Enzastaurin (LY317615)

Bezeichnung:Enzastaurin (LY317615)

CAS-Nr170364-57-5

Englisch Name:Enzastaurin (LY317615)

CBNumberCB92128716

SummenformelC32H29N5O2

Molgewicht515.6

MOL-Datei170364-57-5.mol

Enzastaurin (LY317615) physikalisch-chemischer Eigenschaften

Schmelzpunkt	249-261℃
Siedepunkt	767.2±60.0 °C(Predicted)
Dichte	1.34
RTECS-Nr.	UX9626850
Flammpunkt	417.8℃
storage temp.	-20°C
Löslichkeit	DMSO: soluble10mg/mL, clear (warmed)
Aggregatzustand	powder
pka	7.88±0.60(Predicted)
Farbe	, light orange to dark orange-red
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22
WGK Germany	3
HS Code	29339900

Gefahreninformationscode (GHS)

Enzastaurin (LY317615) Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Enzastaurin (170364-57-5) is a potent and selective PKCβ inhibitor.? IC50 = 6, 39, 83 and 110 nM, for PKCβ, PKCα, PKCγ and PKCε respectively.1 Induces apoptosis in multiple myeloma cell lines via inhibition of the AKT signaling pathway.2 Induces mitotic missegregation and preferential cytotoxicity in colorectal cancer cells with chromosomal instability.3 Attenuates amphetamine-stimulated dopamine efflux.4 Inhibits blood-brain barrier leakiness in a mouse model.5
Verwenden
PKCβ-selective inhibitor, suppresses angiogenesis.
Verwenden
Enzastaurin has been used in splicing analysis to study its effects on splicing of a mutated exon.
Definition
ChEBI: 3-(1-methyl-3-indolyl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-3-indolyl]pyrrole-2,5-dione is a member of indoles and a member of maleimides.
Biochem/physiol Actions
Enzastaurin is a potent and PKCβ preferring inhibitor. Also, Enzastaurin inhibits AKT and GSK3β. Enzastaurin acts as anti-angiogenic and antineoplastic agent.
Einzelnachweise
1) Graff et al. (2005), The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts; Cancer Res. 65 7462 2) Rizvi et al. (2006) Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines; Mol.Cancer Ther. 5 1783 3) Ouaret and Larsen (2014), Protein kinase Cβ inhibition by enzastaurin leads to mitotic missegregation and preferential cytotoxicity toward colorectal cancer cells with chromosomal instability (CIN); Cell Cycle 13 2697 4) Zestos et al. (2016), PKCβ Inhibitors Attenuate Amphetamine-Stimulated Dopamine Efflux; ACS Chem.Neurosci. 7 757 5) Stranahan et al. (2016), Blood-brain barrier breakdown promotes macrophage infiltration and cognitive impairment in leptin receptor-deficient mice; J.Cereb.Blood Flow Metab. 36 2108

Enzastaurin (LY317615) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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