QUINOMYCIN A Struktur

QUINOMYCIN A

Bezeichnung:QUINOMYCIN A

CAS-Nr512-64-1

Englisch Name:QUINOMYCIN A

CBNumberCB6394145

SummenformelC51H64N12O12S2

Molgewicht1101.26

MOL-Datei512-64-1.mol

QUINOMYCIN A physikalisch-chemischer Eigenschaften

Schmelzpunkt	217-218℃
alpha	D20 -310° (c = 0.86 in chloroform)
Siedepunkt	1427.2±65.0 °C(Predicted)
Dichte	1.0964 (rough estimate)
Brechungsindex	1.6700 (estimate)
storage temp.	-20°C
Löslichkeit	Soluble in DMSO (up to 5 mg/ml)
pka	9.38±0.70(Predicted)
Aggregatzustand	White solid
Farbe	white to beige
Merck	13,3531
Stabilität	Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	46-23/24/25
S-Sätze:	53-36/37/39-45
RIDADR	UN 3462 6.1/PG 2
WGK Germany	3
RTECS-Nr.	JW5250000
F	10
HazardClass	6.1(b)
PackingGroup	III
HS Code	2941900000

Gefahreninformationscode (GHS)

QUINOMYCIN A Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R46:Kann vererbbare Schäden verursachen.
R23/24/25:Giftig beim Einatmen, Verschlucken und Berührung mit der Haut.
S-Sätze Betriebsanweisung:
S53:Exposition vermeiden - vor Gebrauch besondere Anweisungen einholen.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Beschreibung
Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that controls genes involved in glycolysis, angiogenesis, migration, and invasion. Echinomycin is a cell-permeable inhibitor of HIF-1-mediated gene transcription. It acts by intercalating into DNA in a sequence-specific manner, blocking the binding of either HIF-1α or HIF-1β to the hypoxia-responsive element. Echinomycin reversibly inhibits hypoxia-induced HIF-1 transcription activity in U215 cells with an EC₅₀ value of 1.2 nM. It inhibits hypoxia-induced expression of vascular endothelial growth factor, blocking angiogenesis and altering excitatory synaptic transmission in hippocampal neurons. Echinomycin also impairs expression of survivin, enhancing the sensitivity of multiple myeloma cells to melphalan.
Verwenden
Quinomycin A is a cyclic depsipeptide metabolite. Quinomycin A has broad activity against bacteria, fungi and viruses, and has found application as an antitumor agent. Quinomycin A acts by bifunctional intercalation of nucleic acids. Recent research has shown quinomycin A to be an extremely potent inhibitor of hypoxia-inducible factor-1 (HIF-1). This transcription factor plays an essential role in tumor progression and metastasis.
Verwenden
Quiniomycin A is a cyclic depsipeptide metabolite. Quinomycin A has broad activity against bacteria, fungi and viruses, and has found application as an antitumour agent. Quinomycin A acts by bifunctional intercalation of nucleic acids. Recent research has shown quinomycin A to be an extremely potent inhibitor of hypoxia-inducible factor-1 (HIF-1). This transcription factor plays an essential role in tumour progression and metastasis.
Verwenden
Echinomycin has been used for inhibition of hypoxia-inducible factor 1.
Biochem/physiol Actions
Echinomycin is an antitumor antibiotic and potent hypoxia inducible factor 1α (HIF-1α) inhibitor. It binds to DNA via bifunctional intercalation, blocking the binding of HIF-1α, a transcription factor important in tumor growth. Echinomycin selectively eliminated cancer stem cells in a study with mouse lymphoma and human AML xenogeneic models, eradicating the lymphomas. Recently, echinomycin was also found to act as an antibiotic adjuvant having synergistic effects with novobiocin in gram negative bacteria.
Lager
Store at -20°C
Einzelnachweise
1) Kong?et al.?(2005),?Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity; Cancer Res.,?65?9047 2) Wang?et al. (2014),?Echinomycin protects mice against relapsed acute myeloid leukemia without adverse effect on hematopoietic stem cells; Blood,?124?1127 3) Wang?et al. (2011),?Targeting HIF1α eliminates cancer stem cells in hematological malignancies; Cell Stem Cell.,?8?399 4) Li?et al. (2015),?Hypoxia-inducible factor-1α regulates the expression of L-type voltage-dependent Ca(2+) channels in PC12 cells under hypoxia; Cell Stress Chaperones,?20?507

QUINOMYCIN A Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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