Home Apoptosis Bcl-2 inhibitor UMI-77 For research use only.

UMI-77

UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.

UMI-77 Chemical Structure

UMI-77 Chemical Structure

CAS No. 518303-20-3

Purity & Quality Control

UMI-77 Related Products

Signaling Pathway

Bcl-2 Signaling Pathways

Bcl-2 Signaling Pathway

Biological Activity

Description UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
Targets
Mcl-1 [1]
(Cell-free assay)
490 nM(Ki)
In vitro
In vitro UMI-77 effectively disrupts the interactions between BL-Noxa and cellular Mcl-1, as well as Mcl-1/Bax protein–protein interactions. [1] 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. [1]
Kinase Assay 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.
Cell Research Cell lines Human pancreatic cancer cell lines AsPC-1, BxPC-3, Panc-1, MiaPaCa and Capan-2
Concentrations ~100 μM
Incubation Time 4 days
Method

Human pancreatic cancer cell lines AsPC-1, BxPC-3, and Capan-2 are cultured in RPMI-1640 medium, whereas Panc-1 and MiaPaCa are cultured in Dulbeccos' Modified Eagle's Medium (DMEM), all supplemented with 10% FBS. The cell growth inhibition after treatment with increasing concentrations of the compounds is determined by WST-8 assay.
In Vivo
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. [1]
Animal Research Animal Models ICR-SCID mice bearing BxPC-3 tumor xenograft
Dosages ~60 mg/kg daily
Administration i.v.

Chemical Information & Solubility

Molecular Weight 468.34 Formula

C18H14BrNO5S2
CAS No. 518303-20-3 SDF Download UMI-77 SDF
Smiles C1=CC=C2C(=C1)C(=CC(=C2O)SCC(=O)O)NS(=O)(=O)C3=CC=C(C=C3)Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 93 mg/mL ( (198.57 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 93 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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