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HomeProduct name listUMI-77

UMI-77

UMI-77 Structural

What is UMI-77?

The Uses of UMI-77

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.

Properties of UMI-77

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

Safety information for UMI-77

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for UMI-77

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