MT1

Names

[ CAS No. ]:
2060573-82-0

[ Name ]:
MT1

Biological Activity

[Description]:

MT1 is a bivalent chemical probe of BET bromodomains, with an IC50 of 0.789 nM for BRD4(1)[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[In Vitro]

MT1 (100 nM, 24 h) significantly induces apoptosis via caspase-3 and PARP in MV4;11 cells[1]. Western Blot Analysis[1] Cell Line: MV4;11 cells[1]. Concentration: 100 nM. Incubation Time: 24 h. Result: Significant apoptosis was observed by caspase-3 and PARP cleavage after treatment.

[In Vivo]

MT1 (44.2 and 22.1 µmol/kg, ip daily, for 14 days) significantly delayed leukemia progression in mice (Mus musculus) compared to JQ1[1]. MT1 exhibits terminal t1/2 of 2.70 h in mice[1]. Animal Model: Leukemia xenograft models[1]. Dosage: 44.2 and 22.1 µmol/kg. Administration: Intraperitoneally for 14 subsequent days. Result: Significantly reduced leukemic burden over the course of the study compared to either vehicle or JQ1.

[References]

[1]. Minoru Tanaka, et al. Design and characterization of bivalent BET inhibitors. Nat Chem Biol. 2016 Dec;12(12):1089-1096.

Chemical & Physical Properties

[ Molecular Formula ]:
C₅₄H₆₆Cl₂N₁₀O₉S₂

[ Molecular Weight ]:
1134.20

Related Compounds

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