Molecular Weight(MW): 468.34
UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
2 Customer Reviews
MCL-1 pharmacological inhibitor UMI-77 induces apoptosis of ESCC cells. a, b KYSE150 (a) and KYSE510 (b) cells were starved in 0.1% FBS/RPMI 1640 medium overnight and then cultured without (DMSO) or with different concentrations of UMI-77 in 10% FBS/RPMI 1640 medium for 48 h. After treatment, attached and floating cells were harvested. Cleavage of caspase-3 and PARP were analyzed by Western blotting. β-actin was used as a loading control. c KYSE150 and KYSE510 cells were starved in 0.1% FBS/RPMI 1640 medium overnight and then cultured without (DMSO) or with 10 μM UMI-77 in 10% FBS/RPMI 1640 medium for 48 h. After treatment, attached and floating cells were harvested. Cleavage of PARP was analyzed by Western blotting. β-actin was used as a loading control. Arrow head: 17KD or 19 KD of cleaved caspase-3
BMC Cancer, 2017, 17(1):449. UMI-77 purchased from Selleck.
Purity & Quality Control
Choose Selective Bcl-2 Inhibitors
|Description||UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.|
UMI-77 effectively disrupts the interactions between BL-Noxa and cellular Mcl-1, as well as Mcl-1/Bax protein–protein interactions.  UMI-77 inhibits growth of pancreatic cancer cells with IC50 of 3.4, 4.4, 12.5, 16.1, and 5.5 μM for BxPC-3, Panc-1, MiaPaCa-2, AsPC-1 and Capan-2 cells, respectively. UMI-77 induced apoptosis in pancreatic cancer through activation of the intrinsic apoptotic pathway and/or Bax conformational change. 
|In vivo||In a BxPC-3 xenograft mouse model, UMI-77 (60 mg/kg i.v.) exhibits single-agent antitumor activity without any damage normal tissues. |
Fluorescence polarization (FP)-based binding assays:Based on the Kd values, the concentrations of the proteins used in the competitive binding experiments are 90 nM for Mcl-1, 40 nM for Bcl-w, 50 nM for Bcl-xL, 60 nM for Bcl-2, and 4 nM for A1/Bfl-1. The fluorescent probes, Flu-BID and FAM-BID are fixed at 2 nM for all assays except for A1/Bfl-1 where FAMBID is used at 1 nM. 5 μL of the tested compound in DMSO and 120 μL of protein/probe complex in the assay buffer (100 mM potassium phosphate, pH 7.5; 100 μg/ml bovine gamma globulin; 0.02% sodium azide) are added to assay plates (Microfluor 2Black), incubated at room temperature for 3 h and the polarization values (mP) are measured at an excitation wavelength at 485 nm and an emission wavelength at 530 nm using the plate reader Synergy H1Hybrid. IC50 values are determined by nonlinear regression fitting of the competition curves.
|In vitro||DMSO||93 mg/mL (198.57 mM)|
|Ethanol||93 mg/mL warmed (198.57 mM)|
|In vivo||Add solvents individually and in order:
5% DMSO+30% PEG 300+dd H2O
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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