m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG00054)
Name
SIS-3
Synonyms
SIS3 free base; Smad3 Inhibitor, SIS3; 1009104-85-1; Specific Inhibitor of Smad3; SIS3 (free base); (E)-1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one; 521985-36-4; Smad3 inhibitor SIS3; (E)-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3-(1-methyl-2-phenylpyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one; SCHEMBL6479525; SCHEMBL6479530; CHEMBL4303604; CHEBI:87589; 1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one; ZINC34299760; NCGC00387473-03; 6,7-Dimethyl-2-((2E)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-prop-2-enoyl))-1,2,3,4-tetrahydroisoquinoline; HY-100444; CS-0019029; J3.550.832E; J-000258; Q27159754; (2E)-1-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one; 2-Propen-1-one, 1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-
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Status
Preclinical
Structure
Formula
C28H27N3O3
InChI
1S/C28H27N3O3/c1-30-27(19-8-5-4-6-9-19)22(23-10-7-14-29-28(23)30)11-12-26(32)31-15-13-20-16-24(33-2)25(34-3)17-21(20)18-31/h4-12,14,16-17H,13,15,18H2,1-3H3/b12-11+
InChIKey
IJYPHMXWKKKHGT-VAWYXSNFSA-N
PubChem CID
10138988
TTD Drug ID
DF90DS
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Mothers against decapentaplegic homolog 3 (SMAD3)
ETS-related transcription factor Elf-3 (ELF3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Mothers against decapentaplegic homolog 3 (SMAD3) is a therapeutic target for SIS-3. The ETS-related transcription factor Elf-3 (ELF3) has potential in affecting the response of SIS-3 through regulating the expression of Mothers against decapentaplegic homolog 3 (SMAD3). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Mothers against decapentaplegic homolog 3 (SMAD3) is a therapeutic target for SIS-3. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of SIS-3 through regulating the expression of Mothers against decapentaplegic homolog 3 (SMAD3). [2], [3]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Mothers against decapentaplegic homolog 3 (SMAD3) is a therapeutic target for SIS-3. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of SIS-3 through regulating the expression of Mothers against decapentaplegic homolog 3 (SMAD3). [2], [4]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Mothers against decapentaplegic homolog 3 (SMAD3) is a therapeutic target for SIS-3. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of SIS-3 through regulating the expression of Mothers against decapentaplegic homolog 3 (SMAD3). [2], [5]
References
Ref 1 Involvement of Elf3 on Smad3 activation-dependent injuries in podocytes and excretion of urinary exosome in diabetic nephropathy. PLoS One. 2019 May 31;14(5):e0216788. doi: 10.1371/journal.pone.0216788. eCollection 2019.
Ref 2 In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
Ref 3 N6-methyladenosine-induced circ1662 promotes metastasis of colorectal cancer by accelerating YAP1 nuclear localization. Theranostics. 2021 Feb 25;11(9):4298-4315. doi: 10.7150/thno.51342. eCollection 2021.
Ref 4 RNA demethylase ALKBH5 inhibits TGF-Beta-induced EMT by regulating TGF-Beta/SMAD signaling in non-small cell lung?cancer. FASEB J. 2022 May;36(5):e22283. doi: 10.1096/fj.202200005RR.
Ref 5 YTHDF2 Inhibits the Migration and Invasion of Lung Adenocarcinoma by Negatively Regulating the FAM83D-TGFBeta1-SMAD2/3 Pathway. Front Oncol. 2022 Feb 2;12:763341. doi: 10.3389/fonc.2022.763341. eCollection 2022.