DMXAA - CAS 117570-53-3
Catalog number: B0084-082134
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C17H14O4
Molecular Weight:
282.29
COA:
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Targets:
STING | Others
Description:
STING agonist; Induces antitumor immunological responses
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-082134 25 mg $199 In stock
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Brife Description:
STING agonist; Induces antitumor immunological responses
Appearance:
Solid powder
Synonyms:
ASA404; ASA 404; ASA404; AS1404; AS 1404; AS1404; DMXAA; Vadimezan; 2-(5,6-dimethyl-9-oxoxanthen-4-yl)acetic acid
Solubility:
Soluble to 20 mM in DMSO
Storage:
Store at +4°C
MSDS:
Inquire
Quality Standard:
In-house
Quantity:
Grams-Kilos
Boiling Point:
~520.9° C at 760 mmHg (Predicted)
Melting Point:
189.81° C (Predicted)
InChIKey:
XGOYIMQSIKSOBS-UHFFFAOYSA-N
InChI:
1S/C17H14O4/c1-9-6-7-13-15(20)12-5-3-4-11(8-14(18)19)17(12)21-16(13)10(9)2/h3-7H,8H2,1-2H3,(H,18,19)
Canonical SMILES:
CC1=C(C2=C(C=C1)C(=O)C3=C(O2)C(=CC=C3)CC(=O)O)C
1.STING agonists induce an innate antiviral immune response against hepatitis B virus.
Guo F1, Han Y2, Zhao X3, Wang J4, Liu F1, Xu C1, Wei L4, Jiang JD5, Block TM3, Guo JT1, Chang J6. Antimicrob Agents Chemother. 2015 Feb;59(2):1273-81. doi: 10.1128/AAC.04321-14. Epub 2014 Dec 15.
Chronicity of hepatitis B virus (HBV) infection is due to the failure of a host to mount a sufficient immune response to clear the virus. The aim of this study was to identify small-molecular agonists of the pattern recognition receptor (PRR)-mediated innate immune response to control HBV infection. To achieve this goal, a coupled mouse macrophage and hepatocyte culture system mimicking the intrahepatic environment was established and used to screen small-molecular compounds that activate macrophages to produce cytokines, which in turn suppress HBV replication in a hepatocyte-derived stable cell line supporting HBV replication in a tetracycline-inducible manner. An agonist of the mouse stimulator of interferon (IFN) genes (STING), 5,6-dimethylxanthenone-4-acetic acid (DMXAA), was found to induce a robust cytokine response in macrophages that efficiently suppressed HBV replication in mouse hepatocytes by reducing the amount of cytoplasmic viral nucleocapsids.
2.Tumor interstitial fluid promotes malignant phenotypes of lung cancer independently of angiogenesis.
Li H1, Li G1, Liu L1, Guo Z1, Ma X1, Cao N1, Lin H1, Han G1, Duan Y2, Du G3. Cancer Prev Res (Phila). 2015 Nov;8(11):1120-9. doi: 10.1158/1940-6207.CAPR-15-0242. Epub 2015 Sep 4.
Angiogenesis is necessary for cancer progression, but antiangiogenic therapy actually promotes tumor recurrence, progression, and metastasis. This study focused on the contribution of the tumor interstitial fluid (TIF) to lung cancer progression. TIF was isolated and quantified for 10 μg protein/mL. Malignant driver characteristics of TIF were examined by tumor-initiating cells (TIC), self-renewal, epithelial-mesenchymal transition (EMT), autophagy, and apoptosis in vitro. In vivo tumor model was used to investigate the mechanistic roles of TIF in lung cancer progression. In vitro, TIF exhibited distinct malignant driver characteristics, which led to increased numbers of TICs, increased self-renewal and EMT, as well as to decreased autophagy and apoptosis under cell starvation conditions. In vivo, the contribution of TIF was similar, as judged by increased TICs indicated by the cancer stem cell marker Nanog, the proliferation marker proliferating cell nuclear antigen, and the EMT marker N-cadherin; TIF also increased the formation of pulmonary tumors.
3.Preliminary Evidence That High-Dose Vitamin C has a Vascular Disrupting Action in Mice.
Baguley BC1, Ding Q1, Richardson E1. Front Oncol. 2014 Nov 5;4:310. doi: 10.3389/fonc.2014.00310. eCollection 2014.
High intravenous doses of vitamin C (ascorbic acid) have been reported to benefit cancer patients, but the data are controversial and there is incomplete knowledge of what physiological mechanisms might be involved in any response. Vitamin C is taken up efficiently by cells expressing SVCT2 transporters and since vascular endothelial cells express SVCT2, we explored the hypothesis that administration of high-dose vitamin C (up to 5 g/kg) to mice might affect vascular endothelial function. A single administration of vitamin C to mice induced time- and dose-dependent increases in plasma concentrations of the serotonin metabolite 5-hydroxyindole acetic acid (5-HIAA), a marker for vascular disrupting effects. Responses were comparable to those for the tumor vascular disrupting agents, vadimezan and fosbretabulin. High-dose vitamin C administration decreased tumor serotonin concentrations, consistent with the release of serotonin from platelets and its metabolism to 5-HIAA.
4.Binding-pocket and lid-region substitutions render human STING sensitive to the species-specific drug DMXAA.
Gao P1, Zillinger T2, Wang W3, Ascano M4, Dai P3, Hartmann G2, Tuschl T4, Deng L3, Barchet W5, Patel DJ6. Cell Rep. 2014 Sep 25;8(6):1668-76. doi: 10.1016/j.celrep.2014.08.010. Epub 2014 Sep 4.
The drug DMXAA (5,6-dimethylxanthenone-4-acetic acid) showed therapeutic promise against solid tumors in mouse models but subsequently failed in human clinical trials. DMXAA was later discovered to activate mouse, but not human, STING, an adaptor protein in the cyclic dinucleotide cGAMP-mediated signaling pathway, inducing type I interferon expression. To facilitate the development of compounds that target human STING, we combined structural, biophysical, and cellular assays to study mouse and human chimeric proteins and their interaction with DMXAA. We identified a single substitution (G230I) that enables a DMXAA-induced conformational transition of hSTING from an inactive "open" to an active "closed" state. We also identified a substitution within the binding pocket (Q266I) that cooperates with G230I and the previously identified S162A binding-pocket point substitution, rendering hSTING highly sensitive to DMXAA. These findings should facilitate the reciprocal engineering of DMXAA analogs that bind and stimulate wild-type hSTING and their exploitation for vaccine-adjuvant and anticancer drug development.
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CAS 117570-53-3 DMXAA

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