General Information of the Drug (ID: M6APDG00711)
Name
NT219
Synonyms
UNII-K1WT1A1UP5; K1WT1A1UP5; 1198078-60-2; (E)-3-(2-Bromo-3,4-dihydroxyphenyl)-N-(3,4,5-trihydroxybenzyl)prop-2-enethioamide; CHEMBL3679680; SCHEMBL12659248; BDBM101913; NT-219; US8536227, 5; 2-Propenethioamide, 3-(2-bromo-3,4-dihydroxyphenyl)-N-((3,4,5-trihydroxyphenyl)methyl)-; 2-Propenethioamide, 3-(2-bromo-3,4-dihydroxyphenyl)-N-((3,4,5-trihydroxyphenyl)methyl)-, (2E)-
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Status
Phase 1/2
Structure
Formula
C16H14BrNO5S
InChI
1S/C16H14BrNO5S/c17-14-9(1-3-10(19)16(14)23)2-4-13(24)18-7-8-5-11(20)15(22)12(21)6-8/h1-6,19-23H,7H2,(H,18,24)/b4-2+
InChIKey
XDDQKKXXQHUUHJ-DUXPYHPUSA-N
PubChem CID
135914977
TTD Drug ID
DUI59O
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.
Insulin receptor substrate-1 (IRS1)
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
Response Summary Insulin receptor substrate-1 (IRS1) is a therapeutic target for NT219. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of NT219 through regulating the expression of Insulin receptor substrate-1 (IRS1). [1], [2]
Signal transducer and activator of transcription 3 (STAT3)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Signal transducer and activator of transcription 3 (STAT3) is a therapeutic target for NT219. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of NT219 through regulating the expression of Signal transducer and activator of transcription 3 (STAT3). [3], [4]
Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1)
In total 1 mechanisms lead to this potential drug response
Response Summary Signal transducer and activator of transcription 3 (STAT3) is a therapeutic target for NT219. The Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1) has potential in affecting the response of NT219 through regulating the expression of Signal transducer and activator of transcription 3 (STAT3). [4], [5]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Signal transducer and activator of transcription 3 (STAT3) is a therapeutic target for NT219. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of NT219 through regulating the expression of Signal transducer and activator of transcription 3 (STAT3). [4], [5]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary Signal transducer and activator of transcription 3 (STAT3) is a therapeutic target for NT219. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of NT219 through regulating the expression of Signal transducer and activator of transcription 3 (STAT3). [4], [6]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
Response Summary Signal transducer and activator of transcription 3 (STAT3) is a therapeutic target for NT219. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of NT219 through regulating the expression of Signal transducer and activator of transcription 3 (STAT3). [4], [6]
References
Ref 1 YTHDF2 inhibit the tumorigenicity of endometrial cancer via downregulating the expression of IRS1 methylated with m(6)A. J Cancer. 2021 May 5;12(13):3809-3818. doi: 10.7150/jca.54527. eCollection 2021.
Ref 2 APR-246/PRIMA-1MET inhibits thioredoxin reductase 1 and converts the enzyme to a dedicated NADPH oxidase. Cell Death Dis. 2013 Oct 24;4(10):e881. doi: 10.1038/cddis.2013.417.
Ref 3 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 4 National Cancer Institute Drug Dictionary (drug id 617379).
Ref 5 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 6 ALKBH5 regulates STAT3 activity to affect the proliferation and tumorigenicity of osteosarcoma via an m6A-YTHDF2-dependent manner. EBioMedicine. 2022 Jun;80:104019. doi: 10.1016/j.ebiom.2022.104019. Epub 2022 Apr 28.