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Merck
모든 사진(1)

주요 문서

SML1658

Sigma-Aldrich

GSK484

≥98% (HPLC)

동의어(들):

((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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About This Item

실험식(Hill 표기법):
C27H31N5O3 · HCl
CAS Number:
Molecular Weight:
510.03
UNSPSC 코드:
51111800
PubChem Substance ID:
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

H2O: 2 mg/mL, clear (warmed)

저장 온도

2-8°C

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

생화학적/생리학적 작용

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.

특징 및 장점

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.

기타 정보

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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