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AdipoGen Life Sciences
DMB [GLP-1R Agonist]
50
CHF
CHF 50.00
In stock
AG-CR1-3759-M0011 mgCHF 50.00
AG-CR1-3759-M0055 mgCHF 200.00
AG-CR1-3759-M02525 mgCHF 680.00
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| Product Details | |
|---|---|
| Synonyms | GSDMD Activator; 6,7-Dichloro-N-(1,1-dimethylethyl)-3-(methyl-sulfonyl)-2-quinoxalinamine; 6,7-Dichloro-2-methylsulfonyl-3-N-tert-butylaminoquinoxaline (DMB) |
| Product Type | Chemical |
| Properties | |
| Formula |
C13H15Cl2N3O2S |
| MW | 348.2 |
| CAS | 281209-71-0 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | Yellow solid. |
| Solubility | Soluble in DMSO (20mg/ml). |
| InChi Key | GNZCSGYHILBXLL-UHFFFAOYSA-N |
| Smiles | ClC1=C(Cl)C=C(N=C(NC(C)(C)C)C(S(C)(=O)=O)=N2)C2=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS | Inquire |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
Description
- DMB is a small molecule GLP-1 receptor agonist (GLP-1R; KB = 26.3 nM for the recombinant human receptor). DMB exerts its activating effect by forming hydrogen bonds with the Tyr42, Cys71 and Ser84 residues of GLP-1R.
- GLP-1 receptor signaling is a predominant mechanism for regulating glucose homeostasis. DMB represents a unique non-peptide tool for studying the role of GLP-1 in both in vivo and in vitro diabetes and obesity models.
- DMB is a selective small molecule gasdermin D (GSDMD) agonist for inducing pyroptosis and enhancing anti-tumor immunity.
- DMB can directly activate GSDMD-mediated cancer cell pyroptosis. Unlike traditional pathways requiring GSDMD cleavage, DMB induces pyroptosis without this step, effectively stimulating anti-tumor immune responses with minimal toxicity. It achieves this by covalently modifying the Cys191 residue in GSDMD, disrupting the interaction between the N-terminus (NT) and C-terminus (CT). This keeps GSDMD in an activated state without cleavage, promoting pore formation and inducing pyroptosis while preserving the overall GSDMD structure.
Product References
- Small-molecule agonists for the glucagon-like peptide 1 receptor: L.B. Knudsen, et al.; PNAS 104, 937 (2007)
- Insulin-releasing and metabolic effects of small molecule GLP-1 receptor agonist 6,7-dichloro-2-methylsulfonyl-3-N-tert-butylaminoquinoxaline: N. Irwin, et al.; Eur. J. Pharmacol. 628, 268 (2010)
- Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: Implications for drug screening: C. Koole, et al.; Mol. Pharmacol. 78, 456 (2010)
- An Orally Active Allosteric GLP-1 Receptor Agonist Is Neuroprotective in Cellular and Rodent Models of Stroke: H. Zhang, et al.; PLoS One 11, e0148827 (2016)
- Intermittent Use of a Short-Course Glucagon-like Peptide-1 Receptor Agonist Therapy Limits Adverse Cardiac Remodeling via Parkin-dependent Mitochondrial Turnover: J.F. Germano, et al.; Sci. Rep. 10, 8284 (2020)
- A quinoxaline-based compound ameliorates bone loss in ovariectomized mice: Y. Zhou, et al.; Exp. Biol. Med. 246, 2502 (2021)
- Small-molecule GSDMD agonism in tumors stimulates antitumor immunity without toxicity: P. Fontana, et al.; Cell 187, 6165 (2024)
- DMB-induced GSDMD-mediated pyroptosis: a novel therapeutic strategy for enhancing anti-tumor immunity: J. Shentu, et al.; Cell Death Discov. 10, 482 (2024) (Review)