Stattic
STAT3 inhibitor / STAT3 inhibitor. Inhibits binding of tyrosine-phosphorylated peptides to STAT3 SH2 domain and inhibiting STAT3 activation, dimerization and nuclear translocation1. 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 STAT32. Exhibits potent antitumor activity3. Protects against angiotensin II-induced vascular dysfunction and hypertension4. An extremely useful tool to probe involvement of STAT3 in cellular signaling.
Biochemicals & reagents
19983-44-9
1) Schust et al. (2006), Stattic: a small molecule inhibitor of STAT3 activation and dimerization; Chem. Biol., 13 1235 2) Heildelberger 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 ani-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
-20°C
TARGET: Transcription factor -- PATHWAY: Apoptosis inducer; JAK/STAT; Transcription -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer; Hypertension