NMS 873
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- CAS-Nr.
- 1418013-75-8
- Englisch Name:
- NMS 873
- Synonyma:
- NMS-873;CS-952;NMS873;NMS 873;NMS873/NMS-873;NMS-873, >=98%;NMS 873 USP/EP/BP;NMS-873, 10 mM in DMSO;VCP Inhibitor III, NMS-873;3-(3-(Cyclopentylthio)-5-(((2-methyl-4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)oxy)methyl)-4H-1
- CBNumber:
- CB82668408
- Summenformel:
- C27H28N4O3S2
- Molgewicht:
- 520.67
- MOL-Datei:
- 1418013-75-8.mol
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NMS 873 Eigenschaften
- Schmelzpunkt:
- >220°C (dec.)
- Siedepunkt:
- 769.3±70.0 °C(Predicted)
- Dichte
- 1.33±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- L?slichkeit
- DMSO: soluble25mg/mL, clear
- pka
- 2.48±0.12(Predicted)
- Aggregatzustand
- powder
- Farbe
- white to beige
- InChIKey
- UJGTUKMAJVCBIS-UHFFFAOYSA-N
- SMILES
- C1=NC=CC=C1N1C(COC2=CC=C(C3=CC=C(S(C)(=O)=O)C=C3)C(C)=C2)=NN=C1SC1CCCC1
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Kennzeichnung gef?hrlicher |
Xn |
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| R-S?tze: |
22 |
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| WGK Germany |
3 |
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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 |
Gesundheitssch?dlich bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 4 |
Warnung |
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P264, P270, P301+P312, P330, P501 |
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| Sicherheit |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
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NMS 873 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
The p97 AAA (ATPase associated with diverse cellular activities) is a ubiquitin-selective chaperone known to play a critical role in the degradation of misfolded membrane and secretory proteins and has been linked to various cellular processes that require unfolding and disassembly of protein complexes. Valosin-containing protein (VCP), also known as VCP/p97, is an AAA ATPase family member that serves as an integral component of the ubiquitin fusion degradation pathway and is overexpressed in many tumor types. NMS-873 is a VCP inhibitor (IC
50 = 24 nM) that demonstrates potent selectivity for VCP/p97 compared to a panel of other AAA ATPases, Hsp90, and 53 additional analyzed kinases (IC
50s >10 μM). It has been shown to inhibit the proliferation of HCT116 cancer cells with an IC
50 value of 380 nM.
Verwenden
NMS-873 is a potent and specific VCP inhibitor, which has shown to activate the unfolded protein response, interfere with autophagy and induce cancer cell death.
Biochem/physiol Actions
NMS-873 is a selective allosteric non–ATP-competitive inhibitor of the AAA ATPase family member valosine containing protein (VCP), also known as p97 (VCP/p97), an integral component of the ubiquitin fusion degradation (UFD) pathway. VCP/p97 plays a role in degradation of misfolded proteins, Golgi membrane reassembly, membrane transport, myofibril assembly, autophagosome maturation, and cell division, and is overexpressed in many tumor types. NMS-873 is the most potent and specific VCP inhibitor described to date. NMS-873 has an IC50 of 30 nM for VCP/p97 compared to IC50 >10 μM against all of the AAA ATPases, HSP90 or the 53 kinases analyzed. NMS-873 inhibited proliferation of HCT116 cancer cell line cells with an IC50 value of 400 nM.
NMS 873 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
NMS 873 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 138)Lieferanten
- NMS 873
- NMS873
- NMS873/NMS-873
- 3-[3-(CYCLOPENTYLSULFANYL)-5-({[2-METHYL-4'-(METHYLSULFONYL)-4-BI PHENYLYL]OXY}METHYL)-4H-1,2,4-TRIAZOL-4-YL]PYRIDINE
- Pyridine, 3-[3-(cyclopentylthio)-5-[[[2-methyl-4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]oxy]methyl]-4H-1,2,4-triazol-4-yl]-
- 3-[3-(Cyclopentylthio)-5-[[[2-methyl-4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]oxy]methyl]-4H-1,2,4-triazol-4-yl]pyridine NMS-873
- NMS 873 3-[3-(Cyclopentylthio)-5-[[[2-methyl-4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]oxy]methyl]-4H-1,2,4-triazol-4-yl]pyridine
- 3-[3-Cyclopentylsulfanyl-5-(4′-methanesulfonyl-2-methylbiphenyl-4-yloxymethyl)-[1,2,4]triazol-4-yl]-pyridine
- 3-(3-(Cyclopentylthio)-5-(((2-methyl-4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)oxy)methyl)-4H-1
- NMS-873, >=98%
- CS-952
- NMS 873 USP/EP/BP
- 3-(3-(Cyclopentylthio)-5-(((2-methyl-4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)oxy)methyl)-4H-1,2,4-triazol-4-yl)pyridine
- NMS-873, 10 mM in DMSO
- VCP Inhibitor III, NMS-873
- 3-[3-(cyclopentylthioyl)-5-[[[2-methyl-4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]oxy]methyl]-4H-1,2,4-triazole-4-yl]pyridine
- NMS-873
- 1418013-75-8
- Inhibitors
- api
