SML2161
STA-21
≥95% (HPLC)
别名:
(±)-Deoxytetrangomycin, (±)-Ochromycinone, 3,4-Dihydro-8-hydroxy-3-methylbenz[a]anthracene-1,7,12(2H)-trione, NSC 628869, STA 21, STA21
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关于此项目
经验公式（希尔记法）:
C19H14O4
化学文摘社编号:
分子量:
306.31
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
InChI
1S/C19H14O4/c1-9-7-10-5-6-12-17(15(10)14(21)8-9)19(23)11-3-2-4-13(20)16(11)18(12)22/h2-6,9,20H,7-8H2,1H3
InChI key
ZAWXOCUFQSQDJS-UHFFFAOYSA-N
SMILES string
CC1CC(C(C(C(C(C=CC=C2O)=C2C3=O)=O)=C3C=C4)=C4C1)=O
assay
≥95% (HPLC)
form
powder
color
yellow to brown
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Application
STA-21 has been used as a signal transducer and activator of transcription 3 (STAT3) inhibitor to study its effects on glioblastoma and primary glioblastoma cells. It has also been used as a STAT3 dimerization inhibitor to study its effects on severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) production in human lung cancer cell line.
Biochem/physiol Actions
STA-21 is a STAT3 inhibitor that reduces the constitutively high STAT3 transcriptional activity in Caov-3 and MDA-MB-435s cultures (by 9.125- and 5.765-fold, respectively, post 48-hr 20 μM treatment) by disrupting STAT3 homodimerization, an essential process for STAT3 nuclear localization and DNA-binding activity. STA-21 selectively inhibits the growth and survival of breast carcinoma cells with constitutive Stat3 signaling (26%, 25%, 56% apoptotic cells, respectively, in MDA-MB-231, MDA-MB-435s, and MDA-MB-468 cultures, respectively, post 48-hr 20 μM treatment) but not those without (<10% apoptosis in MCF7, MDA-MB-453, HSF cultures post 48-hr 20 μM treatmen). STA-21 is reported to alleviate autoimmune inflammation in a murine model of rheumatoid arthritis (RA; 0.5 mg/kg; 3X i.p./week) and reduce airway inflammation in allergic mice with psoriatic inflammation (20 μg/mouse/day topically) in vivo.
STAT3 homodimerization inhibitor with anti-cancer and anti-inflammation efficacy in vitro and in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
涉药品监管产品
此项目有
Chun-Liang Chen et al.
Molecular cancer, 7, 78-78 (2008-10-23)
Constitutive activation of signal transducer and activator of transcription 3 (Stat3) signaling pathway plays an important role in several human cancers. Activation of Stat3 is dependent on the phosphorylation at the tyrosine residue 705 by upstream kinases and subsequent nuclear
Chun-Liang Chen et al.
BMC cancer, 7, 111-111 (2007-06-30)
Stat3 has been classified as a proto-oncogene and constitutive Stat3 signaling appears to be involved in oncogenesis of human cancers. However, whether constitutive Stat3 signaling plays a role in the survival and growth of osteosarcomas, rhabdomyosarcomas, and soft-tissue sarcomas is
Sheikh Fayaz Ahmad et al.
Immunobiology, 222(2), 206-217 (2016-10-09)
We set out to investigate the influence of STA-21, a dynamic STAT-3 inhibitor, on the expansion and progression of rheumatoid arthritis (RA), and to determine its potential mechanisms of action in a mouse model of collagen antibody-induced arthritis (CAIA). To
Davide Genini et al.
Proceedings of the National Academy of Sciences of the United States of America, 114(25), E4924-E4933 (2017-06-07)
In addition to its canonical role in nuclear transcription, signal transducer and activator of transcription 3 (STAT3) is emerging as an important regulator of mitochondrial function. Here, we demonstrate that a novel inhibitor that binds with high affinity to the
Hui Song et al.
Proceedings of the National Academy of Sciences of the United States of America, 102(13), 4700-4705 (2005-03-23)
This study focused on the screening of small-molecule inhibitors that target signal transducers and activators of transcription 3 (Stat3) in human breast carcinoma. The constitutive activation of Stat3 is frequently detected in human breast cancer cell lines as well as
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