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UMI-77

Catalog No. T6034 CAS 518303-20-3

Synonyms: UMI77, UMI 77

UMI-77, a specific Mcl-1 inhibitor (Ki: 490 nM), has selectivity over other members of Bcl-2 family.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

UMI-77, CAS 518303-20-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 51.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 222.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 531.00
200 mg	In stock	$ 768.00
500 mg	In stock	$ 1,150.00
1 mL * 10 mM (in DMSO)	In stock	$ 83.00

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Purity: 99.57%

Purity: 99.24%

Purity: 98.88%

Purity: 98.03%

Purity: 98%

Purity: 97.88%

Purity: 97.6%

Purity: 97.27%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	UMI-77, a specific Mcl-1 inhibitor (Ki: 490 nM), has selectivity over other members of Bcl-2 family.
Targets&IC50	MCL1:490 nM(Ki)
In vitro	UMI-77, administered intravenously at a dose of 60 mg/kg, exhibits single-dose antitumor activity in the BxPC-3 xenograft mouse model without damaging normal tissues.
In vivo	UMI-77 activates the intrinsic apoptosis pathway and/or induces a conformational change in Bax, thereby promoting apoptosis in pancreatic cancer cells. It disrupts the interaction between cell Mcl-1 and BL-Noxa as well as the protein-protein interaction between Mcl-1 and Bax. UMI-77 inhibits the growth of various pancreatic cancer cell lines, including BxPC-3, Panc-1, MiaPaCa-2, AsPC-1, and Capan-2 cells, with IC50 values of 3.4/4.4/12.5/16.1/5.5 μM, respectively.
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	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.(Only for Reference)

Synonyms	UMI77, UMI 77
Molecular Weight	468.34
Formula	C18H14BrNO5S2
CAS No.	518303-20-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 86 mg/mL (183.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 86 mg/mL (183.6 mM)

References and Literature

1. Abulwerdi F, et al. Mol Cancer Ther. 2014, 13(3), 565-575. 2. Cen X, Chen Y, Xu X, et al. Pharmacological targeting of MCL-1 promotes mitophagy and improves disease pathologies in an Alzheimer’s disease mouse model[J]. Nature Communications . 2020, 11(1): 1-13.

Citations

1. Cen X, Chen Y, Xu X, et al. Pharmacological targeting of MCL-1 promotes mitophagy and improves disease pathologies in an Alzheimer’s disease mouse model. Nature Communications. 2020, 11(1): 1-13. 2. Xu Y, Chen Q, Jiang Y, et al.UMI-77 Modulates the Complement Cascade Pathway and Inhibits Inflammatory Factor Storm in Sepsis Based on TMT Proteomics and Inflammation Array Glass Chip.Journal of Proteome Research.2023

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Target-Focused Phenotypic Screening Library Anti-Cancer Compound Library Bioactive Compounds Library Max Bioactive Compound Library PPI Inhibitor Library Apoptosis Compound Library Anti-Aging Compound Library Cuproptosis Compound Library Mitochondria-Targeted Compound Library

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Keywords

UMI-77 518303-20-3 Apoptosis BCL Bcl-2 Family Inhibitor UMI77 UMI 77 inhibit inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.