General Information of the Drug (ID: M6APDG02349)
Name
AG490
Synonyms
(E)-N-Benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide; 133550-30-8; AG-490; Tyrphostin B42; Tyrphostin AG 490; AG 490; (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide; Tyrphostin AG490; tyrphostin AG-490; AG-490 (Tyrphostin B42); alpha-Cyano-(3,4-dihydroxy)-N-benzylcinnamide; N-Benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide; 134036-52-5; (2E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide; CHEMBL56543; (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide; (2E)-2-CYANO-3-(3,4-DIHYDROXYPHENYL)-N-(PHENYLMETHYL)-2-PROPENAMIDE; SMR001230665
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Status
Terminated
Structure
Formula
C17H14N2O3
InChI
1S/C17H14N2O3/c18-10-14(8-13-6-7-15(20)16(21)9-13)17(22)19-11-12-4-2-1-3-5-12/h1-9,20-21H,11H2,(H,19,22)/b14-8+
InChIKey
TUCIOBMMDDOEMM-RIYZIHGNSA-N
PubChem CID
5328779
TTD Drug ID
D0GZ7B
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.
Janus kinase 2 (JAK-2)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for AG490. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of AG490 through regulating the expression of Janus kinase 2 (JAK-2). [1], [2]
Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1)
In total 1 mechanisms lead to this potential drug response
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for AG490. The Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1) has potential in affecting the response of AG490 through regulating the expression of Janus kinase 2 (JAK-2). [2], [3]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for AG490. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of AG490 through regulating the expression of Janus kinase 2 (JAK-2). [2], [3]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for AG490. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of AG490 through regulating the expression of Janus kinase 2 (JAK-2). [2], [4]
Janus kinase 3 (JAK-3)
Wilms tumor 1-associating protein (WTAP)
In total 1 mechanisms lead to this potential drug response
Response Summary Janus kinase 3 (JAK-3) is a therapeutic target for AG490. The Wilms tumor 1-associating protein (WTAP) has potential in affecting the response of AG490 through regulating the expression of Janus kinase 3 (JAK-3). [5], [6]
References
Ref 1 FTO inhibits UPR(mt)-induced apoptosis by activating JAK2/STAT3 pathway and reducing m6A level in adipocytes. Apoptosis. 2021 Aug;26(7-8):474-487. doi: 10.1007/s10495-021-01683-z. Epub 2021 Jul 1.
Ref 2 Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77. doi: 10.1517/13543784.2014.918604. Epub 2014 May 12.
Ref 3 N6-Methyladenosine Methyltransferase METTL3 Promotes Angiogenesis and Atherosclerosis by Upregulating the JAK2/STAT3 Pathway via m6A Reader IGF2BP1. Front Cell Dev Biol. 2021 Dec 7;9:731810. doi: 10.3389/fcell.2021.731810. eCollection 2021.
Ref 4 ALKBH5-HOXA10 loop-mediated JAK2 m6A demethylation and cisplatin resistance in epithelial ovarian cancer. J Exp Clin Cancer Res. 2021 Sep 8;40(1):284. doi: 10.1186/s13046-021-02088-1.
Ref 5 Transcriptome-Wide High-Throughput m6A Sequencing of Differential m6A Methylation Patterns in the Human Rheumatoid Arthritis Fibroblast-Like Synoviocytes Cell Line MH7A. J Inflamm Res. 2021 Feb 25;14:575-586. doi: 10.2147/JIR.S296006. eCollection 2021.
Ref 6 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)