GSK484 HCl

Catalog No.S7803 Batch:S780301

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Technical Data

Formula

C27H32ClN5O3

Molecular Weight 510.03 CAS No. 1652591-81-5
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)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[2]

  • Animal Models

    MMTV-PyMT mouse model (FVB) and RIP1-Tag2 mouse model (C57BL)

  • Dosages

    4 mg/kg

  • Administration

    IP

Selleck's GSK484 HCl has been cited by 5 publications

Berbamine ameliorates DSS-induced colitis by inhibiting peptidyl-arginine deiminase 4-dependent neutrophil extracellular traps formation [ Eur J Pharmacol, 2024, S0014-2999(24)00322-4] PubMed: 38710356
Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
Re-Du-Ning injection ameliorates LPS-induced lung injury through inhibiting neutrophil extracellular traps formation [ Phytomedicine, 2021, 90:153635] PubMed: 34229173
The PAD4 inhibitor GSK484 enhances the radiosensitivity of triple-negative breast cancer [ Hum Exp Toxicol, 2020, 960327120979028] PubMed: 33355008

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.