General Information of the Drug (ID: M6APDG00048)
Name
AS-601245
Synonyms
JNK Inhibitor V; SAPK Inhibitor V; 1,3-Benzothiazol-2-yl-(2-((2-(3-pyridinyl)ethyl)amino)-4-pyrimidinyl)acetonitrile; GTPL5997; SCHEMBL12242792; MolPort-044-724-552; HMS3229I20; CCG-206858; RT-013405; J-019673
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Status
Investigative
Structure
Formula
C20H16N6S
InChI
1S/C20H16N6S/c21-12-15(19-25-17-5-1-2-6-18(17)27-19)16-8-11-24-20(26-16)23-10-7-14-4-3-9-22-13-14/h1-6,8-9,11,13,15H,7,10H2,(H,23,24,26)
InChIKey
RCYPVQCPYKNSTG-UHFFFAOYSA-N
PubChem CID
10109823
TTD Drug ID
D04QCF
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.
Glycogen synthase kinase-3 beta (GSK-3B)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Glycogen synthase kinase-3 beta (GSK-3B) is a therapeutic target for AS-601245. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of AS-601245 through regulating the expression of Glycogen synthase kinase-3 beta (GSK-3B). [1], [2]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Glycogen synthase kinase-3 beta (GSK-3B) is a therapeutic target for AS-601245. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of AS-601245 through regulating the expression of Glycogen synthase kinase-3 beta (GSK-3B). [2], [3]
Stress-activated protein kinase JNK1 (JNK1)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Stress-activated protein kinase JNK1 (JNK1) is a therapeutic target for AS-601245. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of AS-601245 through regulating the expression of Stress-activated protein kinase JNK1 (JNK1). [4], [5]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary Stress-activated protein kinase JNK1 (JNK1) is a therapeutic target for AS-601245. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of AS-601245 through regulating the expression of Stress-activated protein kinase JNK1 (JNK1). [5], [6]
References
Ref 1 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 2 Novel GSK-3beta inhibitors from sequential virtual screening. Bioorg Med Chem. 2008 Jan 15;16(2):636-43. doi: 10.1016/j.bmc.2007.10.047. Epub 2007 Oct 22.
Ref 3 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.
Ref 4 METTL3 regulates alternative splicing of MyD88 upon the lipopolysaccharide-induced inflammatory response in human dental pulp cells. J Cell Mol Med. 2018 May;22(5):2558-2568. doi: 10.1111/jcmm.13491. Epub 2018 Mar 4.
Ref 5 Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies. Bioorg Med Chem Lett. 2007 Feb 1;17(3):668-72. doi: 10.1016/j.bmcl.2006.10.093. Epub 2006 Nov 2.
Ref 6 Post-translational modification of RNA m6A demethylase ALKBH5 regulates ROS-induced DNA damage response. Nucleic Acids Res. 2021 Jun 4;49(10):5779-5797. doi: 10.1093/nar/gkab415.