, in the presence of 1% DMSO, 200 μM BSO and 1 mM DEM at 37°C. Control cultures are treated with 1% DMSO alone or with 100 μM Z-FA-DMK in the presence of 200 μM BSO and 1 mM DEM. Untreated HL-60 cells are incubated with 100 μM CA-074 or CA-074Me, in the presence of 1% DMSO at 37°C. Untreated control cultures are incubated with 1% DMSO alone or with 100 μM Z-FA-DMK. After 2 h incubation, cells are washed three times with PBS/1% glucose and lysed in 100 mM citrate, pH 5.0, 2% Chaps (106 cells/100 μl). Subsequently, the lysate is centrifuged and the clarified supernatant used to assay for proteolytic activity.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cathepsin B Inhibitor IV, Cathepsin B, Cathepsin, CysteineProtease, Cysteine Protease, CA074 methyl ester, CA-074 methyl ester, CA-074Me, CA 074 methyl ester, Inhibitor, inhibit

Compound Identifiers

PubChem CID

23760717