Synthetic Alpha-Bromo-2′,3,4,4′-Tetramethoxychalcone (Alpha-Br-TMC) Inhibits the JAK/STAT Signaling Pathway

IL-3 binding to the α/βc chains of the IL-3 receptor leads to activation of the receptor-associated JAK2 tyrosine kinase by trans-phosphorylation. In turn, JAK2-mediated activation of the STAT5, MAPK and AKT pathways via phosphorylation (broad arrows) results in induced transcription of downstream target genes (thin arrows). We showed that α-Br-TMC inhibits JAK2 phosphorylation, hence impairing JAK2-regulated signaling pathways. In addition and independently of JAK2, α-Br-TMC inhibits STAT5 activity. Concomitantly, STAT5A and STAT5B protein mobility in SDS-PAGE is altered, indicating a change in their post-translational modification state induced by α-Br-TMC, which might be associated to STAT5 altered transcriptional activity.
Synthetic Alpha-Bromo-2′,3,4,4′-Tetramethoxychalcone (Alpha-Br-TMC) Inhibits the JAK/STAT Signaling Pathway
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The Synthetic α-Bromo-2′,3,4,4′-Tetramethoxychalcone (α-Br-TMC) Inhibits the JAK/STAT Signaling Pathway. (2014) Sophia Pinz, et al. PLoS One. 2014;9(3):e90275. Figure: F7.

Gene mentions


Organism Group Word Match Source NCBI Symbol NCBI ID
Bos taurus Mammals IL-3 IL3 ncbigene_symbol IL3 280823
Bos taurus Mammals JAK2 JAK2 ncbigene_symbol JAK2 525246
Bos taurus Mammals AKT AKT ncbigene_synonym AKT1 280991
Bos taurus Mammals c-Fos FOS ncbigene_symbol FOS 280795
Bos taurus Mammals JunB JUNB ncbigene_symbol JUNB 514246
Bos taurus Mammals Osm OSM ncbigene_symbol OSM 319086
Bos taurus Mammals C-Myc MYC ncbigene_symbol MYC 511077
Mus musculus Rodents IL-3 IL-3 ncbigene_synonym Il3 16187
Mus musculus Rodents JAK2 JAK2 ncbigene_symbol Jak2 16452
Mus musculus Rodents Br BR ncbigene_symbol Br 103946
Mus musculus Rodents AKT AKT ncbigene_synonym Akt1 11651
Mus musculus Rodents STAT5 STAT5 ncbigene_synonym Stat5a 20850
Mus musculus Rodents c-Fos C-FOS ncbigene_synonym Fos 14281
Mus musculus Rodents Cis CIS ncbigene_synonym Cish 12700
Mus musculus Rodents Cis CIS ncbigene_synonym Cs 12974
Mus musculus Rodents JunB JUNB ncbigene_symbol Junb 16477
Mus musculus Rodents Osm OSM ncbigene_symbol Osm 18413
Mus musculus Rodents C-Myc MYC ncbigene_symbol Myc 17869
Mus musculus Rodents C-Myc MYC ncbigene_synonym Nol3 78688
Oryctolagus cuniculus Mammals JAK2 JAK2 ncbigene_symbol JAK2 100358134
Oryctolagus cuniculus Mammals c-Fos FOS ncbigene_symbol FOS 100338345
Oryctolagus cuniculus Mammals JunB JUNB ncbigene_symbol JUNB 127488466
Oryctolagus cuniculus Mammals Osm OSM ncbigene_symbol OSM 100342491
Oryctolagus cuniculus Mammals C-Myc C-MYC ncbigene_synonym MYC 100327265
Homo sapiens Primates IL-3 IL-3 ncbigene_synonym IL3 3562
Homo sapiens Primates JAK2 JAK2 ncbigene_symbol JAK2 3717
Homo sapiens Primates MAPK MAPK famplex_relations MAPK1 5594
Homo sapiens Primates MAPK MAPK famplex_relations MAPK3 5595
Homo sapiens Primates MAPK MAPK famplex_relations MAPK11 5600
Homo sapiens Primates MAPK MAPK famplex_relations MAPK12 6300
Homo sapiens Primates MAPK MAPK famplex_relations MAPK13 5603
Homo sapiens Primates MAPK MAPK famplex_relations MAPK14 1432
Homo sapiens Primates MAPK MAPK famplex_relations MAPK8 5599
Homo sapiens Primates MAPK MAPK famplex_relations MAPK9 5601
Homo sapiens Primates MAPK MAPK famplex_relations MAPK10 5602
Homo sapiens Primates AKT AKT ncbigene_synonym AKT1 207
Homo sapiens Primates AKT AKT famplex_relations AKT2 208
Homo sapiens Primates AKT AKT famplex_relations AKT3 10000
Homo sapiens Primates STAT5 STAT5 ncbigene_synonym STAT5A 6776
Homo sapiens Primates STAT5 STAT5 ncbigene_synonym STAT5B 6777
Homo sapiens Primates c-Fos C-FOS ncbigene_synonym FOS 2353
Homo sapiens Primates Cis CIS ncbigene_synonym CISH 1154
Homo sapiens Primates JunB JUNB ncbigene_symbol JUNB 3726
Homo sapiens Primates JunB JUNB ncbigene_synonym RNASEH2A 10535
Homo sapiens Primates Osm OSM ncbigene_symbol OSM 5008
Homo sapiens Primates Osm OSM ncbigene_synonym CCM2 83605
Homo sapiens Primates C-Myc C-MYC ncbigene_synonym MYC 4609
Drosophila melanogaster Invertebrates Br BR ncbigene_symbol br 44505
Drosophila melanogaster Invertebrates MAPK MAPK ncbigene_synonym MKP-4 32963
Drosophila melanogaster Invertebrates MAPK MAPK ncbigene_synonym p38b 34780
Drosophila melanogaster Invertebrates MAPK MAPK ncbigene_synonym rl 3354888
Drosophila melanogaster Invertebrates AKT AKT ncbigene_symbol Akt 41957
Drosophila melanogaster Invertebrates c-Fos C-FOS ncbigene_synonym kay 3772082
Drosophila melanogaster Invertebrates C-Myc C-MYC ncbigene_synonym Myc 31310

Chemical mentions

Word Match MeSH Name ChEBI

Disease mentions

Word Match MeSH Name DOID
Cancer NA