1. Anti-infection
    Metabolic Enzyme/Protease
    Apoptosis
  2. HIV
    HIV Protease
    SARS-CoV
    Apoptosis
    MMP
  3. Indinavir sulfate

Indinavir sulfate (Synonyms: MK-639; L735524)

Cat. No.: HY-B0689A Purity: 99.82%
Handling Instructions

Indinavir sulfate (MK-639) is an orally active and selective HIV-1 Protease inhibitor with Kis of 0.54 nM for PR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate is also a SARS-CoV 3CLpro inhibitor.

For research use only. We do not sell to patients.

Indinavir sulfate Chemical Structure

Indinavir sulfate Chemical Structure

CAS No. : 157810-81-6

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Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 66 In-stock
Estimated Time of Arrival: December 31
Solid
50 mg USD 60 In-stock
Estimated Time of Arrival: December 31
100 mg USD 96 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Indinavir sulfate:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

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Description

Indinavir sulfate (MK-639) is an orally active and selective HIV-1 Protease inhibitor with Kis of 0.54 nM for PR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate is also a SARS-CoV 3CLpro inhibitor[1][2][3][4].

IC50 & Target

MMP-2

 

HIV-1

 

In Vitro

Indinavir sulfate (0-50 µM; 18 h) blocks lymphocyte cell cycle in G0/G1 phase in PBMCs cells and impairs lymphoproliferative responses[1].
Indinavir sulfate (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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 Invasion Assay[2]

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.

Western Blot Analysis[2]

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.
In Vivo

Indinavir sulfate (70 mg/kg; i.g.; once a day for 3 weeks) inhibits the growth of hepatocarcinoma cells in vivo[2].

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.
Clinical Trial
Molecular Weight

711.87

Formula

C36H49N5O8S

CAS No.
SMILES

O=C([[email protected]@H](C[[email protected]](O)CN(CCN(CC1=CN=CC=C1)C2)[[email protected]@H]2C(NC(C)(C)C)=O)CC3=CC=CC=C3)N[[email protected]]4C(C=CC=C5)=C5C[[email protected]]4O.O=S(O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (140.48 mM)

H2O : 50 mg/mL (70.24 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4048 mL 7.0238 mL 14.0475 mL
5 mM 0.2810 mL 1.4048 mL 2.8095 mL
10 mM 0.1405 mL 0.7024 mL 1.4048 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.51 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.51 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.51 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 99.82%

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Indinavir sulfate
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