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Enzyme Inhibitors

GSK484 View larger

GSK484

AOB6992

CAS No: 1652591-81-5

Chemical Name: ((3S,4R)-3-Amino-4-hydroxypiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-indol-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride

AOBIOUS launched this product in 2015

CITATIONS - Publications That Use AOBIOUS Product

1) Front Immunol. 2019; 10: 2088

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$29.00

$29.00 per mg

Quantity Discount Table - Order More To Get More Price Discount

QuantitymgUnit Price ($/mg or $/Unit)Final Price
15 $24.65 Total: $123.25
110 $20.88 Total: $208.80
125 $17.69 Total: $442.25
150 $15.08 Total: $754.00
1100 $13.05 Total: $1,305.00

Data sheet

Molecular FormulaC27H32ClN5O3
Molecular Weight510.03
CAS Numbers1652591-81-5
Storage Condition0°C (short term), -20°C (long term), desiccated
SolubilityDMSO
Stock Solution Guide10 mMol/5.10 mg/1 mL; 5 mMol/2.55mg/1 mL in DMSO
Purity98% by HPLC
SynonymGSK484; GSK-484; GSK 484.
IUPAC/Chemical 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
InChl KeyMULKOGJHUZTANI-ADMBKAPUSA-N
InChl CodeInChI=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
SMILES CodeO[C@@H]1CCN(C(C2=CC(N=C(C3=CC(C=CC=C4)=C4N3CC5CC5)N6C)=C6C(OC)=C2)=O)C[C@@H]1N.Cl
References1) Jones, J.E., Causey, C.P., Knuckley, B., et al. Protein 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 al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat. Chem. Biol. 11(3), 189-191 (2015).

More info

GSK484 is a potent, well-characterized PAD4 inhibitor used extensively in research to dissect PAD4’s role in inflammation, immunity, cancer biology, and epigenetic regulation. Its reversible and selective nature, along with strong structural validation, make it an excellent tool—especially for cellular systems.


  • It selectively targets PAD4 over PAD1–3, disrupting citrullination—the conversion of arginine to citrulline—particularly important in neutrophil function and inflammation WikipediaAbcamStructural Genomics Consortium.

  • It binds to the low-calcium form of PAD4 with nanomolar potency (IC₅₀ ≈ 50 nM, increasing to ~250 nM in the presence of calcium) Structural Genomics Consortium

  • Structural studies revealed that GSK484 acts by inducing a conformational change—forming a β-hairpin in the PAD4 active site—distinct from older irreversible amidine inhibitors Structural Genomics Consortium.



Biological & Functional Effects

  • Inhibition of NETosis (Neutrophil Extracellular Trap formation): GSK484 blocks citrullination in neutrophils and prevents NET formation in both mouse and human cells, a process linked to thrombosis, autoimmune conditions, and cancer-related inflammation Structural Genomics ConsortiumAb

  • Anti-inflammatory and Radiosensitizing Effects:

    • In colorectal cancer models, GSK484 enhances radiosensitivity, promoting DNA double-strand breaks and cell death, while inhibiting NET formation PubMedWiley Online Library.

    • It has demonstrated anti-inflammatory benefits in other in vivo models, such as alleviating inflammation in giant cell myocarditis by suppressing NETosis ScienceDirect.

A Chemical Probe with Strong Selectivity

  • The Structural Genomics Consortium (SGC) and GlaxoSmithKline developed GSK484 as part of an epigenetic probe collection—making it a high-quality tool for studying PAD4’s biological role Structural Genomics ConsortiumIUPHAR/BPS Guide to Pharmacology.

  • The Chemical Probes Portal rates GSK484 as a mixed-mode PAD4 inhibitor with strong selectivity, recommending cellular use up to ~10 µM, but cautioning about calcium-dependent variability and calling attention to use of an inactive control (GSK106) in studies Chemical Probes Portal.

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