2. Apoptosis
  3. Bcl-2 Family
  4. UMI-77

UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.

For research use only. We do not sell to patients.

CAS No. : 518303-20-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of UMI-77:

UMI-77 Related Antibodies

Top Publications Citing Use of Products

    UMI-77 purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2022 Oct 7;22(1):304.  [Abstract]

    UMI-77 (10 μM, 24 h) activated the expression of mitophagyrelated proteins suppressed by cirsiliol, including PINK1, Parkin, BNIP3, and FUNDC1 by western blot analysis.

    UMI-77 purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2022 Oct 7;22(1):304.  [Abstract]

    UMI-77 (10 μM) relieved ∆Ψm loss caused by cirsiliol. Representative images of JC-1 staining.

    View All Bcl-2 Family Isoform Specific Products:

    View All Isoforms
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.

    IC50 & Target[1]

    Mcl-1

    0.49 μM (Ki)

    Bfl-1

    5.33 μM (Ki)

    Bcl-W

    8.19 μM (Ki)

    Bcl-2

    23.83 μM (Ki)

    Bcl-xL

    32.99 μM (Ki)

    Cellular Effect
    Cell Line Type Value Description References
    HL-60 IC50
    3.13 μM
    Compound: 10
    Cytotoxicity against human HL60 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
    Cytotoxicity against human HL60 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
    		[PMID: 24749893]
    HepG2 IC50
    11.37 μM
    Compound: UMI-77
    Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay
    		[PMID: 32088497]
    Jurkat IC50
    9.79 μM
    Compound: UMI-77
    Antiproliferative activity against human Jurkat cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human Jurkat cells incubated for 72 hrs by MTT assay
    		[PMID: 32088497]
    K562 IC50
    15.11 μM
    Compound: 10
    Cytotoxicity against human K562 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
    Cytotoxicity against human K562 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
    		[PMID: 24749893]
    MOLT-4 IC50
    3.14 μM
    Compound: UMI-77
    Antiproliferative activity against human MOLT-4 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MOLT-4 cells incubated for 72 hrs by MTT assay
    		[PMID: 32088497]
    MV4-11 IC50
    10.87 μM
    Compound: 10
    Cytotoxicity against human MV4-11 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
    Cytotoxicity against human MV4-11 cells assessed as intracellular ATP level after 3 days by CellTiterGlo assay
    		[PMID: 24749893]
    NCI-H1299 IC50
    6.08 μM
    Compound: UMI-77
    Antiproliferative activity against human NCI-H1299 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1299 cells incubated for 72 hrs by MTT assay
    		[PMID: 32088497]
    PC-3 IC50
    8.43 μM
    Compound: UMI-77
    Antiproliferative activity against human PC-3 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human PC-3 cells incubated for 72 hrs by MTT assay
    		[PMID: 32088497]
    RPMI-8226 IC50
    5.77 μM
    Compound: UMI-77
    Antiproliferative activity against human RPMI-8226 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human RPMI-8226 cells incubated for 72 hrs by MTT assay
    		[PMID: 32088497]
    In Vitro

    Competitive binding curve of UMI-77 against Mcl-1 is obtained by FP based binding assay using fluorescent labeled Bid BH3 peptide with an IC50 of 1.87±0.22 μM. UMI-77 potently inhibits the cell growth of BxPC-3 and Panc-1 cell lines with IC50 values of 3.4 μM and 4.4 μM respectively, and shows 3 to 5 times less potency in inhibition of the cell growth of two other tested cell lines MiaPaCa-2 (12.5 μM) and AsPC-1 (16.1 μM). The cell growth inhibition potency of UMI-77 correlates with the highest expression of Mcl-1 and Bak, and lowest expression of Bcl-xL in the sensitive cell lines, BxPC-3 and Panc-1. Capan-2 cells are showing similar sensitivity to UMI-77 (IC50 of 5.5 μM) as BxPC-3 and Panc-1, although has low Mcl-1 levels[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    UMI-77 Related Antibodies
    In Vivo

    UMI-77 exhibits moderate metabolic stability with a half-life of 45 minutes.The maximum tolerated dose (MTD) of UMI-77 in SCID mice is determined. Administered 60 mg/kg i.v. for 5 consecutive days per week for two weeks does not cause any loss in the animal weight and there is no obvious sign of toxicity during the course of the treatment. Increasing the dose to 80 mg/kg show severe animal weight loss (>20%), therefore 60 mg/kg is used as a therapeutic dose for the in vivo efficacy studies. Daily treatment with UMI-77 for 5 consecutive days a week for two weeks results in statistically significant tumor growth inhibition by 65% and 56% in comparison with the controls in day 19 (p<0.0001) and day 22 (p<0.003) respectively[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    468.34

    Formula

    C18H14BrNO5S2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)CSC1=CC(NS(=O)(C2=CC=C(Br)C=C2)=O)=C3C=CC=CC3=C1O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 28 mg/mL (59.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1352 mL 10.6760 mL 21.3520 mL
    5 mM 0.4270 mL 2.1352 mL 4.2704 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.34 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.66%

    SDS (393 KB)

    COA (258 KB) HNMR (312 KB) RP-HPLC (127 KB) MS (82 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Human PC cell lines AsPC-1, BxPC-3 and Capan-2 are cultured in RPMI 1640 medium, while Panc-1 and MiaPaCa are cultured in DMEM medium, all supplemented with 10% fetal bovine serum. The cell growth inhibition after treatment with increasing concentrations of the compounds (e.g., UMI-77; 1,10, and 100 μM) is determined by WST-8 assay[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    For BxPC-3 subcutaneous model, 10×106 cells are subcutaneously injected into the flanks of 4-5 week old female severe combined immune deficient mice (ICR-SCID). Palpable tumors start to appear in 3-5 weeks. Tumors are measured twice weekly. To prevent any pain or discomfort, mice are euthanized and their tumors remove once they reach ~1800 mg burden. Tumors are then dissected into 50 mg pieces and re-transplanted into naïve ICR-SCID for serial propagation. Animals are treated with either vehicle or UMI-77 given i.v. (60 mg/kg) on day three post BxPC-3 transplantation for two weeks (5 days a week). Tumor weight is recorded throughout the treatment period. At the end of the treatment period, animals are euthanized and their tumors harvested for protein isolation and western blot analysis for apoptotic markers.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1352 mL 10.6760 mL 21.3520 mL 53.3800 mL
    5 mM 0.4270 mL 2.1352 mL 4.2704 mL 10.6760 mL
    10 mM 0.2135 mL 1.0676 mL 2.1352 mL 5.3380 mL
    15 mM 0.1423 mL 0.7117 mL 1.4235 mL 3.5587 mL
    20 mM 0.1068 mL 0.5338 mL 1.0676 mL 2.6690 mL
    25 mM 0.0854 mL 0.4270 mL 0.8541 mL 2.1352 mL
    30 mM 0.0712 mL 0.3559 mL 0.7117 mL 1.7793 mL
    40 mM 0.0534 mL 0.2669 mL 0.5338 mL 1.3345 mL
    50 mM 0.0427 mL 0.2135 mL 0.4270 mL 1.0676 mL
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    UMI-77 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    UMI-77518303-20-3UMI77UMI 77Bcl-2 FamilyInhibitorinhibitorinhibit

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