Stattic
Synonym(s):6-Nitrobenzo[b]thiophene-1,1-dioxide;6-Nitrobenzo[b]thiophene-1,1-dioxide, Stat three inhibitory compound;Stat three inhibitory compound;STAT3 Inhibitor V, Stattic - CAS 19983-44-9 - Calbiochem
- CAS NO.:19983-44-9
- Empirical Formula: C8H5NO4S
- Molecular Weight: 211.19
- MDL number: MFCD00173799
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-09 19:38:33
What is Stattic?
Description
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.
The Uses of Stattic
Stattic is a Stat3 inhibitor which exhibited potent anti-tumor and induced chemo- and radio-sensitivity in nasopharyngeal carcinoma.
The Uses of Stattic
Stattic was used to study Stat3-mediated cell signaling in human lung carcinoma cells.5
What are the applications of Application
Stat3 inhibitor V, stattic is an inhibitor of Stat3 activation
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.
Biological Activity
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
storage
+4°C
References
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
Properties of Stattic
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 for Stattic
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P270:Do not eat, drink or smoke when using this product. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Stattic
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