Art. -Nr.: HY-10969

Obatoclax Mesylate

(Synonyms: GX15-070 Mesylate)

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a K_i 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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Reinheit: 99.85%
CAS. Nr.: 803712-79-0
Formel: C₂₁H₂₃N₃O₄S
Molecular Weight:413.49

Speicherung:

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)

Obatoclax Mesylate Chemical Structure

CAS. Nr.: 803712-79-0

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Use of MCE Products

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a K_i 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)

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Alle Parasite Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 803712-79-0
Appearance Solid
Molecular Weight 413.49
Formel C₂₁H₂₃N₃O₄S
Color Purple to black
SMILES

COC1=CC(C2=CC3=C(C=CC=C3)N2)=N/C1=C\C4=C(C=C(N4)C)C.CS(=O)(O)=O
Synonyms

GX15-070 Mesylate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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)

Publications (12)

All In Vivo Efficacy StudyOthersCell Proliferation/Viability AssayIFWB

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Journal Impact Factor

Cancer Lett

High-content drug screening in zebrafish xenografts reveals high efficacy of dual MCL-1/BCL-XL inhibition against Ewing sarcoma. [Abstract]

2023 Feb 1:554:216028. PMID: 36462556
Acta Pharmacol Sin

Combinations of proteasome inhibitors with obatoclax are effective for small cell lung cancer. [Abstract]

2021 Aug;42(8):1298-1310. PMID: 33139838
Drug Deliv Transl Res

Leveraging quantum chemical properties in transfer learning for predicting blood-brain barrier permeability of drugs. [Abstract]

2025 Oct 29. PMID: 41160380
Sci Rep

Drivers of AR indifferent anti-androgen resistance in prostate cancer cells. [Abstract]

2019 Sep 24;9(1):13786. PMID: 31551480

Obatoclax Mesylate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2019 Sep 24;9(1):13786. [Abstract]

Dose response curves showing the proliferation at increasing concentrations of the PARP inhibitor olaparib and the pan-BCL-2 inhibitor Obatoclax Mesylate in normal growth medium (containing 10 µM enzalutamide for ResA/ResB).
ACS Infect Dis

Bcl-2 Antagonist Obatoclax Reactivates Latent HIV-1 via the NF-κB Pathway and Induces Latent Reservoir Cell Apoptosis in Latently Infected Cells. [Abstract]

2023 Nov 10;9(11):2105-2118. PMID: 37796279
iScience

Identification of potent inhibitors of SARS-CoV-2 infection by combined pharmacological evaluation and cellular network prioritization. [Abstract]

2022 Sep 16;25(9):104925. PMID: 35992305

Obatoclax Mesylate purchased from MedChemExpress. Usage Cited in: iScience. 2022 Sep 16;25(9):104925. [Abstract]

Male and female mice were infected with SARS-CoV-2 virus intranasally, and infection began 6 hours after daily treatment with 3 mg/kg Obatoclax Mesylate. Viral load in the lungs (FFU/g tissue) was measured 4 days post-infection.
Viruses

Identification and Tracking of Antiviral Drug Combinations. [Abstract]

2020 Oct 18;12(10):1178. PMID: 33080984

Obatoclax Mesylate purchased from MedChemExpress. Usage Cited in: Viruses. 2020 Oct 18;12(10):1178. [Abstract]

The effects of 5 µM vemurafenib plus 0.1% DMSO, 0.2 µM emetine, 0.2 µM homoharringtonine, 0.2 µM Obatoclax Mesylate, 1 µL Gemcitabine, 0.1 µL Anisomycin and 1 µL Cycloheximide on viral replication measured by plaque reduction assay.
Am J Cancer Res

Targeting sphingosine kinase 2 suppresses cell growth and synergizes with BCL2/BCL-XL inhibitors through NOXA-mediated MCL1 degradation in cholangiocarcinoma. [Abstract]

2019 Mar 1;9(3):546-561. PMID: 30949409

Obatoclax Mesylate purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2019 Mar 1;9(3):546-561. [Abstract]

RBE, HCCC9810, and HuH28 cells were treated with different concentrations of ABC294640 or Obatoclax Mesylate, alone or in combination, for 72 hours, and then cell viability was analyzed using the CCK-8 assay.
bioRxiv

2024 Jul 25.
Norwegian University of Science and Technology

2021 Oct.
Universitat Politècnica de València

2020 Sep 7.
Biomed Pharmacother

Biomimetic nanoparticle loading obatoclax mesylate for the treatment of non-small-cell lung cancer (NSCLC) through suppressing Bcl-2 signaling. [Abstract]

2020 Sep;129:110371. PMID: 32563984

Obatoclax Mesylate purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Sep;129:110371. [Abstract]

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.

Obatoclax Mesylate purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Sep;129:110371. [Abstract]

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.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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

Solubility: ≥ 0.83 mg/mL (2.01 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.83 mg/mL (2.01 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Keywords

Obatoclax Mesylate

12 Cited Publications

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Obatoclax Mesylate

Anti-Infection Compound Library

Apoptosis Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Autophagy Compound Library

Anti-Blood Cancer Compound Library

Antiparasitic Compound library

Mitochondria-Targeted Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Protein-protein Interaction Inhibitor Library

Anti-Pulmonary Fibrosis Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Obatoclax Mesylate

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Obatoclax Mesylate

Anti-Infection Compound Library

Apoptosis Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Autophagy Compound Library

Anti-Blood Cancer Compound Library

Antiparasitic Compound library

Mitochondria-Targeted Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Protein-protein Interaction Inhibitor Library

Anti-Pulmonary Fibrosis Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Obatoclax Mesylate

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Obatoclax Mesylate Related Classifications

HY-10969 Related Classifications