m6A-centered Drug Response Information

General Information of the Drug (ID: M6ADRUG0056)
Name
JQ-1
Synonyms
1268524-70-4; (+)-JQ-1; JQ1 compound; (+)-JQ1; JQ-1; UNII-1MRH0IMX0W; (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-triMethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate; (S)-JQ1; 1MRH0IMX0W; JQ1; CHEMBL1957266; AK109409; (S)-(+)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate; (S)-(+)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-6-yl)acetate; (S)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3
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Status Phase 1 [1]
Structure
Formula
C23H25ClN4O2S
InChI
InChI=1S/C23H25ClN4O2S/c1-12-13(2)31-22-19(12)20(15-7-9-16(24)10-8-15)25-17(11-18(29)30-23(4,5)6)21-27-26-14(3)28(21)22/h7-10,17H,11H2,1-6H3/t17-/m0/s1
InChIKey
DNVXATUJJDPFDM-KRWDZBQOSA-N
PubChem CID
46907787
TTD Drug ID
D0ZW4W
Full List of m6A Targets Related to This Drug
Metastasis associated lung adenocarcinoma transcript 1 (MALAT1)
 Target Info 
In total 1 item(s) under this target gene
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene [2]
Response Summary This study highlighted METTL3 as a tumor promoter in Thymic tumors and c-MYC as a promising target to be exploited for the treatment of TET. High expression of c-MYC protein is enabled by lncRNA Metastasis associated lung adenocarcinoma transcript 1 (MALAT1), which is methylated and delocalized by METTL3. Silencing of METTL3 combined with cisplatin or c-MYC inhibitor induces cell death in TET cells. Blocking of c-MYC by using JQ1 inhibitor cooperates with METTL3 depletion in the inhibition of proliferation and induction of cell death.
Responsed Disease Thymic epithelial tumors ICD-11: 2C27.Y
 Disease Info 
Target Regulator Methyltransferase-like 3 (METTL3) WRITER
 Regulator Info 
Target Regulation Up regulation
Pathway Response Cellular senescence hsa04218
Cell Process Cell viability and proliferation
In-vitro Model T1889 Thymic undifferentiated carcinoma Homo sapiens CVCL_D024
References
Ref 1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 2 METTL3-dependent MALAT1 delocalization drives c-Myc induction in thymic epithelial tumors. Clin Epigenetics. 2021 Sep 16;13(1):173. doi: 10.1186/s13148-021-01159-6.