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Obatoclax

CAS No. : 803712-67-6

MCE 国际站：Obatoclax

产品活性：Obatoclax (GX15-070) 是 BH3 模拟物，是泛 BCL-2 家族蛋白抑制剂，对 BCL-2 的 K_i 值为 220 nM。Obatoclax 诱导自噬 (autophagy) 依赖性细胞死亡，并靶向细胞周期蛋白 D1 进行蛋白酶体降解。Obatoclax 具有抗癌和广谱抗寄生虫 (antiparasitic) 活性。

研究领域：Apoptosis | Autophagy | Anti-infection

作用靶点：Bcl-2 Family | Autophagy | Parasite

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.

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.

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