Stattic

Bezeichnung:Stattic

CAS-Nr19983-44-9

Englisch Name:Stattic

CBNumberCB7294835

SummenformelC8H5NO4S

Molgewicht211.19

MOL-Datei19983-44-9.mol

Stattic physikalisch-chemischer Eigenschaften

Schmelzpunkt	187-188 °C
Siedepunkt	461.1±45.0 °C(Predicted)
Dichte	1.621±0.06 g/cm3(Predicted)
storage temp.	Sealed in dry,2-8°C
Löslichkeit	DMSO: >20mg/mL
Aggregatzustand	powder
Farbe	white to beige
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.

Sicherheit

Kennzeichnung gefährlicher	Xi,Xn
R-Sätze:	20/21/22-36/37/38-22
S-Sätze:	26-36/37/39
WGK Germany	3
Hazard Note	Irritant
HS Code	2934999090

Gefahreninformationscode (GHS)

Stattic Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R22:Gesundheitsschädlich beim Verschlucken.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
Beschreibung
Stattic (19983-44-9) is a STAT3 inhibitor that inhibits binding of tyrosine-phosphorylated peptides to STAT3 SH2 domain and inhibiting STAT3 activation, dimerization and nuclear translocation.1 Displays selectivity over STAT1, STAT5, c-Myc/Max, Jun/Jun and Lck. Induces apoptosis in STAT3-dependent cancer cell lines. Alkyates four cysteine residues on STAT3.2 Exhibits potent antitumor activity.3 Protects against angiotensin II-induced vascular dysfunction and hypertension.4?Stattic is an extremely useful tool to probe involvement of STAT3 in cellular signaling.
Verwenden
Stattic was used to study Stat3-mediated cell signaling in human lung carcinoma cells.⁵
Verwenden
Stattic is a Stat3 inhibitor which exhibited potent anti-tumor and induced chemo- and radio-sensitivity in nasopharyngeal carcinoma.
Definition
ChEBI: Stattic is a member of the class of 1-benzothiophenes that is 1-benzothiophene-1,1-dioxide substituted at position 6 by a nitro group. Used as a radiosensitising agent for esophageal squamous cell carcinoma. It has a role as an antineoplastic agent, a STAT3 inhibitor and a radiosensitizing agent. It is a member of 1-benzothiophenes, a C-nitro compound and a sulfone.
Biologische Aktivität
Small molecule inhibitor of STAT3. Inhibits binding of tyrosine-phosphorylated peptide motifs to STAT3 SH2 domain and inhibits STAT3 activation, dimerization and nuclear translocation. Displays selectivity over STAT1, STAT5, c-Myc/Max, Jun/Jun and Lck. Induces apoptosis in STAT3-dependent cancer cell lines.
Biochem/physiol Actions
Stattic (Stat3 three inhibitory compound) alters the SH2 domain of Stat3 and indirectly inhibits with phosphopeptide binding. It is readily transported across the cell membrane compared to other phosphopeptides.2 Stattic induces increased formation of ROS and negatively affects the cardiomyocyte mitochondrial function,3 and sensitizes nasopharyngeal carcinoma cells to chemoradiotherapy.4
Lager
+4°C
Einzelnachweise
1) Schust et al. (2006), Stattic: a small molecule inhibitor of STAT3 activation and dimerization; Chem. Biol., 13 1235 2) Heidelberger et al. (2013), Investigation of the protein alkylation sites of the STAT3:STAT3 inhibitor Stattic by mass spectrometry; Bioorg. Med. Chem. Lett., 23 4719 3) Pan et al. (2013), Stat3 inhibitor Stattic exhibits potent anti-tumor activity and induces chemo- and radio-sensitivity in nasopharyngeal carcinoma; PLoS One, 8(1) e54565 4) Johnson et al. (2013), Small-molecules inhibitors of signal transducer and activator of transcription 3 protect against angiotensin II-induced vascular dysfunction and hypertension; Hypertension, 61 437

Stattic Upstream-Materialien And Downstream Produkte

Stattic Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

19983-44-9, Stattic Verwandte Suche:

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