Cathepsin-IN-5
Cathepsin-IN-5 is a cathepsin inhibitor with IC50 values of 6.2 μM and 81 nM for cathepsin L and cathepsin S. Cathepsin-IN-5 inhibits cancer cells proliferation, induces apoptosis, reduces growth of hepatocellular tumors in mouse models, and modulates expression of genes linked to cell death, cell proliferation, and cellular processes. Cathepsin-IN-5 can be used for the research of hepatocellular carcinoma.
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- No. CAS: 2475078-38-5
- Fòrmula: C22H20N2O6S
- Peso molecular:440.47
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Almacenamiento:
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Actividad biológica
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cathepsin S 81 nM (IC50) |
cathepsin L 6.2 μM (IC50) |
PARP1 |
Caspase 3 |
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Cell Line
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Type | Value | Description | References |
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| HepG2 | CC50 |
5.17 μM
Compound: 1
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Cytotoxicity against human HepG2 cells assessed as cell growth measured after 72 hrs mby MTT assay
Cytotoxicity against human HepG2 cells assessed as cell growth measured after 72 hrs mby MTT assay
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[PMID: 37984297] |
Cathepsin-IN-5 (Compound 1) (0.15-300 μM; 24-72 h) exhibits time-dependent antiproliferative activity against Hep G2 and Hep 3B hepatocellular carcinoma cell lines, with IC50 values ranging from 1.8 to 6.4 μM[1].
Cathepsin-IN-5 (7.5-10 μM; 72-96 h) inhibits Hep G2 cell motility and proliferation in a wound healing assay[1].
Cathepsin-IN-5 (0.1-50 μM; 2-24 h) inhibits endogenous cathepsin L (IC50 = 6.2 μM) and cathepsin S (IC50 = 81 nM) activity in Hep G2 cell lysates in a concentration- and time-dependent manner[1].
Cathepsin-IN-5 (0.1-50 μM; 2.5-24 h) does not induce significant intracellular ROS production in Hep G2 or Hep 3B cells[1].
Cathepsin-IN-5 (5-20 μM; 1-24 h) induces concentration- and time-dependent changes in gene expression in Hep G2 cells, enriching pathways related to macroautophagy, apoptosis, and cell migration[1].
Cathepsin-IN-5 (5-20 μM; 6-24 h) significantly upregulates expression of sqstm1, gabarapl1, akr1c1, and akap12 in Hep G2 cells[1].
Cathepsin-IN-5 (5-20 μM; 6-24 h) activates apoptosis in Hep G2 cells in a concentration- and time-dependent manner, increasing cleaved PARP1 and cleaved caspase-3 levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hep G2
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Concentration:5, 20 μM
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Incubation Time:6 h; 24 h
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Result:Significantly upregulated sqstm1, gabarapl1, and akr1c1 expression at 5 μM and 20 μM after 6 h.
Significantly upregulated sqstm1, gabarapl1, akr1c1, and akap12 expression at 20 μM after 24 h.
Modestly decreased angptl8 expression at 20 μM after 24 h.
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Cell Line:Hep G2
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Concentration:5, 20 μM
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Incubation Time:6 h; 24 h
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Result:Increased cleaved PARP1 levels at 20 μM after 6 h and 24 h.
Increased cleaved caspase-3 levels at 5 μM and 20 μM after 6 h and 24 h.
Showed concentration- and time-dependent increases in cleaved PARP1 and cleaved caspase-3 levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Foxn1nu (immunocompromised, subcutaneous Hep 3B2.1−7 xenograft model)[1]
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Dosage:100 mg/kg; 150 mg/kg
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Administration:s.c.; daily; 15 days (administered proximal to the tumor)
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Result:Resulted in a tumor volume fold increase of ~1 (100 mg/kg) and ~2 (150 mg/kg), compared to ~7 in vehicle-treated mice.
Did not significantly elevate plasma AST and ALT levels relative to vehicle-treated mice.
Showed no significant difference in BUN and creatinine levels from vehicle controls.
Showed no signs of systemic toxicity (e.g., lethargy, weight loss).
Chemical Information
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No. CAS 2475078-38-5
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Peso molecular 440.47
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Fòrmula C22H20N2O6S
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SMILES
O=C(C1=CC=C([N+]([O-])=O)O1)N[C@@H](CCC2=CC=CC=C2)/C=C/S(=O)(C3=CC=CC=C3)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cathepsin-IN-5 Related Classifications
HY-182269 Related Classifications
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