GSK484 HCl

Catalog No.S7803 Synonyms: GSK484 hydrochloride

For research use only.

GSK484 HCl, a benzoimidazole derivative, is a selective and reversible inhibitor of peptidylarginine deiminase 4 (PAD4) with IC50 of 50 nM in the absence of Calcium.

GSK484 HCl Chemical Structure

CAS No. 1652591-81-5

Selleck's GSK484 HCl has been cited by 2 Publications

Purity & Quality Control

Choose Selective PAD Inhibitors

Biological Activity

Description GSK484 HCl, a benzoimidazole derivative, is a selective and reversible inhibitor of peptidylarginine deiminase 4 (PAD4) with IC50 of 50 nM in the absence of Calcium.
Targets
PAD4 [1]
(in the absence of Calcium)
50 nM
In vitro

GSK484 also inhibits PAD4 citrullination (at 0.2 mM calcium) of benzoyl-arginine ethyl ester (BAEE) substrate in a concentration-dependent manner, as detected using an NH3 release assay. GSK484 causes a clear, statistically-significant reduction in diffused NETs.[1]

In vivo

GSK484 prevents tumor-induced NETosis in vivo and can antagonize kidney injury in mice with mammary carcinoma or pancreatic neuroendocrine tumors.[2]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: NB4 cells, HEK293 cells
  • Concentrations: 10 μM, 100 μM
  • Incubation Time: 20 min
  • Method:

    HEK293 cells stably expressing N-terminal FLAG-tagged PAD1, PAD2, PAD3 or PAD4 are engineered by retroviral transduction. Cells are grown in 15 cm diameter plates to subconfluency in DMEM supplemented with 10% Foetal Bovine Serum, harvested by centrifugation and washed once in PBS/2 mM EGTA. Cells are lysed in 50 mM Tris-Cl, pH 7.4, 1.5 mM MgCl2, 5% glycerol, 150 mM NaCl, 25 mM NaF, 1 mM Na3VO4, 0.4% NP40, 1 mM DTT with protease inhibitors. Lysates are pre-incubated for 20 min at 4℃ with DMSO alone (2%) or 100 μM of GSK484. Citrullination reactions are performed for 30 min at 37℃ in the presence of 2 mM calcium.

Animal Research:

[2]

  • Animal Models: MMTV-PyMT mouse model (FVB) and RIP1-Tag2 mouse model (C57BL)
  • Dosages: 4 mg/kg
  • Administration: IP

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(196.06 mM)
Ethanol 100 mg/mL
(196.06 mM)
Water 8 mg/mL
(15.68 mM)

Chemical Information

Molecular Weight 510.03
Formula

C27H32ClN5O3

CAS No. 1652591-81-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C2=C(C=C(C=C2OC)C(=O)N3CCC(C(C3)N)O)N=C1C4=CC5=CC=CC=C5N4CC6CC6.Cl

In vivo Formulation Calculator (Clear solution)

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

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% 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.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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