Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.
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Obatoclax Mesylate Estructura química
No. CAS : 803712-79-0
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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.
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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Descripciòn
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2[1][2]. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity[3][4].
IC50 & Target[5]
Bcl-2
220 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 Mesylate (GX15-070 Mesylate) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM[2]. ?
Obatoclax Mesylate (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 Mesylate (400 nM; for 24 hours) induces autophagy in OSCC cells[3]. ?
Obatoclax Mesylate (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations[1]. ?
Obatoclax Mesylate (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM[1]. ?
Obatoclax Mesylate 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 Mesylate (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax Mesylate inhibits GSK3β but activates p38MAPK, while barely affecting ERK1/2 activity in HT-29 cells[1]. ?
Obatoclax Mesylate (50-450 nM) potently inhibits the clonogenic potential of oral cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Obatoclax Mesylate Related Antibodies
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:
25, 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 Mesylate (GX15-070 Mesylate; 1.15-5 mg/kg; intravenously injected; five consecutive days) exhibits potent antitumor activity in xenograft mouse models in a dose-dependent manner[4].
MedChemExpress (MCE) 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.
Room temperature in continental US; may vary elsewhere.
Almacenamiento
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
In Vitro:
DMSO : 12.5 mg/mL (30.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.4184 mL
12.0922 mL
24.1844 mL
5 mM
0.4837 mL
2.4184 mL
4.8369 mL
10 mM
0.2418 mL
1.2092 mL
2.4184 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[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).
[Content Brief]
[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.
[Content Brief]
[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.
[Content Brief]
[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.
[Content Brief]
[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.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
2.4184 mL
12.0922 mL
24.1844 mL
60.4610 mL
5 mM
0.4837 mL
2.4184 mL
4.8369 mL
12.0922 mL
10 mM
0.2418 mL
1.2092 mL
2.4184 mL
6.0461 mL
15 mM
0.1612 mL
0.8061 mL
1.6123 mL
4.0307 mL
20 mM
0.1209 mL
0.6046 mL
1.2092 mL
3.0230 mL
25 mM
0.0967 mL
0.4837 mL
0.9674 mL
2.4184 mL
30 mM
0.0806 mL
0.4031 mL
0.8061 mL
2.0154 mL
Obatoclax Mesylate Related Classifications
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.