Cat. No.: HY-117043

GRL0617

14 Cited Publications

Customer Review

Based on 14 publication(s) in Google Scholar

GRL0617 is a selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro), with an IC₅₀ of 0.6 μM and a Ki value of 0.49 μM. GRL0617 also inhibits SARS-CoV with an EC₅₀ of 14.5 μM. GRL0617 can be used for the research of severe acute respiratory syndrome.

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

Purity: 99.49%
CAS No.: 1093070-16-6
Formula: C₂₀H₂₀N₂O
Molecular Weight:304.39

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GRL0617 Chemical Structure

CAS No.: 1093070-16-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (14)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 0.6 μM (SARS-CoV PLpro)^[1]

All Deubiquitinase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Vero	CC₅₀	500 μM Compound: 4; GRL0617	Cytotoxicity against African green monkey Vero cells treated for 24 hrs by CCK8 assay Cytotoxicity against African green monkey Vero cells treated for 24 hrs by CCK8 assay	[PMID: 35620927]
Vero	EC₅₀	13.1 μM Compound: 25	Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs	[PMID: 19645480]
Vero	EC₅₀	14.5 μM Compound: GRL0617	Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells at 0.1 to 50 uM after 48 hrs Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells at 0.1 to 50 uM after 48 hrs	[PMID: 23231439]
Vero C1008	CC₅₀	253.2 μM Compound: GRL0617	Cytotoxicity against african green monkey Vero E6 cells incubated for 48 hrs Cytotoxicity against african green monkey Vero E6 cells incubated for 48 hrs	[PMID: 38871484]
Vero C1008	EC₅₀	10 μM Compound: 5	Antiviral activity against SARS coronavirus Urbani infected in monkey Vero E6 cells assessed as reduction in virus-induced cytopathogenicity incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay Antiviral activity against SARS coronavirus Urbani infected in monkey Vero E6 cells assessed as reduction in virus-induced cytopathogenicity incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 32665808]

In Vitro

GRL0617 (0-50 μM; 48 h) exibits significantly antiviral activity in SARS-CoV infected Vero E6 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

Vero E6 cells
Concentration:

0, 10, 20, 30, 40 and 50 μM
Incubation Time:

48 hours
Result:

Showed significant antiviral activity in SARS-CoV infected Vero E6 cells with an EC₅₀ value of 14.5 μM.

Chemical Information

CAS No. 1093070-16-6
Appearance Solid
Molecular Weight 304.39
Formula C₂₀H₂₀N₂O
Color Light yellow to yellow
SMILES

O=C(N[C@@H](C1=C2C=CC=CC2=CC=C1)C)C3=CC(N)=CC=C3C
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All WBRT-PCRCell Proliferation/Viability Assay

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Journal Impact Factor

Nat Commun

The complex structure of GRL0617 and SARS-CoV-2 PLpro reveals a hot spot for antiviral drug discovery. [Abstract]

2021 Jan 20;12(1):488. PMID: 33473130

GRL0617 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 20;12(1):488. [Abstract]

Cells were treated for an additional 24 h with indicated concentrations of GRL0617 (0, 20, 40, 60 μM). Cell lysates were subjected to immunoblotting with anti-ubiquitin, anti-ISG15, and anti-GFP antibodies. GAPDH served as a loading control.

GRL0617 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 20;12(1):488. [Abstract]

The quantification of absolute viral RNA copies (per mL) in the supernatant at 48 h post-infection was determined by qRT-PCR analysis treated with GRL0617.

GRL0617 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 20;12(1):488. [Abstract]

The cytotoxicity of GRL0617 on Vero E6 cells was measured using CCK8.
Nucleic Acids Res

COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]

2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390
Acta Pharm Sin B

Crystal structure of SARS-CoV-2 papain-like protease. [Abstract]

2021 Jan;11(1):237-245. PMID: 32895623
J Immunother Cancer

CD47 destabilization via manipulating the SPOP-USP2 axis augments macrophage phagocytosis and cancer immunotherapy. [Abstract]

2026 Jan 14;14(1):e013498. PMID: 41534899
Cell Chem Biol

Identifying enhancers of innate immune signaling as broad-spectrum antivirals active against emerging viruses. [Abstract]

2022 Jul 21;29(7):1113-1125.e6. PMID: 35728599
Cell Chem Biol

Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2. [Abstract]

2021 Jun 17;28(6):855-865.e9. PMID: 33979649
Cell Rep

ISGylation by HERCs facilitates STING activation. [Abstract]

2024 Apr 21;43(5):114135. PMID: 38652662
J Med Chem

Discovery of Novel Nonpeptidic and Noncovalent Small Molecule 3CLpro Inhibitors as anti-SARS-CoV-2 Drug Candidate. [Abstract]

2024 Aug 8;67(15):12760-12783. PMID: 39072488
Sci Signal

The SARS-CoV-2 papain-like protease suppresses type I interferon responses by deubiquitinating STING. [Abstract]

2023 May 2;16(783):eadd0082. PMID: 37130168
ACS Omega

SARS-CoV‑2 Papain-Like Protease Inhibitors Based on Naphthalen-1-ylethanamine and Halogenated Benzene Moieties. [Abstract]

2025 Oct 2;10(40):47165-47175. PMID: 41114162
Sci Rep

9-aminominocycline potentiates the efficacy of EIDD-1931 and PF-332 by targeting the papain like protease enzyme of SARS-CoV-2. [Abstract]

2025 Feb 15;15(1):5671. PMID: 39955340
ACS Infect Dis

Exploring Noncovalent Protease Inhibitors for the Treatment of Severe Acute Respiratory Syndrome and Severe Acute Respiratory Syndrome-Like Coronaviruses. [Abstract]

2022 Mar 11;8(3):596-611. PMID: 35199517
Anim Cells Syst

Blocking SLC7A11 attenuates the proliferation of esophageal squamous cell carcinoma cells. [Abstract]

2024 May 11;28(1):237-250. PMID: 38741950
ChemMedChem

2026 May 8;21(9):e202600007.

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (410.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2853 mL

16.4263 mL

32.8526 mL

5 mM

0.6571 mL

3.2853 mL

6.5705 mL

10 mM

0.3285 mL

1.6426 mL

3.2853 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.5 mg/mL (8.21 mM); Suspended solution; Need ultrasonic

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (6.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (6.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ratia K, et al. A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication. Proc Natl Acad Sci U S A. 2008 Oct 21;105(42):16119-24. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2853 mL	16.4263 mL	32.8526 mL	82.1315 mL
	5 mM	0.6571 mL	3.2853 mL	6.5705 mL	16.4263 mL
	10 mM	0.3285 mL	1.6426 mL	3.2853 mL	8.2131 mL
	15 mM	0.2190 mL	1.0951 mL	2.1902 mL	5.4754 mL
	20 mM	0.1643 mL	0.8213 mL	1.6426 mL	4.1066 mL
	25 mM	0.1314 mL	0.6571 mL	1.3141 mL	3.2853 mL
	30 mM	0.1095 mL	0.5475 mL	1.0951 mL	2.7377 mL
	40 mM	0.0821 mL	0.4107 mL	0.8213 mL	2.0533 mL
	50 mM	0.0657 mL	0.3285 mL	0.6571 mL	1.6426 mL
	60 mM	0.0548 mL	0.2738 mL	0.5475 mL	1.3689 mL
	80 mM	0.0411 mL	0.2053 mL	0.4107 mL	1.0266 mL
	100 mM	0.0329 mL	0.1643 mL	0.3285 mL	0.8213 mL

Keywords

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GRL0617

Ubiquitination Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) GRL0617

All Deubiquitinase Isoforms

Biological Activity

Chemical Information

Publications (14)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GRL0617

Ubiquitination Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Anti-Infection Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) GRL0617

All Deubiquitinase Isoforms

Biological Activity

Chemical Information

Publications (14)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GRL0617 Related Classifications

HY-117043 Related Classifications