m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02709)
Name
AZAKENPAULLONE
Synonyms
1-Azakenpaullone; 676596-65-9; azakenpaullone; 9-bromo-7,12-dihydropyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one; C15H10BrN3O; Kinome_3492; 1-AKP; SCHEMBL378920; GTPL8018; CHEMBL336961; BDBM7497; DTXSID8042686; NOCAS_42686; CTK8F0375; MolPort-003-844-675; CHEBI:131490; HMS3653A17; HMS3229B07; BCP21061; ZINC13588927; s7193; 2138AH; 1-Azakenpaullone, > AKOS030240424; SB19270; TRA0006688; NCGC00386322-01; RT-006179; FT-0662368; SW220021-1; KS-00001866
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Status
Investigative
Structure
Formula
C15H10BrN3O
InChI
1S/C15H10BrN3O/c16-8-3-4-11-9(6-8)10-7-13(20)18-12-2-1-5-17-15(12)14(10)19-11/h1-6,19H,7H2,(H,18,20)
InChIKey
NTSBZVCEIVPKBJ-UHFFFAOYSA-N
PubChem CID
6538897
TTD Drug ID
D0DR8N
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.
Cyclin-dependent kinase 1 (CDK1)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 1 (CDK1) is a therapeutic target for AZAKENPAULLONE. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of AZAKENPAULLONE through regulating the expression of Cyclin-dependent kinase 1 (CDK1). [1], [2]
Protein virilizer homolog (VIRMA)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 1 (CDK1) is a therapeutic target for AZAKENPAULLONE. The Protein virilizer homolog (VIRMA) has potential in affecting the response of AZAKENPAULLONE through regulating the expression of Cyclin-dependent kinase 1 (CDK1). [2], [3]
Glycogen synthase kinase-3 beta (GSK-3B)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Glycogen synthase kinase-3 beta (GSK-3B) is a therapeutic target for AZAKENPAULLONE. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of AZAKENPAULLONE through regulating the expression of Glycogen synthase kinase-3 beta (GSK-3B). [2], [4]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Glycogen synthase kinase-3 beta (GSK-3B) is a therapeutic target for AZAKENPAULLONE. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of AZAKENPAULLONE through regulating the expression of Glycogen synthase kinase-3 beta (GSK-3B). [2], [5]
References
Ref 1 CircMETTL3, upregulated in a m6A-dependent manner, promotes breast cancer progression. Int J Biol Sci. 2021 Mar 15;17(5):1178-1190. doi: 10.7150/ijbs.57783. eCollection 2021.
Ref 2 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6. doi: 10.1016/j.bmcl.2003.10.062.
Ref 3 KIAA1429 acts as an oncogenic factor in breast cancer by regulating CDK1 in an N6-methyladenosine-independent manner. Oncogene. 2019 Aug;38(33):6123-6141. doi: 10.1038/s41388-019-0861-z. Epub 2019 Jul 8.
Ref 4 Vascular Smooth Muscle FTO Promotes Aortic Dissecting Aneurysms via m6A Modification of Klf5. Front Cardiovasc Med. 2020 Nov 20;7:592550. doi: 10.3389/fcvm.2020.592550. eCollection 2020.
Ref 5 N6-methyladenosine regulated FGFR4 attenuates ferroptotic cell death in recalcitrant HER2-positive breast cancer. Nat Commun. 2022 May 13;13(1):2672. doi: 10.1038/s41467-022-30217-7.