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  3. Obatoclax

Obatoclax (Synonyms: GX15-070)

Cat. No.: HY-10969A
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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.

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Obatoclax Chemical Structure

Obatoclax Chemical Structure

CAS No. : 803712-67-6

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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.

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Keywords:

ObatoclaxGX15-070Bcl-2 FamilyAutophagyParasiteBH3mimeticproteasomaldegradationanti-cancerbroad-spectrumantiparasitichumancolorectalcancerInhibitorinhibitorinhibit

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