TPCA-1
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- CAS-Nr.
- 507475-17-4
- Englisch Name:
- TPCA-1
- Synonyma:
- TPCA-1;CS-991;GW683965;GW683965A;TPCA-1(TPCA 1);TPCA-1 USP/EP/BP;TPCA-1 (GW-683965;TPCA-1
IKK-2 Inhibitor IV;IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem;5-(4-Fluorophenyl)-2-ureidothiophene-3-carboxamide
- CBNumber:
- CB41073580
- Summenformel:
- C12H10FN3O2S
- Molgewicht:
- 279.29
- MOL-Datei:
- 507475-17-4.mol
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TPCA-1 Eigenschaften
- Schmelzpunkt:
- >217°C (dec.)
- Siedepunkt:
- 442.6±45.0 °C(Predicted)
- Dichte
- 1.490
- storage temp.
- 2-8°C
- Löslichkeit
- DMSO: soluble5mg/mL, clear
- pka
- 13.12±0.50(Predicted)
- Aggregatzustand
- powder
- Farbe
- white to light brown
- Stabilität:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
TPCA-1 Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36:Reizt die Augen.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Verwenden
TPCA-1 is a direct dual inhibitor for both IKKβ (IKK-2) and STAT3. It inhibits STAT3 phosphorylation, DNA binding, and transactivation in vivo. Synergistic treatment of TPCA-1 with tyrosine kinase inhibitors (TKIs) can potentially be a more effective method for treating cancers.
Biologische Aktivität
Potent, selective inhibitor of I κ B kinase-2 (IKK-2) (IC 50 = 17.9 nM) that displays > 22-fold selectivity over IKK-1 and > 550-fold selectivity over other kinases and enzymes. Inhibits production of pro-inflammatory cytokines in vitro and in vivo and inhibits NF- κ B nuclear localisation. Reduces the severity and onset of collagen-induced arthritis; anti-inflammatory.
Biochem/physiol Actions
TPCA-1 is a potent and selective inhibitor of human IκB kinase-2 (IKK-2) with IC50 = 17.9 nM for IKK-2 compared to 400nm for IKK-1. It has been used to study inhibition of IKK-2 to prevent inflammatory mediator release in animal models of arthritis and airway inflammation.
TPCA-1 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
TPCA-1 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 113)Lieferanten
507475-17-4()Verwandte Suche:
- TPCA-1
- 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide
- 5-(4-Fluorophenyl)-2-ureidothiophene-3-carboxamide
- TPCA-1(TPCA 1)
- 3-ThiophenecarboxaMide, 2-[(aMinocarbonyl)aMino]-5-(4-fluorophenyl)-
- 5-(4-Fluorophenyl)-2-ureidothiophene-3-carboxamide TPCA-1
- TPCA-1
IKK-2 Inhibitor IV
- GW683965
- GW683965A
- CS-991
- IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem
- TPCA-1 USP/EP/BP
- TPCA-1 (GW-683965
- 2-(carbamoylamino)-5-(4-fluorophenyl)thiophene-3-carboxamide
- TPCA-1,Inhibitor,STAT,TPCA 1,Apoptosis,IKK,I kappa B kinase,IκB kinase,inhibit
- 507475-17-4
- NF-kB
