Indinavir
Based on 8 publication(s) in Google Scholar
Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CLpro inhibitor.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.96%
- CAS. Nr.: 150378-17-9
- Formel: C36H47N5O4
- Molecular Weight:613.79
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Indinavir
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.
Biologische Aktivität
|
HIV-1 |
MMP-2 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| C8166 | EC50 |
8.2 nM
Compound: indinavir
|
Inhibition of HIV1 viral replication infected in human C8166 cells assessed as suppression of virion-associated p24 antigen production after 4 days by ELISA
Inhibition of HIV1 viral replication infected in human C8166 cells assessed as suppression of virion-associated p24 antigen production after 4 days by ELISA
|
[PMID: 19919067] |
| CCRF-CEM | EC50 |
24 nM
Compound: IDV
|
Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
|
[PMID: 17576848] |
| CCRF-CEM | EC50 |
34 nM
Compound: IDV
|
Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
|
[PMID: 17576848] |
| CCRF-CEM | EC50 |
52 nM
Compound: IDV
|
Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
|
[PMID: 17576848] |
| CCRF-CEM | EC50 |
65 nM
Compound: IDV
|
Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay
|
[PMID: 17576848] |
| HEK293 | EC50 |
7.8 nM
Compound: IDV
|
Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay
Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay
|
[PMID: 17638694] |
| HEK293 | IC50 |
>500 μM
Compound: indinavir
|
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
|
[PMID: 23241029] |
| HEK293 | IC50 |
>500 μM
Compound: indinavir
|
Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
|
[PMID: 23241029] |
| HEK293 | IC50 |
1.7 μM
Compound: indinavir
|
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis
|
[PMID: 23241029] |
| HEK293 | IC50 |
142 μM
Compound: indinavir
|
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
|
[PMID: 23241029] |
| HEK293 | IC50 |
208 μM
Compound: indinavir
|
Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
|
[PMID: 23241029] |
| HEK293 | IC50 |
7.8 μM
Compound: indinavir
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
|
[PMID: 23241029] |
| HEK293 | IC50 |
7.8 μM
Compound: indinavir
|
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay
|
[PMID: 23241029] |
| Hepatocyte | IC50 |
5 μM
Compound: Indinavir
|
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs
|
[PMID: 18212104] |
| HepG2 | CC50 |
74.7 μM
Compound: Indinavir
|
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay
|
10.1039/C1MD00147G |
| MDCK-II | IC50 |
1.9 μM
Compound: indinavir
|
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis
|
[PMID: 23241029] |
| MT2 | CC50 |
>100 μM
Compound: Indinavir
|
Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay
Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay
|
10.1039/C1MD00147G |
| MT2 | CC50 |
69.8 μM
Compound: IDV
|
Cytotoxicity against human MT2 cells by MTT assay
Cytotoxicity against human MT2 cells by MTT assay
|
[PMID: 18955518] |
| MT2 | CC50 |
69.8 μM
Compound: indinavir, IDV
|
Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT2 | EC50 |
0.005 nM
Compound: Indinavir
|
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days
|
[PMID: 20660667] |
| MT2 | EC50 |
0.024 μM
Compound: indinavir, IDV
|
Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT2 | EC50 |
0.044 μM
Compound: IDV
|
Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay
Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay
|
[PMID: 18955518] |
| MT2 | EC50 |
0.048 μM
Compound: indinavir, IDV
|
Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT2 | EC50 |
0.05 nM
Compound: Indinavir
|
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days
|
[PMID: 20660667] |
| MT2 | EC50 |
0.054 μM
Compound: indinavir, IDV
|
Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT2 | EC50 |
0.5 nM
Compound: Indinavir
|
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days
|
[PMID: 20660667] |
| MT2 | EC50 |
12.4 nM
Compound: Indinavir
|
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay
|
10.1039/C1MD00147G |
| MT2 | IC50 |
0.03 μM
Compound: IDV
|
Antiviral activity against HIV1 LAI infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
Antiviral activity against HIV1 LAI infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
|
[PMID: 21194227] |
| MT2 | IC50 |
30 nM
Compound: IDV
|
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay
|
[PMID: 23947685] |
| MT4 | CC50 |
>100 μM
Compound: IDV
|
Cytotoxicity against human MT4 cells after 6 days by MTT assay
Cytotoxicity against human MT4 cells after 6 days by MTT assay
|
[PMID: 17638694] |
| MT4 | EC50 |
>1 μM
Compound: IDV
|
Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA
Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA
|
[PMID: 18955518] |
| MT4 | EC50 |
>1 μM
Compound: IDV
|
Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA
Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA
|
[PMID: 18955518] |
| MT4 | EC50 |
>1 μM
Compound: IDV
|
Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA
Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA
|
[PMID: 18955518] |
| MT4 | EC50 |
>1 μM
Compound: indinavir, IDV
|
Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
>1 μM
Compound: indinavir, IDV
|
Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
>1 μM
Compound: indinavir, IDV
|
Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
0.014 μM
Compound: IDV
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA
|
[PMID: 18955518] |
| MT4 | EC50 |
0.034 μM
Compound: indinavir, IDV
|
Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay
Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
0.04 μM
Compound: indinavir, IDV
|
Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
0.041 μM
Compound: indinavir
|
Antiviral activity against HIV1 in MT4 cells by XTT assay
Antiviral activity against HIV1 in MT4 cells by XTT assay
|
[PMID: 18215014] |
| MT4 | EC50 |
0.044 μM
Compound: IDV
|
Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E
Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E
|
[PMID: 18955518] |
| MT4 | EC50 |
0.059 μM
Compound: indinavir, IDV
|
Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
0.067 μM
Compound: IDV
|
Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay
Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay
|
[PMID: 17638694] |
| MT4 | EC50 |
0.2 μM
Compound: indinavir, IDV
|
Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
0.22 μM
Compound: IDV
|
Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA
Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA
|
[PMID: 18955518] |
| MT4 | EC50 |
0.25 μM
Compound: indinavir, IDV
|
Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
0.27 μM
Compound: IDV
|
Antiviral activity against HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of nelfinavir by ELISA
Antiviral activity against HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of nelfinavir by ELISA
|
[PMID: 18955518] |
| MT4 | EC50 |
0.27 μM
Compound: indinavir, IDV
|
Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
0.28 μM
Compound: indinavir, IDV
|
Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
0.3 μM
Compound: IDV
|
Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA
Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA
|
[PMID: 18955518] |
| MT4 | EC50 |
0.33 μM
Compound: IDV
|
Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA
Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA
|
[PMID: 18955518] |
| MT4 | EC50 |
0.388 μM
Compound: indinavir, IDV
|
Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay
|
[PMID: 17371811] |
| MT4 | EC50 |
22 nM
Compound: IDV
|
Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
|
[PMID: 17576848] |
| MT4 | EC50 |
38 nM
Compound: IDV
|
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay
|
[PMID: 17576848] |
| MT4 | EC50 |
50 nM
Compound: IDV
|
Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay
Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay
|
[PMID: 19961222] |
| MT4 | ED50 |
0.04 μg/mL
Compound: 3
|
In vitro anti-HIV activity in MT-4 cells by using an HIV cytopathic assay
In vitro anti-HIV activity in MT-4 cells by using an HIV cytopathic assay
|
[PMID: 9748353] |
| PBMC | EC50 |
>1 μM
Compound: IDV
|
Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay
|
[PMID: 20439612] |
| PBMC | EC50 |
>1 μM
Compound: IDV
|
Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay
|
[PMID: 20439612] |
| PBMC | EC50 |
>1 μM
Compound: IDV
|
Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay
|
[PMID: 20439612] |
| PBMC | EC50 |
>1 μM
Compound: IDV
|
Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay
|
[PMID: 20439612] |
| PBMC | EC50 |
>1 μM
Compound: IDV
|
Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay
|
[PMID: 20439612] |
| PBMC | EC50 |
0.043 μM
Compound: IDV
|
Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay
|
[PMID: 20439612] |
| PBMC | EC50 |
0.34 μM
Compound: IDV
|
Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay
Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay
|
[PMID: 20439612] |
Indinavir (0-50 μM; 18 h) blocks lymphocyte cell cycle in G0/G1 phase in PBMCs cells and impairs lymphoproliferative responses[1].
Indinavir (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.
-
Cell Line:PBMCs (from healthy and HIV-infected volunteers)
-
Concentration:0-50 µM
-
Incubation Time:18 h (pretreatment; stimulation with anti-CD3 for an additional 48 hours)
-
Result:Blocked anti-CD3-induced cell-cycle progression in a dose-dependent manner.
Resulted in dose-dependent reduction of lymphoproliferative responses.
-
Cell Line:Huh7 and SK-HEP-1 cells
-
Concentration:40 µM-40 nM
-
Incubation Time:5 days
-
Result:Reduced ability to invade an in vitro constituted extracellular matrix for both cell lines treated compared with the untreated cells.
-
Cell Line:Huh7 and SK-HEP-1 cells
-
Concentration:40 µM-40 nM
-
Incubation Time:48 h
-
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.
-
Animal Model:Nude mice(s.c. into Huh7 and SK-HEP-1 cells)[2].
-
Dosage:70 mg/kg
-
Administration:Oral gavage; once a day for 3 weeks.
-
Result:Delaied the growth of s.c. implanted hepatocarcinoma xenografts in nude mice compared with placebo.
Chemical Information
-
CAS. Nr. 150378-17-9
-
Appearance Solid
-
Molecular Weight 613.79
-
Formel C36H47N5O4
-
Color White to off-white
-
SMILES
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
-
Synonyms
MK-639 free base; L-735524 free base
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (8)
-
Journal Impact Factor
-
Most Recent
-
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 -
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (162.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
-
Data Sheet (279 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6292 mL | 8.1461 mL | 16.2922 mL | 40.7305 mL |
| 5 mM | 0.3258 mL | 1.6292 mL | 3.2584 mL | 8.1461 mL | |
| 10 mM | 0.1629 mL | 0.8146 mL | 1.6292 mL | 4.0731 mL | |
| 15 mM | 0.1086 mL | 0.5431 mL | 1.0861 mL | 2.7154 mL | |
| 20 mM | 0.0815 mL | 0.4073 mL | 0.8146 mL | 2.0365 mL | |
| 25 mM | 0.0652 mL | 0.3258 mL | 0.6517 mL | 1.6292 mL | |
| 30 mM | 0.0543 mL | 0.2715 mL | 0.5431 mL | 1.3577 mL | |
| 40 mM | 0.0407 mL | 0.2037 mL | 0.4073 mL | 1.0183 mL | |
| 50 mM | 0.0326 mL | 0.1629 mL | 0.3258 mL | 0.8146 mL | |
| 60 mM | 0.0272 mL | 0.1358 mL | 0.2715 mL | 0.6788 mL | |
| 80 mM | 0.0204 mL | 0.1018 mL | 0.2037 mL | 0.5091 mL | |
| 100 mM | 0.0163 mL | 0.0815 mL | 0.1629 mL | 0.4073 mL |