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

Obatoclax Mesylate  (Synonyms: GX15-070 Mesylate)

Cat. No.: HY-10969 Purity: 99.74%
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Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.

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

Obatoclax Mesylate Chemical Structure

Obatoclax Mesylate Chemical Structure

CAS No. : 803712-79-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 85 In-stock
50 mg USD 290 In-stock
100 mg USD 475 In-stock
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Based on 12 publication(s) in Google Scholar

Other Forms of Obatoclax Mesylate:

Obatoclax Mesylate Related Antibodies

Top Publications Citing Use of Products

    Obatoclax Mesylate 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 Mesylate 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.

    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

    View All Parasite Isoform Specific Products:

    View All Isoforms
    Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

    • Biological Activity

    • Purity & Documentation

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    Description

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

    IC50 & Target[5]

    Bcl-2

    220 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 Mesylate (GX15-070 Mesylate) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM[2].
    ? Obatoclax Mesylate (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 Mesylate (400 nM; for 24 hours) induces autophagy in OSCC cells[3].
    ? Obatoclax Mesylate (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations[1].
    ? Obatoclax Mesylate (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM[1].
    ? Obatoclax Mesylate 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 Mesylate (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax Mesylate inhibits GSK3β but activates p38MAPK, while barely affecting ERK1/2 activity in HT-29 cells[1].
    ? Obatoclax Mesylate (50-450 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 Mesylate 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: 25, 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 Mesylate (GX15-070 Mesylate; 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

    413.49

    Formula

    C21H23N3O4S
    CAS No.
    Appearance

    Solid

    Color

    Purple to black

    SMILES

    COC1=CC(C2=CC3=C(C=CC=C3)N2)=N/C1=C\C4=C(C=C(N4)C)C.CS(=O)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 12.5 mg/mL (30.23 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 2.4184 mL 12.0922 mL 24.1844 mL
    5 mM 0.4837 mL 2.4184 mL 4.8369 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 (sealed storage, away from moisture and light). 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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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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: ≥ 0.83 mg/mL (2.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (2.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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

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    Dosing volume
    (per animal)

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    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    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: 99.74%

    SDS (419 KB)

    COA (250 KB) HNMR (228 KB) LCMS (120 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 (sealed storage, away from moisture and light). 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 2.4184 mL 12.0922 mL 24.1844 mL 60.4610 mL
    5 mM 0.4837 mL 2.4184 mL 4.8369 mL 12.0922 mL
    10 mM 0.2418 mL 1.2092 mL 2.4184 mL 6.0461 mL
    15 mM 0.1612 mL 0.8061 mL 1.6123 mL 4.0307 mL
    20 mM 0.1209 mL 0.6046 mL 1.2092 mL 3.0230 mL
    25 mM 0.0967 mL 0.4837 mL 0.9674 mL 2.4184 mL
    30 mM 0.0806 mL 0.4031 mL 0.8061 mL 2.0154 mL
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    Obatoclax Mesylate 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:

    Obatoclax803712-79-0GX15-070Bcl-2 FamilyAutophagyParasiteBH3mimeticproteasomaldegradationanti-cancerbroad-spectrumantiparasitichumancolorectalcancerInhibitorinhibitorinhibit

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