OTX015

OTX015

CAT N°: 15947
Price:

From 74.00 62.90

The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).{25844} It displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias, downregulating c-Myc expression and inducing cell cycle arrest and apoptosis.{25844,25845,25843} At 100 mg/kg, OTX015 has been shown to inhibit the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79%.{25844}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • (6S)-4-(4-chlorophenyl)-N-(4-hydroxyphenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
  • Correlated keywords
    • epigenetics bromodomains BETs inhibitors inhibits inhibitions BRD2 BRD3 BRD4 anticancer anti-cancer anti cancers leukemia antiproliferation anti-proliferation oral orally bioavailable small molecules BRDs BRD-2 BRD-3 BRD-4 sub-micromolar ranges submicromolor tumors genes regulations histones modifications chromatin research OTX-015 OTXs 015 extra terminal domains antiproliferative carcinomas HY15743 HY 15743
  • Product Overview:
    The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).{25844} It displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias, downregulating c-Myc expression and inducing cell cycle arrest and apoptosis.{25844,25845,25843} At 100 mg/kg, OTX015 has been shown to inhibit the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79%.{25844}

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