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GRL0617 DUB inhibitor

Name: GRL0617
Brand: Selleck Chemicals
SKU: S6845
Rating: 5 (1 reviews)

Cat.No.S6845

GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLPro)/deubiquitinase with IC50 of 0.6 μM and Ki of 0.49 μM. This compound inhibits SARS-CoV viral replication in Vero E6 cells with EC50 of 15 microM and has no associated cytotoxicity.

Chemical Structure

Molecular Weight: 304.39

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Quality Control

Batch: S684501 DMSO]65 mg/mL]false]Ethanol]22 mg/mL]false]Water]Insoluble]false Purity: 99.86%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.86

Related Targets	Proteasome E1 Activating E3 Ligase p97 SUMO E2 conjugating
Other DUB Inhibitors	PR-619 P5091 IU1 P22077 b-AP15 ML323 LDN-57444 VLX1570 TCID EOAI3402143

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
Vero E6	Antiviral assay		48 hrs	Antiviral activity against SARS coronavirus in african green monkey Vero E6 cells assessed as inhibition of replication after 48 hrs, EC50=13.1μM	19645480
Vero E6	Antiviral assay	0.1 to 50 uM	48 hrs	Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells at 0.1 to 50 uM after 48 hrs, EC50=14.5μM	23231439
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	304.39	Formula	C₂₀H₂₀N₂O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1093070-16-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C=C(C=C1)N)C(=O)NCCC2=CC=CC3=CC=CC=C32

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (213.54 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 22 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.250mg/ml (10.68mM)	Taking the 1 mL working solution as an example, add 50 μL of 65 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.405mg/ml (1.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.1 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	PLPro/deubiquitinase (Cell-free assay) 0.49 μM(Ki) PLPro/deubiquitinase (Cell-free assay) 0.6 μM
References	[1] https://pubmed.ncbi.nlm.nih.gov/18852458/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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