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Merck
CN

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:
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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

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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
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
Hye-Jin Son et al.
Journal of immunology (Baltimore, Md. : 1950), 198(4), 1484-1491 (2017-01-18)
Oncostatin M (OSM) is a pleiotropic cytokine and a member of the IL-6 family. It has both proinflammatory and anti-inflammatory functions and is involved in the activation of STAT3 and STAT5. Rheumatoid arthritis is an autoimmune disease that causes chronic
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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