m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG00559)
Name
H3B-6545
Synonyms
EX-A2942; H3B-6545; HY-112596;2052130-80-8; CS-0047714; SCHEMBL18261010
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Status
Phase 1
Structure
Formula
C30H29F4N5O2
InChI
1S/C30H29F4N5O2/c1-39(2)27(40)9-6-14-35-15-16-41-26-13-11-22(19-36-26)28(21-10-12-25-23(17-21)29(31)38-37-25)24(18-30(32,33)34)20-7-4-3-5-8-20/h3-13,17,19,35H,14-16,18H2,1-2H3,(H,37,38)/b9-6+,28-24-
InChIKey
JPFTZIJTXCHJNE-HMOQVRKWSA-N
PubChem CID
124091040
INTEDE Drug ID
DR1799
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.
Cytochrome P450 2C8 (CYP2C8)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for H3B-6545. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of H3B-6545 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for H3B-6545. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of H3B-6545 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for H3B-6545. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of H3B-6545 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for H3B-6545. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of H3B-6545 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
References
Ref 1 Methylation of adenosine at the N(6) position post-transcriptionally regulates hepatic P450s expression. Biochem Pharmacol. 2020 Jan;171:113697. doi: 10.1016/j.bcp.2019.113697. Epub 2019 Nov 7.
Ref 2 Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novel selective ERAlpha covalent antagonist (SERCA). Cancer Chemother Pharmacol. 2019 Jan;83(1):151-160. doi: 10.1007/s00280-018-3716-3. Epub 2018 Nov 1.