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

Obatoclax Mesylate (Synonyms: GX15-070 Mesylate)

Cat. No.: HY-10969 Purity: 99.74%
Handling Instructions

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
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 264 In-stock
Estimated Time of Arrival: December 31
100 mg USD 432 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Obatoclax Mesylate:

Top Publications Citing Use of Products

    Obatoclax Mesylate purchased from MCE. Usage Cited in: Biomed Pharmacother. 2020 Jun 18;129:110371.

    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 MCE. Usage Cited in: Biomed Pharmacother. 2020 Jun 18;129:110371.

    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:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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, 100, 150, 200, 250, 300, 350, 400, 450 nM) potently inhibits the clonogenic potential of oral cancer cells[1].

    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].

    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.

    803712-79-0

    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, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 12.5 mg/mL (30.23 mM; Need ultrasonic)

    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
    10 mM 0.2418 mL 1.2092 mL 2.4184 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.74%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    ObatoclaxGX15-070Bcl-2 FamilyAutophagyParasiteBH3mimeticproteasomaldegradationanti-cancerbroad-spectrumantiparasitichumancolorectalcancerInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email address *

    Phone number *

     

    Organization name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Obatoclax Mesylate
    Cat. No.:
    HY-10969
    Quantity:
    MCE Japan Authorized Agent: