General Information of the Drug (ID: M6ADRUG0040)
Name
P5091
Synonyms
P005091; P5091; P-5091; 1-(5-(2,3-dichlorophenylthio)-4-nitrothiophen-2-yl)ethanone; 1-[5-(2,3-Dichloro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone; CHEMBL2159495; P5091 (P005091); 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone; 1-(5-((2,3-Dichlorophenyl)thio)-4-nitrothiophen-2-yl)ethanone; Cyto5D7; C12H7Cl2NO3S2; SCHEMBL2681288; DTXSID90384841; 1-[5-[(2,3-Dichlorophenyl)thio]-4-nitro-2-thienyl]ethanone; HMS3653E09; HMS3743M19; ZINC125366; BCP07750; EX-A2120; BDBM50393437; MFCD00123202; s7132; AKOS024458314; CCG-240421; CS-1445; MCULE-6661883192; QC-8200; SB19505; NCGC00379189-01; AC-32692; BS-17872; DA-40897; HY-15667; FT-0714931; SW219710-1; Y1893; J3.502.625H; C76908; P 5091; P-05091; P005091(P5091); P 005091; 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitro-2-thienyl]ethanone; 1-[5-(2,3-dichlorophenylsulfanyl)-4-nitro-2-thienyl]ethanone; 1-[5-[(2,3-Dichlorophenyl)thio]-4-n?itro-2-thienyl]ethanone; 1-(5-((2,3-Dichlorophenyl)thio)-4-nitrothiophen-2-yl)ethan-1-one; 1-{5-[(2,3-Dichlorophenyl)sulfanyl]-4-nitrothiophen-2-yl}ethan-1-one
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Status Investigative [1]
Structure
Formula
C12H7Cl2NO3S2
InChI
InChI=1S/C12H7Cl2NO3S2/c1-6(16)10-5-8(15(17)18)12(20-10)19-9-4-2-3-7(13)11(9)14/h2-5H,1H3
InChIKey
LKZLGMAAKNEGCH-UHFFFAOYSA-N
PubChem CID
2819993
Full List of m6A Targets Related to This Drug
Ubiquitin carboxyl-terminal hydrolase 7 (USP7)
In total 1 item(s) under this target gene
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene [2]
Response Summary The m6A demethylase FTO promotes the growth of Non-small cell lung cancer cells by increasing the expression of USP7.Genetic knockdown or pharmacological inhibition (P5091 or P22027) of Ubiquitin carboxyl-terminal hydrolase 7 (USP7) reduced the proliferation rate of lung cancer cells and decreased the capacity of colony formation of lung cancer cells in vitro, whereas lung cancer cells growth inhibition by FTO knockdown is restored by overexertion of USP7.
Responsed Disease Non-small-cell lung carcinoma ICD-11: 2C25.Y
Target Regulator Fat mass and obesity-associated protein (FTO) ERASER
Target Regulation Up regulation
Cell Process Ubiquitination degradation
In-vitro Model A-549 Lung adenocarcinoma Homo sapiens CVCL_0023
NCI-H522 Lung adenocarcinoma Homo sapiens CVCL_1567
HSAEC (Human small airway epithelial cells)
RERF-LC-A1 Lung squamous cell carcinoma Homo sapiens CVCL_4402
NCI-H1882 Lung small cell carcinoma Homo sapiens CVCL_1504
NCl-H466 (Human lung cancer cell line)
In-vivo Model Equal numbers of A549 cells expressing either control or shFTO were injected subcutaneously, within 30 min of harvesting, over the right and left flanks in male nu/nu mice between 4 and 6 weeks of age.
References
Ref 1 A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance. Cancer Cell. 2012 Sep 11;22(3):345-58. doi: 10.1016/j.ccr.2012.08.007.
Ref 2 The m6A demethylase FTO promotes the growth of lung cancer cells by regulating the m6A level of USP7 mRNA. Biochem Biophys Res Commun. 2019 May 7;512(3):479-485. doi: 10.1016/j.bbrc.2019.03.093. Epub 2019 Mar 21.