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2-(N-(5-bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-((3,5-dichlorophenyl)sulfonamido)benzoic acid methyl ester, also known as MDL-800, is a complex organic compound with a unique chemical structure. It is an allosteric activator of SIRT6, a protein deacetylase enzyme involved in various cellular processes, including DNA repair and cell cycle regulation. MDL-800 specifically activates the deacetylase activity of SIRT6, without affecting other SIRT proteins or HDACs. It has demonstrated inhibitory effects on the growth of human hepatocarcinoma cells and non-small cell lung carcinoma cell lines, making it a promising candidate for cancer therapy.

2275619-53-7

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2275619-53-7 Usage

Uses

Used in Cancer Therapy:
MDL-800 is used as an anticancer agent for the treatment of hepatocellular carcinoma (HCC) and non-small cell lung carcinoma (NSCLC). It inhibits the growth of cancer cells by activating the tumor suppressor deacetylase activity of SIRT6, leading to cell cycle arrest and reduced proliferation. Additionally, MDL-800 has shown synergistic effects when combined with EGFR kinase inhibitors, enhancing the efficacy of these drugs in resistant cancer cells.
Used in Age-Related Disease Treatment:
MDL-800 is used as a potential treatment for age-related diseases through its ability to improve the genetic stability of induced pluripotent stem cells (iPSCs) derived from old murine sources. By activating the NHEJ and BER DNA repair pathways, MDL-800 enhances the functionality and therapeutic potential of iPSC-based therapies for age-related conditions.
Used in Drug Resistance Overcoming:
MDL-800 is used to overcome drug resistance in cancer treatment, particularly in cases of resistance to EGFR kinase inhibitors. Its ability to enhance the effects of these drugs in resistant cancer cells, such as Osimertinib-resistant HCC827 and PC9 cells, as well as in patient-derived primary tumor cells, makes it a valuable tool in the development of more effective cancer therapies.

References

Huang et al. (2018) Identification of a cellularly active SIRT6 allosteric activator; Chem. Biol.?14 1118 Chen et al. (2020) The SIRT6 activator MDL-800 improves genomic stability and pluripotency of old murine-derived iPS cells; Aging Cell?19 e13185 Shang et al. (2021) MDL-800, an allosteric activator of SIRT6, suppresses proliferation and enhances EGFR-TKIs therapy in non-small cell lung cancer; Acta Pharmacol. Sin.?42 120

Check Digit Verification of cas no

The CAS Registry Mumber 2275619-53-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 2,2,7,5,6,1 and 9 respectively; the second part has 2 digits, 5 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 2275619-53:
(9*2)+(8*2)+(7*7)+(6*5)+(5*6)+(4*1)+(3*9)+(2*5)+(1*3)=187
187 % 10 = 7
So 2275619-53-7 is a valid CAS Registry Number.

2275619-53-7Downstream Products

2275619-53-7Relevant academic research and scientific papers

MDL-800, an allosteric activator of SIRT6, suppresses proliferation and enhances EGFR-TKIs therapy in non-small cell lung cancer

Shang, Jia-lin,Ning, Shao-bo,Chen, Ying-yi,Chen, Tian-xiang,Zhang, Jian

, p. 120 - 131 (2021)

Sirtuin 6 (SIRT6), a member of the sirtuin family, is a nicotinamide adenine dinucleotide (NAD+)-dependent deacetylase that is involved in various physiological and pathological processes. SIRT6 is generally downregulated and linked to tumorige

Compounds having effect of activating SIRT6 deacetylation activity, SIRT6 activator and application of SIRT6 activator

-

Paragraph 0033; 0035; 0043-0045, (2020/01/25)

The invention provides compounds having an effect of activating SIRT6 deacetylation activity, or a pharmaceutically acceptable salt of the compounds. The compounds have a structure represented a formula (I) shown in the description. The invention also pro

Discovery of Potent Small-Molecule SIRT6 Activators: Structure-Activity Relationship and Anti-Pancreatic Ductal Adenocarcinoma Activity

Chen, Xiuli,Sun, Weining,Huang, Shenzhen,Zhang, Hailin,Lin, Guifeng,Li, Hui,Qiao, Jingxin,Li, Linli,Yang, Shengyong

supporting information, p. 10474 - 10495 (2020/11/02)

SIRT6 activation is thought to be a promising target for the treatment of many diseases, particularly cancer. Herein, we report the discovery of a series of new small-molecule SIRT6 activators. Structure-activity relationship analyses led to the identific

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