2. Apoptosis Autophagy Anti-infection
  3. Bcl-2 Family Autophagy Parasite
  4. Obatoclax

Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.

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

CAS No. : 803712-67-6

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Based on 12 publication(s) in Google Scholar

Other Forms of Obatoclax:

Obatoclax Related Antibodies

Top Publications Citing Use of Products

    Obatoclax purchased from MedChemExpress. Usage Cited in: iScience. 2022 Sep 16;25(9):104925.

    Male and female mice were infected with SARS-CoV-2 virus intranasally, and infection began 6 hours after daily treatment with 3 mg/kg Obatoclax Mesylate. Viral load in the lungs (FFU/g tissue) was measured 4 days post-infection.

    Obatoclax purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Sep;129:110371.  [Abstract]

    Immunofluorescence staining displays weaker Bcl-2 fluorescence intensity in lung cancer cells incubated with RBCm-Obatoclax Mesylate (OM)/PLGA, accompanied with stronger expression of pro-apoptotic signal Bax in comparison to the Con group.

    Obatoclax purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Sep;129:110371.  [Abstract]

    Bcl-2 and Bcl-xl protein expression levels are restrained in A549 and H1975 cells treated with RBCm-OM/PLGA; however, Bax, cleaved Caspase-3, Caspase-9 and PARP are up-regulated following RBCm-OM/PLGA incubation. Also, free Obatoclax Mesylate (OM) does not influence the expression change of all these proteins.

    Obatoclax purchased from MedChemExpress. Usage Cited in: Viruses. 2020 Oct 18;12(10):1178.  [Abstract]

    The effects of 5 µM vemurafenib plus 0.1% DMSO, 0.2 µM emetine, 0.2 µM homoharringtonine, 0.2 µM Obatoclax Mesylate, 1 µL Gemcitabine, 0.1 µL Anisomycin and 1 µL Cycloheximide on viral replication measured by plaque reduction assay.

    Obatoclax purchased from MedChemExpress. Usage Cited in: Sci Rep. 2019 Sep 24;9(1):13786.  [Abstract]

    Dose response curves showing the proliferation at increasing concentrations of the PARP inhibitor olaparib and the pan-BCL-2 inhibitor Obatoclax Mesylate in normal growth medium (containing 10 µM enzalutamide for ResA/ResB).

    Obatoclax purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2019 Mar 1;9(3):546-561.  [Abstract]

    RBE, HCCC9810, and HuH28 cells were treated with different concentrations of ABC294640 or Obatoclax Mesylate, alone or in combination, for 72 hours, and then cell viability was analyzed using the CCK-8 assay.

    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

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    View All Isoforms
    Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

    • Biological Activity

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    Description

    Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2[1][2]. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity[3][4].

    IC50 & Target[1][2]

    BCL2

    200 nM (Ki)

    Mcl-1

    1-7 μM (Ki)

    Bcl-xL

    1-7 μM (Ki)

    Bcl-W

    1-7 μM (Ki)

    Bcl-B

    1-7 μM (Ki)

    In Vitro

    Obatoclax (GX15-070) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM[2].
    Obatoclax (50-200 nM; 24-72 hours) induces a dose- and time-dependent reduction of cell numbers in all human colorectal cancer cell lines. In particular, the IC50 of cell proliferation at 72 h are 25.85, 40.69, and 40.01 nM for HCT116, HT-29, and LoVo cells, respectively[1].
    Obatoclax (400 nM; for 24 hours) induces autophagy in OSCC cells[3].
    Obatoclax (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations[1].
    Obatoclax (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM[1].
    Obatoclax induces T286 phosphorylation-dependent or -independent cyclin D1 degradation. in HCT116 and LoVo cells, the steady-state levels of p-Cyclin D (T286) began to decline once exposed to obatoclax (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax inhibits GSK3β but activates p38 MAPK, while barely affecting ERK1/2 activity in HT-29 cells[1].
    Obatoclax (50, 100, 150, 200, 250, 300, 350, 400, 450 nM) potently inhibits the clonogenic potential of oral cancer cells[1].

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

    Obatoclax Related Antibodies

    Cell Proliferation Assay[1]

    Cell Line: human colorectal cancer HCT116, HT-29 and LoVo cells
    Concentration: 50, 100, 200 nM
    Incubation Time: 24, 48, and 72 hours
    Result: Induced a dose- and time-dependent reduction of cell numbers.

    Cell Autophagy Assay[3]

    Cell Line: AW8507 and SCC029B cells
    Concentration: 400 nM
    Incubation Time: 24 hours
    Result: Induced autophagy in OSCC cells.

    Cell Cycle Analysis[1]

    Cell Line: HCT116 and HT-29 cells
    Concentration: 50, 100, 200 nM
    Incubation Time: 24 hours
    Result: Provoked a dose-dependent increase in the G1-phase cell populations.

    Western Blot Analysis[1]

    Cell Line: HCT116, HT-29 and LoVo cells
    Concentration: 50, 100, 200 nM
    Incubation Time: 24 hours
    Result: Indicated a marked drop in cyclin D1 levels as low as 50 nM.
    In Vivo

    Obatoclax (GX15-070; 1.15-5 mg/kg; intravenously injected; five consecutive days) exhibits potent antitumor activity in xenograft mouse models in a dose-dependent manner[4].

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

    Animal Model: 6-8 weeks old female BALB/C nude mice bearing subcutaneous tumors[4]
    Dosage: 1.15, 2.5, 5 mg/kg
    Administration: Intravenously injected (through lateral tail vein); five consecutive days (i.e. 5 injections)
    Result: Exhibited potent antitumor activity in xenograft mouse models in a dose-dependent manner.
    Clinical Trial
    Molecular Weight

    317.38

    Formula

    C20H19N3O
    CAS No.
    Appearance

    Solid

    Color

    Light brown to brown

    SMILES

    COC1=CC(C(N2)=CC3=C2C=CC=C3)=N/C1=C\C4=C(C)C=C(C)N4
    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 : 100 mg/mL (315.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1508 mL 15.7540 mL 31.5080 mL
    5 mM 0.6302 mL 3.1508 mL 6.3016 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.

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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 (7.88 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.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    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: ≥99.0%

    SDS (393 KB)

    COA (254 KB)

    Handling Instructions (2659 KB)
    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 3.1508 mL 15.7540 mL 31.5080 mL 78.7699 mL
    5 mM 0.6302 mL 3.1508 mL 6.3016 mL 15.7540 mL
    10 mM 0.3151 mL 1.5754 mL 3.1508 mL 7.8770 mL
    15 mM 0.2101 mL 1.0503 mL 2.1005 mL 5.2513 mL
    20 mM 0.1575 mL 0.7877 mL 1.5754 mL 3.9385 mL
    25 mM 0.1260 mL 0.6302 mL 1.2603 mL 3.1508 mL
    30 mM 0.1050 mL 0.5251 mL 1.0503 mL 2.6257 mL
    40 mM 0.0788 mL 0.3938 mL 0.7877 mL 1.9692 mL
    50 mM 0.0630 mL 0.3151 mL 0.6302 mL 1.5754 mL
    60 mM 0.0525 mL 0.2626 mL 0.5251 mL 1.3128 mL
    80 mM 0.0394 mL 0.1969 mL 0.3938 mL 0.9846 mL
    100 mM 0.0315 mL 0.1575 mL 0.3151 mL 0.7877 mL
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    Obatoclax 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:

    Obatoclax803712-67-6GX15-070Bcl-2 FamilyAutophagyParasiteBH3mimeticproteasomaldegradationanti-cancerbroad-spectrumantiparasitichumancolorectalcancerInhibitorinhibitorinhibit

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