An inactive control for GSK484 and GSK199
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GSK106 (hydrochloride)

Item No. 17490

Technical Information
Formal Name
(3-amino-1-piperidinyl)[2-(1-ethyl-1H-indol-2-yl)-1-methyl-1H-benzimidazol-6-yl]-methanone, monohydrochloride
CAS Number
1652591-82-6
Molecular Formula
C24H27N5O • HCl
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
206, 320 nm
SMILES
NC1CN(C(C2=CC(N(C)C(C3=CC(C=CC=C4)=C4N3CC)=N5)=C5C=C2)=O)CCC1.Cl
InChi Code
InChI=1S/C24H27N5O.ClH/c1-3-29-20-9-5-4-7-16(20)13-22(29)23-26-19-11-10-17(14-21(19)27(23)2)24(30)28-12-6-8-18(25)15-28;/h4-5,7,9-11,13-14,18H,3,6,8,12,15,25H2,1-2H3;1H
InChi Key
VRPFLFUQMWOJAT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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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
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    Product Description

    Protein arginine deiminase 4 (PAD4) mediates the transformation of protein arginine into citrulline. Citrullination of proteins has normal roles in gene regulation and pathological roles in immunological and inflammatory diseases.1 GSK106 is an inactive control for the selective PAD4 inhibitors, GSK484 (Item No. 17488) and GSK199 (Item No. 17489).2 It does not inhibit PAD4 nor does it prevent the citrullination of PAD4 target proteins or the formation of neutrophil extracellular traps in mouse or human neutrophils (IC50s > 100 µM).2 See the Structural Genomics Consortium (SGC) website for more information on both GSK484 and GSK106.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jones, J.E., Causey, C.P., Knuckley, B., et alProtein arginine deiminase 4 (PAD4): Current understanding and future therapeutic potential. Curr. Opin. Drug Discov. Devel. 12(5), 616-627 (2009).

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