Indinavir sulfate ethanolate
Based on 8 publication(s) in Google Scholar
Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate ethanolate is also a SARS-CoV 3CLpro inhibitor.
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- No. CAS: 2563866-80-6
- Fòrmula: C38H55N5O9S
- Peso molecular:757.94
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Indinavir sulfate ethanolate
More- Signal Transduct Target Ther. 2021 May 29;6(1):212. [Abstract]
- Nat Commun. 2020 Sep 4;11(1):4417. [Abstract]
- Front Pharmacol. 2021 Apr 12;12:634097. [Abstract]
- Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
- Antiviral Res. 2022 Dec:208:105463. [Abstract]
- Antimicrob Agents Chemother. 2020 Aug 20;64(9):e00872-20. [Abstract]
- Toxicol In Vitro. 2023 Dec:93:105689. [Abstract]
- bioRxiv. 2020 Apr.
Actividad biológica
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HIV-1 |
MMP-2 |
Indinavir sulfate ethanolate (0-50 µM; 18 h) blocks lymphocyte cell cycle in G0/G1 phase in PBMCs cells and impairs lymphoproliferative responses[1].
Indinavir sulfate ethanolate (40 µM-40 nM; 5 days) inhibits cell invasion and (40 µM-40 nM; 48 h) MMPs-2 activation of the Huh7 and SK-HEP-1 hepatocarcinoma cells in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PBMCs (from healthy and HIV-infected volunteers)
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Concentration:0-50 µM
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Incubation Time:18 h (pretreatment; stimulation with anti-CD3 for an additional 48 hours)
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Result:Blocked anti-CD3-induced cell-cycle progression in a dose-dependent manner.
Resulted in dose-dependent reduction of lymphoproliferative responses.
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Cell Line:Huh7 and SK-HEP-1 cells
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Concentration:40 µM-40 nM
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Incubation Time:5 days
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Result:Reduced ability to invade an in vitro constituted extracellular matrix for both cell lines treated compared with the untreated cells.
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Cell Line:Huh7 and SK-HEP-1 cells
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Concentration:40 µM-40 nM
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Incubation Time:48 h
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Result:Blocked the conversion of latent MMP-2 to its 62/64-kDa active form.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice(s.c. into Huh7 and SK-HEP-1 cells)[2].
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Dosage:70 mg/kg
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Administration:Oral gavage; once a day for 3 weeks
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Result:Delaied the growth of s.c. implanted hepatocarcinoma xenografts in nude mice compared with placebo.
Chemical Information
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No. CAS 2563866-80-6
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Peso molecular 757.94
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Fòrmula C38H55N5O9S
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SMILES
CCO.O=C([C@@H](C[C@H](O)CN(CCN(CC1=CN=CC=C1)C2)[C@@H]2C(NC(C)(C)C)=O)CC3=CC=CC=C3)N[C@H]4C(C=CC=C5)=C5C[C@H]4O.O=S(O)(O)=O
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Synonyms
MK-639 ethanolate; L735524 ethanolate
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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.
Publications (8)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. [Abstract]2021 May 29;6(1):212. PMID: 34052830 -
Nat Commun
Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. [Abstract]2020 Sep 4;11(1):4417. PMID: 32887884 -
Front Pharmacol
Prediction of Synergistic Drug Combinations for Prostate Cancer by Transcriptomic and Network Characteristics. [Abstract]2021 Apr 12;12:634097. PMID: 33986671 -
Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
Antiviral Res
HIV protease inhibitor attenuated astrocyte autophagy involvement in inflammation via p38 MAPK pathway. [Abstract]2022 Dec:208:105463. PMID: 36372295 -
Antimicrob Agents Chemother
2020 Aug 20;64(9):e00872-20. PMID: 32669265 -
Toxicol In Vitro
Evaluating variations in bilirubin glucuronidation activity by protease inhibitors in canine and human primary hepatocytes cultured in a 3D culture system. [Abstract]2023 Dec:93:105689. PMID: 37660998 -
Pureza y Documentación
Referencias
[1]. Chavan S, et al. The HIV protease inhibitor Indinavir inhibits cell-cycle progression in vitro in lymphocytes of HIV-infected and uninfected individuals. Blood. 2001 Jul 15;98(2):383-9. [Content Brief]
[2]. Esposito V, et al. Evaluation of antitumoral properties of the protease inhibitor indinavir in a murine model of hepatocarcinoma. Clin Cancer Res. 2006 Apr 15;12(8):2634-9. [Content Brief]
[3]. Liu F, et al. Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S. J Mol Biol. 2005 Dec 9;354(4):789-800. [Content Brief]
[4]. Hall DC Jr, et al. A search for medications to treat COVID-19 via in silico molecular docking models of the SARS-CoV-2 spike glycoprotein and 3CL protease. Travel Med Infect Dis. 2020 May-Jun;35:101646. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Indinavir sulfate ethanolate Related Classifications
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