Obatoclax B

SKU: orb2900911

Description

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.

Key Properties

• CAS Number: 803712-67-6
• MW: 317.38
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₉N₃O
• SMILES: C(=C1N=C(C=C1OC)C2=CC=3C(N2)=CC=CC3)C4=C(C)C=C(C)N4

Bioactivity

• 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. Animal model: 6-8 weeks old female BALB/C nude mice bearing subcutaneous tumors. 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.
• In Vitro:
  Obatoclax (GX15-070) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM. 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. Obatoclax (400 nM; for 24 hours) induces autophagy in OSCC cells. Obatoclax (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations. Obatoclax (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM. 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. Obatoclax (50, 100, 150, 200, 250, 300, 350, 400, 450 nM) potently inhibits the clonogenic potential of oral cancer cells. Cell Proliferation Assay 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 Cell line: AW8507 and SCC029B cells. Concentration: 400 nM. Incubation time: 24 hours. Result: Induced autophagy in OSCC cells. Cell Cycle Analysis 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only