UMI-77

Catalog No.S7531 Batch:S753103

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Technical Data

Formula

C18H14BrNO5S2
Molecular Weight 468.34 CAS No. 518303-20-3
Solubility (25°C)* In vitro DMSO 93 mg/mL (198.57 mM)
Ethanol 93 mg/mL (198.57 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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]
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]

Protocol (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    ICR-SCID mice bearing BxPC-3 tumor xenograft

  • Dosages

    ~60 mg/kg daily

  • Administration

    i.v.

Customer Product Validation

, , Mol Cell Biochem, 2017, 432(1-2):55-65

Data from [Data independently produced by , , Nat Commun, 2016, 7:10538]

Data from [Data independently produced by , , BMC Cancer, 2017, 17(1):449]

Selleck's UMI-77 has been cited by 22 publications

Therapy-induced normal tissue damage promotes breast cancer metastasis [ iScience, 2024, 27(1):108503] PubMed: 38161426
Deregulation and epigenetic modification of BCL2-family genes cause resistance to venetoclax in hematologic malignancies [ Blood, 2022, blood.2021014304] PubMed: 35704690
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] PubMed: 36266272
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] PubMed: 36266272
AXL/MERTK inhibitor ONO-7475 potently synergizes with venetoclax and overcomes venetoclax resistance to kill FLT3-ITD acute myeloid leukemia [ Haematologica, 2021, 10.3324/haematol.2021.278369] PubMed: 34732043
Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2 [ Cell Chem Biol, 2021, S2451-9456(21)00213-0] PubMed: 33979649
Mesothelioma Cells Depend on the Antiapoptotic Protein Bcl-xL for Survival and Are Sensitized to Ionizing Radiation by BH3-Mimetics. [ Int J Radiat Oncol Biol Phys, 2020, 15;106(4):867-877] PubMed: 31786278
Targeting the Synthetic Vulnerability of PTEN-Deficient Glioblastoma Cells with MCL1 Inhibitors [ Mol Cancer Ther, 2020, 19(10):2001-2011] PubMed: 32737157
AT101 [(-)-Gossypol] Selectively Inhibits MCL1 and Sensitizes Carcinoma to BH3 Mimetics by Inducing and Stabilizing NOXA [ Cancers (Basel), 2020, 12(8):E2298] PubMed: 32824203
Alveolar Macrophage Apoptosis-associated Bacterial Killing Helps Prevent Murine Pneumonia. [ Am J Respir Crit Care Med, 2019, 200(1):84-97] PubMed: 30649895

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.