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GSK484

GSK484 Struktur
1652591-81-5
CAS-Nr.
1652591-81-5
Englisch Name:
GSK484
Synonyma:
GSK484;CS-2265;AOB6992;GTPL8577;GSK484 HCl;GSK484 >=98% (HPLC);PAD4 inhibitor GS484;PAD4 inhibitor GSK484;GSK484 (hydrochloride);GSK484, PAD4 inhibitor
CBNumber:
CB63146499
Summenformel:
C27H32ClN5O3
Molgewicht:
510.04
MOL-Datei:
1652591-81-5.mol

GSK484 Eigenschaften

storage temp. 
2-8°C
L?slichkeit
DMSO:25.0(Max Conc. mg/mL);49.01(Max Conc. mM)
Ethanol:25.0(Max Conc. mg/mL);49.01(Max Conc. mM)
PBS buffer (pH 7.2):5.0(Max Conc. mg/mL);9.8(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);58.82(Max Conc. mM)
Aggregatzustand
powder
Farbe
white to beige
InChIKey
MULKOGJHUZTANI-JEGYXLSDNA-N
SMILES
C(C1CC1)N1C2=CC=CC=C2C=C1C1=NC2=CC(C(N3CC[C@@H](O)[C@@H](N)C3)=O)=CC(OC)=C2N1C.Cl |&1:22,24,r|
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
HS Code  2933399990
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitssch?dlich bei Verschlucken. Akute Toxizit?t oral Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P270, P301+P312, P330, P501
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizit?t (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
Sicherheit
P261 Einatmen von Staub vermeiden.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen.

GSK484 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme. It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils. It exhibits favorable pharmacokinetic profiles in mouse and rat. See the Structural Genomics Consortium (SGC) website for more information.

Verwenden

GSK484 is a novel selective PAD4 inhibitor.

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.

GSK484 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

GSK484 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 92)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hubei Chuchang Biotech Co., Ltd.
+undefined15623860702
 info@chuchangbiotech.com China 212 58
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795
ivan@atkchemical.com China 32956 60
Career Henan Chemica Co 		+86-0371-86658258 +8613203830695
 laboratory@coreychem.com China 30238 58
Zhejiang J&C Biological Technology Co.,Limited 		+1-2135480471 +1-2135480471
 sales@sarms4muscle.com China 10473 58
InvivoChem 		+1-708-310-1919 +1-13798911105
 sales@invivochem.cn United States 6391 58
LEAP CHEM CO., LTD. 		+86-852-30606658
market18@leapchem.com China 24727 58
Nantong HI-FUTURE Biology Co., Ltd. 		+undefined18051384581
 sales@chemhifuture.com China 3135 58
TargetMol Chemicals Inc.
support@targetmol.com United States 38631 58
Hebei Miaoyin Technology Co.,Ltd 		+86-17367732028 +86-17367732028
 kathy@hbyinsheng.com China 3512 58
Wuhan Topule Biopharmaceutical Co., Ltd 		+8618327326525
 masar@topule.com China 8467 58
  • GSK484
  • GSK484 (hydrochloride)
  • CS-2265
  • PAD4 inhibitor GS484
  • GSK484 HCl
  • ((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
  • GTPL8577
  • GSK484 >=98% (HPLC)
  • PAD4 inhibitor GSK484
  • GSK484 hydrochloride,GSK 484,Protein Arginine Deiminase,GSK-484,GSK-484 hydrochloride,GSK484,inhibit,Peptidylarginine Deiminase,Inhibitor
  • ((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 , GSK484 HCl
  • GSK484, PAD4 inhibitor
  • 1652591-81-5
  • 652591-81-5
  • C27H31N5O3ClH
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