A reversible PAD4 inhibitor
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GSK484 (hydrochloride)

Item No. 17488

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)Epigenetic Chemical Probe Guide (PDF)
Technical Information
Formal Name
[(3S,4R)-3-amino-4-hydroxy-1-piperidinyl][2-[1-(cyclopropylmethyl)-1H-indol-2-yl]-7-methoxy-1-methyl-1H-benzimidazol-5-yl]-methanone, monohydrochloride
CAS Number
1652591-81-5
Molecular Formula
C27H31N5O3 • HCl
Formula Weight
510.0
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 25 mg/mlEthanol: 25 mg/mlWater: 10 mg/ml
λmax
227, 242, 304 nm
SMILES
O[C@@H]1CCN(C(C2=CC(N=C(C3=CC(C=CC=C4)=C4N3CC5CC5)N6C)=C6C(OC)=C2)=O)C[C@@H]1N.Cl
InChi Code
InChI=1S/C27H31N5O3.ClH/c1-30-25-20(11-18(13-24(25)35-2)27(34)31-10-9-23(33)19(28)15-31)29-26(30)22-12-17-5-3-4-6-21(17)32(22)14-16-7-8-16;/h3-6,11-13,16,19,23,33H,7-10,14-15,28H2,1-2H3;1H/t19-,23+;/m0./s1
InChi Key
MULKOGJHUZTANI-ADMBKAPUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $42

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    1 mg

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    5 mg

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    10 mg

    $335

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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

    GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme.1 It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.1 It exhibits favorable pharmacokinetic profiles in mouse and rat. See the Structural Genomics Consortium (SGC) website for more information.

    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).

    Product Citations

    Surolia, R., Li, F.J., Wang, Z., et al. NETosis in the pathogenesis of acute lung injury following cutaneous chemical burns. JCI Insight 6(10), e147564 (2021).

    Li, M., Lin, C., Deng, H., et al. A novel peptidylarginine deiminase 4 (PAD4) inhibitor BMS-P5 blocks formation of neutrophil extracellular traps and delays progression of multiple myeloma. Mol. Cancer Ther. 19(7), 1530-1538 (2020).

    Zhou, Y., An, L.-L., Chaerkady, R., et al. Evidence for a direct link between PAD4-mediated citrullination and the oxidative burst in human neutrophils. Sci. Rep. 8(1), 15228 (2018).