A PAD4 inhibitor
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GSK121 (trifluoroacetate salt)

Item No. 17491

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3-amino-1-piperidinyl)[1-methyl-2-(1-methyl-1H-indol-2-yl)-1H-benzimidazol-5-yl]-methanone, 2,2,2-trifluoroacetate
CAS Number
1652591-80-4
Molecular Formula
C23H25N5O • CF3COOH
Formula Weight
501.5
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
λmax
225, 319 nm
SMILES
NC1CN(C(C2=CC(N=C(C3=CC(C=CC=C4)=C4N3C)N5C)=C5C=C2)=O)CCC1.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C23H25N5O.C2HF3O2/c1-26-19-8-4-3-6-15(19)13-21(26)22-25-18-12-16(9-10-20(18)27(22)2)23(29)28-11-5-7-17(24)14-28;3-2(4,5)1(6)7/h3-4,6,8-10,12-13,17H,5,7,11,14,24H2,1-2H3;(H,6,7)
InChi Key
CUCLWQZRCAQPJM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $36

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    1 mg

    $63

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    5 mg

    $290

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    10 mg

    $502

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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

    GSK121 is the initial compound identified in a screen for PAD4 inhibitors and was optimized to produce the more potent PAD4 inhibitors, GSK484 (Item No. 17488) and GSK199 (Item No. 17489).1 GSK121 was shown to inhibit the citrullination of PAD4 target proteins in a functional assay with an IC50 value of 3.2 µM.1

    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).