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MW 510 Da, Purity >98%. Potent and reversible inhibitor of PAD4 (Protein Arginine Deiminase 4) (IC50 = 50 nM). Selective for PAD4 over PAD1-3. GSK484 binds at a different site from the amidines, a conformation of the PAD4 active site where part of the site is re-ordered to form a β-hairpin. It blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.

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Images

Chemical Structure - GSK484, PAD4 inhibitor (AB223598), expandable thumbnail

Publications

Key facts

CAS number

1652591-81-5

Purity

> 98%

Form

Solid

Molecular weight

510 Da

Molecular formula

C27H32ClN5O3

PubChem identifier

86340151

Nature

Synthetic

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MW 510 Da, Purity >98%. Potent and reversible inhibitor of PAD4 (Protein Arginine Deiminase 4) (IC50 = 50 nM). Selective for PAD4 over PAD1-3. GSK484 binds at a different site from the amidines, a conformation of the PAD4 active site where part of the site is re-ordered to form a β-hairpin. It blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.

Key facts

Purity

> 98%

PubChem identifier

86340151

Solubility

Soluble in DMSO to 50 mM.

Biochemical 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

Biological description

Potent and reversible inhibitor of PAD4 (Protein Arginine Deiminase 4) (IC50 = 50 nM). Selective for PAD4 over PAD1-3. GSK484 binds at a different site from the amidines, a conformation of the PAD4 active site where part of the site is re-ordered to form a β-hairpin. It blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.

Canonical SMILES

CN1C2=C(C=C(C=C2OC)C(=O)N3CCC(C(C3)N)O)N=C1C4=CC5=CC=CC=C5N4CC6CC6.Cl

Isomeric SMILES

CN1C2=C(C=C(C=C2OC)C(=O)N3CC[C@H]([C@H](C3)N)O)N=C1C4=CC5=CC=CC=C5N4CC6CC6.Cl

InChI

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

InChIKey

MULKOGJHUZTANI-ADMBKAPUSA-N

IUPAC name

[(3S,4R)-3-amino-4-hydroxypiperidin-1-yl]-[2-[1-(cyclopropylmethyl)indol-2-yl]-7-methoxy-1-methylbenzimidazol-5-yl]methanone;hydrochloride

Storage

Shipped at conditions

Blue Ice

Appropriate long-term storage conditions

-20°C

Storage information

Store under desiccating conditions

Notes

This product is manufactured by BioVision, an Abcam company and was previously called B1035 GSK-484 hydrochloride. B1035-500 is the same size as the 500 µg size of ab223598.

Protect from air and moisture.

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1 product image

  • Chemical Structure - GSK484, PAD4 inhibitor (ab223598), expandable thumbnail

    Chemical Structure - GSK484, PAD4 inhibitor (ab223598)

    2D chemical structure image of ab223598, GSK484, PAD4 inhibitor

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Product protocols

For this product, it's our understanding that no specific protocols are required. You can:

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