A PAD4 inhibitor
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GSK 199 (hydrochloride)

Item No. 17489

Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[(3R)-3-amino-1-piperidinyl][2-(1-ethyl-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzimidazol-5-yl]-methanone, monohydrochloride
CAS Number
1549811-53-1
Molecular Formula
C24H28N6O2 • HCl
Formula Weight
469.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
N[C@H]1CN(C(C2=CC(N=C(C3=CC(C=CC=N4)=C4N3CC)N5C)=C5C(OC)=C2)=O)CCC1.Cl
InChi Code
InChI=1S/C24H28N6O2.ClH/c1-4-30-19(12-15-7-5-9-26-22(15)30)23-27-18-11-16(13-20(32-3)21(18)28(23)2)24(31)29-10-6-8-17(25)14-29;/h5,7,9,11-13,17H,4,6,8,10,14,25H2,1-3H3;1H/t17-;/m1./s1
InChi Key
KRGMIOKDGHBYQE-UNTBIKODSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $83

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    5 mg

    $248

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    10 mg

    $372

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    25 mg

    $825

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    NET Formation Screening & Analysis Services
    Our experts are here to help.
    • Detection of NET formation ex vivo and screening for modulators using:
      • High-content imaging
      • Enzymatic detection
      • Citrullination/carbamylation detection
    • Experienced scientists skilled in neutrophil biology, isolation, and handling
    LEARN MORE
    Product Description

    GSK 199 is an inhibitor of peptidyl arginine deiminase 4 (PAD4; IC50 = 200 nM in the absence of calcium).1 It selectively inhibits the production of citrulline by PAD4 over PAD1, PAD2, and PAD3 in kinetic assays. GSK 199 (10 µM) prevents histone H3 citrullination and neutrophil extracellular trap (NET) formation induced by ionomycin (Item No. 10004974) in isolated mouse peripheral blood neutrophils. It reduces human coronavirus OC43 (HCoV-OC43) replication in infected MRC-5 cells (IC50 = 0.6 µM).2 In vivo, GSK 199 (10 and 30 mg/kg) reduces complement C3 deposition in the synovium and cartilage but does not reduce total synovial or serum citrulline levels in a mouse model of collagen-induced arthritis.3 It reduces disease severity in the same model when administered at a dose of 30 mg/kg. GSK 199 (30 mg/kg) also reduces plasma NET levels and brain infarct volume, as well as improves neurological outcomes, in a mouse model of ischemic stroke induced by transient middle cerebral artery occlusion (tMCAO).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lewis, H.D., Liddle, J., Coote, J.E., et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat. Chem. Biol. 11(3), 189-191 (2015).

    2. Pasquero, S., Gugliesi, F., Griffante, G., et al. Novel antiviral activity of PAD inhibitors against human beta-coronaviruses HCoV-OC43 and SARS-CoV-2. Antiviral Res. 200, 105278 (2022).

    3. Willis, V.C., Banda, N.K., Cordova, K.N., et al. Protein arginine deiminase 4 inhibition is sufficient for the amelioration of collagen-induced arthritis. Clin. Exp. Immunol. 188(2), 263-274 (2017).

    4. Denorme, F., Portier, I., Rustad, J.L., et al. Neutrophil extracellular traps regulate ischemic stroke brain injury. J. Clin. Invest. 132(10), e154225 (2022).

    Product Citations

    Denorme, F., Portier, I., Rustad, J.L., et al. Neutrophil extracellular traps regulate ischemic stroke brain injury. J. Clin. Invest. 132(10), e154225 (2022).

    Koushik, S., Joshi, N., Nagaraju, S., et al. PAD4: Pathophysiology, current therapeutics and future perspective in rheumatoid arthritis. Exp. Opin. Ther. Targets 21(4), 433-447 (2017).