GSK484 (hydrochloride)

GSK484 hydrochloride is a selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor. GSK484 hydrochloride demonstrates high affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed.

Product Specifications

CAS Number

[1652591-81-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Protein Arginine Deiminase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/GSK484.html

Concentration

10mM

Purity

99.48

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)

Smiles

O=C(N1C[C@H](N)[C@H](O)CC1)C2=CC(OC)=C3C(N=C(C(N4CC5CC5)=CC6=C4C=CC=C6)N3C)=C2.[H]Cl

Molecular Formula

C27H32ClN5O3

Molecular Weight

510.03

Precautions

H302, H315, H319, H335

References & Citations

[1]Lewis HD, et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat Chem Biol. 2015 Mar;11 (3) :189-91.|[2]Cedervall J, et al. Pharmacological targeting of peptidylarginine deiminase 4 prevents cancer-associated kidney injury in mice. Oncoimmunology. 2017 Apr 20;6 (8) :e1320009.