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:
产品名称
STA-21, ≥95% (HPLC)
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
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
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
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
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
Macarena Garrido-Tapia et al.
Immunobiology, 222(11), 1043-1051 (2017-06-06)
NKG2D is an activating receptor expressed on NK cells that binds to a variety of ligands, including MICA and MICB. These cell surface glycoproteins are overexpressed under cellular transformation, thus playing an important role in cell-mediated immune response to tumors.
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