GSK484
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- 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
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GSK484 Eigenschaften
- storage temp.
- 2-8°C
- Löslichkeit
- 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
- Wasserlöslichkeit
- H2O: 2mg/mL, clear (warmed)
- 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 Sicherheitserklärung
- Gefahreninformationscode (GHS)
| WGK Germany |
WGK 3 |
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| HS Code |
2933399990 |
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| Speicherklasse |
11 - Combustible Solids |
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| Bildanzeige (GHS) |
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| Alarmwort |
Warnung
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| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitsschädlich bei Verschlucken. |
Akute Toxizität oral |
Kategorie 4 |
Warnung |
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P264, P270, P301+P312, P330, P501 |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
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P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
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P264, P280, P305+P351+P338,P337+P313P |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizität (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
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| 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 Möglichkeit entfernen. Weiter spülen. |
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GSK484 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
GSK484 is a reversible inhibitor of PAD4 (IC
50 = 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 Händler.
Global( 129)Lieferanten
- 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
- GSK484 hydrochloride, 10 mM in DMSO
- GSK-484 hydrochloride (GSK484)
- (3S,4R)-3-amino-1-({2-[1-(cyclopropylmethyl)indol-2-yl]-7-methoxy-1-methyl-1,3-benzodiazol-5-yl}carbonyl)piperidin-4-ol hydrochloride - [AC77953]
- 1652591-81-5
- 652591-81-5
- C27H31N5O3ClH
