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  3. Obatoclax

Obatoclax (Synonyms: GX15-070)

Cat. No.: HY-10969A
Handling Instructions

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.

Obatoclax Chemical Structure

Obatoclax Chemical Structure

CAS No. : 803712-67-6

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Top Publications Citing Use of Products

    Obatoclax 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 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.

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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].

    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].

    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.
    Molecular Weight

    317.38

    Formula

    C₂₀H₁₉N₃O

    CAS No.

    803712-67-6

    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

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Keywords:

    ObatoclaxGX15-070Bcl-2 FamilyAutophagyParasiteBH3mimeticproteasomaldegradationanti-cancerbroad-spectrumantiparasitichumancolorectalcancerInhibitorinhibitorinhibit

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