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Obatoclax (Synonyms: GX15-070)
Obatoclax (GX15-070) 是 BH3 模拟物，是泛 BCL-2 家族蛋白抑制剂，对 BCL-2 的 Ki 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。
Obatoclax Chemical Structure
CAS No. : 803712-67-6
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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* Please select Quantity before adding items.
Obatoclax 的其他形式现货产品:
Obatoclax Mesylate
| 生物活性 |
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].
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| IC50 & Target[1][2] |
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BCL2
200 nM (Ki)
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Mcl-1
1-7 μM (Ki)
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Bcl-xL
1-7 μM (Ki)
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Bcl-W
1-7 μM (Ki)
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Bcl-B
1-7 μM (Ki)
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体外研究
(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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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体内研究
(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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
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| Clinical Trial |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Or CR, et al. Obatoclax, a Pan-BCL-2 Inhibitor, Targets Cyclin D1 for Degradation to Induce Antiproliferation in Human Colorectal Carcinoma Cells. Int J Mol Sci. 2016 Dec 27;18(1).
[2]. Nguyen M, et al. Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7. Epub 2007 Nov 26.
[3]. Sulkshane P, et al. BH3 mimetic Obatoclax (GX15-070) mediates mitochondrial stress predominantly via MCL-1 inhibition and induces autophagy-dependent necroptosis in human oral cancer cells. Oncotarget. 2016 Aug 5;8(36):60060-60079.
[4]. Ehrenkaufer G, et al. Identification of anisomycin, prodigiosin and obatoclax as compounds with broad-spectrum anti-parasitic activity. PLoS Negl Trop Dis. 2020 Mar 20;14(3):e0008150.
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