| Identification | Back Directory | [Name]
UMI-77 | [CAS]
518303-20-3 | [Synonyms]
UMI-77
CS-1799
UMI 77;UMI77
UMI-77 USP/EP/BP
2-((4-(4-Bromophenylsulfonamido)-1-hydroxynaphthalen-2-yl)thio)acetic acid
2-[[4-[[(4-bromophenyl)sulfonyl]amino]-1-hydroxy-2-naphthalenyl]thio]-acetic acid
Acetic acid, 2-[[4-[[(4-bromophenyl)sulfonyl]amino]-1-hydroxy-2-naphthalenyl]thio]-
2-[4-[(4-Bromophenyl)sulfonylamino]-1-hydroxynaphthalen-2-yl]sulfanylacetic acid UMI-77 | [Molecular Formula]
C18H14BrNO5S2 | [MDL Number]
MFCD03471890 | [MOL File]
518303-20-3.mol | [Molecular Weight]
468.34 |
| Chemical Properties | Back Directory | [Boiling point ]
661.2±65.0 °C(Predicted) | [density ]
1.79±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥23.4 mg/mL in DMSO; insoluble in H2O; ≥7.2 mg/mL in EtOH | [form ]
solid | [pka]
2.41±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
UMI-77 acts as a small molecule inhibitor of Mcl-1 which blocks and attenuates pancreatic cell cancer growth. Anticancer agent. | [Biological Activity]
umi-77 is a novel small-molecule inhibitor of mcl-1 with ki and ic50 values of 0.49 μm and 0.31 μm [1].myeloid cell leukemia-1 (mcl-1) is a member of the prosurvival bcl-2 family and is a potent anti-apoptotic protein. mcl-1 acts as an important survival factor in a broad range of human cancers [1].umi-77 is a novel small-molecule mcl-1 inhibitor. in fp-based binding assays, umi-77 potently and selectively displaced fluorescent labeled bid-bh3 peptide from mcl-1 protein with ki value of 0.49μm and bound to the bh3 binding pocket of mcl-1 protein. umi-77 bound to a1/bfl-1, bcl-w, bcl-2 and bcl-xl with ki values of 5.33, 8.19, 23.83 and 32.99μm. in a pull-down assay, umi-77 at 10 μm effectively and dose-dependently inhibited the interactions between bl-noxa and cellular mcl-1. it was reported that mcl-1 regulates pro-apoptotic bax and bak proteins and preventing their pro-apoptotic activity. umi-77 dose-dependently inhibited the binding of mcl-1 to bax with ic50 value of 1.43μm. in pc cells, umi-77 inhibited cell growth and induced apoptosis in a time and dose-dependent way [1].in bxpc-3 xenografted scid mice model, umi-77 exhibited robust anti-tumor efficacy with no toxicity. also, umi-77 decreased the anti-apoptotic protein survivin, which potently inhibited apoptosis by antagonizing caspase activity [1]. | [References]
[1]. abulwerdi f, liao c, liu m, azmi as, et al. a novel small-molecule inhibitor of mcl-1 blocks pancreatic cancer growth in vitro and in vivo. mol cancer ther, 2014, 13(3): 565-575. |
|
|