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Merck

SML1658

GSK484

≥98% (HPLC), PAD4 inhibitor, powder

Synonyme(s) :

((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, AOB6992, GSK 484, GSK-484 hydrochloride, GTPL8577

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A propos de cet article

Formule empirique (notation de Hill) :
C27H31N5O3 · HCl
Numéro CAS:
1652591-81-5
Poids moléculaire :
510.03
UNSPSC Code:
51111800
PubChem Substance ID:
329825997
NACRES:
NA.77

Principaux documents

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Nom du produit

GSK484, ≥98% (HPLC)

form

powder

SMILES string

[H]Cl.CN1C(C2=CC(C=CC=C3)=C3N2CC4CC4)=NC5=C1C(OC)=CC(C(N6C[C@H](N)[C@H](O)CC6)=O)=C5

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

assay

≥98% (HPLC)

color

white to beige

solubility

H2O: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

Quality Level

100

Catégories apparentées

Biochem/physiol Actions

GSK484 is a potent selective reversible inhibitor of protein arginine deiminase PAD4, an enzyme believed to play a role in granulocyte and macrophage development leading to inflammation and immune response, and overexpressed in many tumors. GSK484 has IC50 values of 50 nM without calcium and 250 nM in the presence of 2 mM calcium. GSK484 showed minimal off-target activity tested against 50 other proteins with no activation across HDACs 1–11 even at 100 μM. GSK484 binds at a different site from the amidines, a conformation of the PAD4 active site where part of the site is reordered to form a β-hairpin. For full characterization details, please visit the GSK484 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
GSK484 is a potent selective reversible inhibitor of protein arginine deiminase PAD4.

Features and Benefits

GSK484 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Other Notes

GSK484 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK484 probe summary on the Chemical Probes Portal website.

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000187299
0000187298
0000152497
0000152497
0000187299

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Consulter la Bibliothèque de documents

Jie Zeng et al.
Journal of cellular and molecular medicine, 24(13), 7590-7599 (2020-05-20)
Kaempferol (kaem) is a dietary flavonoid found in a variety of fruits and vegetables. The inhibitory effects of kaem on primary tumour growth have been extensively investigated; however, its effects on tumour metastasis are largely unknown. In the present study
Qingfei Zheng et al.
Nature communications, 11(1), 3241-3241 (2020-06-28)
Protein arginine deiminase 4 (PAD4) facilitates the post-translational citrullination of the core histones H3 and H4. While the precise epigenetic function of this modification has not been resolved, it has been shown to associate with general chromatin decompaction and compete
Luis E Muñoz et al.
Immunity, 51(3), 443-450 (2019-08-20)
The presence of gallstones (cholelithiasis) is a highly prevalent and severe disease and one of the leading causes of hospital admissions worldwide. Due to its substantial health impact, we investigated the biological mechanisms that lead to the formation and growth

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