Stattic

Stattic Basic information
Product Name:Stattic
Synonyms:BUTTPARK 97\04-73;6-NITRO-1H-1LAMBDA6-BENZO[B]THIOPHENE-1,1-DIONE;AKOS 1001;6-Nitro-1-benzothiophene 1,1-dioxide;1,1-DIOXO-6-NITROBENZO(B)THIOPHENE;6-Nitrobenzo[b]thiophene-1,1-dioxide, Stat three inhibitory compound;Stattic;6-Nitrobenzo[b]thiophene1,1-dioxide
CAS:19983-44-9
MF:C8H5NO4S
MW:211.19
EINECS:
Product Categories:Inhibitors;JAK;JAK/STAT;STAT
Mol File:19983-44-9.mol
Stattic Structure
Stattic Chemical Properties
Melting point 187-188 °C
Boiling point 461.1±45.0 °C(Predicted)
density 1.621±0.06 g/cm3(Predicted)
storage temp. Sealed in dry,2-8°C
solubility DMSO: >20mg/mL
form powder
color white to beige
Stability: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.
Safety Information
Hazard Codes Xi,Xn
Risk Statements 20/21/22-36/37/38-22
Safety Statements 26-36/37/39
WGK Germany 3
Hazard Note Irritant
HS Code 2934999090
MSDS Information
Stattic Usage And Synthesis
DescriptionStattic (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.
UsesStattic is a Stat3 inhibitor which exhibited potent anti-tumor and induced chemo- and radio-sensitivity in nasopharyngeal carcinoma.
UsesStattic was used to study Stat3-mediated cell signaling in human lung carcinoma cells.5
DefinitionChEBI: 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.
Biological ActivitySmall 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 ActionsStattic (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
storage+4°C
References1) 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 Preparation Products And Raw materials
Preparation Products2,3-dihydro-1-benzothiophen-6-amine
Ruxolitinib Cantharidin (E)-3-[[[3-[2-(7-CHLORO-2-QUINOLINYL)ETHENYL]PHENYL]-[[(3-DIMETHYLAMINO)-3-OXOPROPYL]THIO]METHYL]THIO]-PROPANOIC ACID, SODIUM SALT S3I-201 Trametinib Cryptotanshinone ZM 336372 Fludarabine Bortezomib ZM 447439 AKOS 93258 AKOS 93253 AKOS 90053 Stattic AKOS 93702 AKOS 93261

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