GSK199

SKU: orb1298574

Description

GSK199 is a potent and selective inhibitor of peptidyl arginine deiminase 4 (PAD4), exhibiting an IC50 of 200 nM under calcium-free conditions. This small molecule is a valuable research tool for studying PAD4's role in chromatin decondensation, neutrophil extracellular trap (NET) formation, and its implications in autoimmune diseases and cancer in both cellular and animal models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1549811-53-1
• MW: 468.98
• Purity: 99.44% (May vary between batches)
• Formula: C₂₄H₂₉ClN₆O₂
• SMILES: Cl.CCn1c(cc2cccnc12)-c1nc2cc(cc(OC)c2n1C)C(=O)N1CCC[C@@H](N)C1
• Target: PAD
• Solubility: DMSO:11 mg/mL (23.46 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (2.13 mM)

Bioactivity

• Target IC50:
  PAD4:200 nM
• In Vivo:
  GSK199, in the murine collagen-induced arthritis model of rheumatoid arthritis. Mice were dosed daily from the time of collagen immunization with GSK199. Efficacy was assessed against a wide range of end-points, including clinical disease scores, joint histology and immunohistochemistry, serum and joint citrulline levels and quantification of synovial autoantibodies using a proteomic array containing joint peptides. Administration of GSK199 at 30 mg/kg led to significant effects on arthritis, assessed both by global clinical disease activity and by histological analyses of synovial inflammation, pannus formation and damage to cartilage and bone. In addition, significant decreases in complement C3 deposition in both synovium and cartilage were observed robustly with GSK199 at 10 mg/kg. Neither the total levels of citrulline measurable in joint and serum, nor levels of circulating collagen antibodies, were affected significantly by treatment with GSK199 at any dose level. In contrast, a subset of serum antibodies reactive against citrullinated and non-citrullinated joint peptides were reduced with GSK199 treatment.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, GSK 199, GSK199, GSK-199, inhibit, PAD4, Peptidylarginine Deiminase, Protein Arginine Deiminase

Compound Identifiers

PubChem CID

86340155