Art. -Nr.: HY-13503

Epothilone A

(Synonyms: Epo A)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Epothilone A is a competitive inhibitor of the binding of [³H] paclitaxel to tubulin polymers, with a K_i of 0.6-1.4 μM.

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Reinheit: 99.81%
CAS. Nr.: 152044-53-6
Formel: C₂₆H₃₉NO₆S
Molecular Weight:493.66

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Epothilone A Chemical Structure

CAS. Nr.: 152044-53-6

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Epothilone A is a competitive inhibitor of the binding of [³H] paclitaxel to tubulin polymers, with a K_i of 0.6-1.4 μM.

Cellular Effect

Cell Line	Type	Value	Description	References
1A9	IC₅₀	2.2 nM Compound: 174 (Epothilone A)	Inhibitory concentration against ovarian carcinoma 1A9 cell growth Inhibitory concentration against ovarian carcinoma 1A9 cell growth	[PMID: 16134928]
1A9/ptx-10	IC₅₀	20 nM Compound: 174 (Epothilone A)	Inhibitory concentration against beta-tubulin mutant 1A9PTX10 cell growth Inhibitory concentration against beta-tubulin mutant 1A9PTX10 cell growth	[PMID: 16134928]
1A9/ptx-22	IC₅₀	5.9 nM Compound: 174 (Epothilone A)	Inhibitory concentration against beta-tubulin mutant 1A9PTX22 cell line Inhibitory concentration against beta-tubulin mutant 1A9PTX22 cell line	[PMID: 16134928]
A549	IC₅₀	2.2 nM Compound: Epo A	Antiproliferative activity against human A549 cells after 72 hrs Antiproliferative activity against human A549 cells after 72 hrs	[PMID: 19433359]
A549	IC₅₀	2.6 nM Compound: EpoA	Cytotoxicity against human A549 cells after 72 hrs by methylene blue assay Cytotoxicity against human A549 cells after 72 hrs by methylene blue assay	[PMID: 19804980]
A549	IC₅₀	>5 μM Compound: 4	Cytotoxicity against human A549 cells after 48 hrs by SRB assay Cytotoxicity against human A549 cells after 48 hrs by SRB assay	[PMID: 25084144]
HCT-116	IC₅₀	2.8 nM Compound: 1a, epothilone A	Antiproliferative activity against human HCT116 cells after 72 hrs by methylene blue staining Antiproliferative activity against human HCT116 cells after 72 hrs by methylene blue staining	[PMID: 18271516]
HT-1080	IC₅₀	1.3 nM Compound: EpoA	Cytotoxicity against human HT1080 cells after 3 days by MTT assay Cytotoxicity against human HT1080 cells after 3 days by MTT assay	[PMID: 19804980]
KB	IC₅₀	1.91 nM Compound: Epothilone A	Concentration required to inhibit the growth of paclitaxel-resistant human epidermoid carcinoma cells KB-8511 by 50 percent (72 hr exposure) Concentration required to inhibit the growth of paclitaxel-resistant human epidermoid carcinoma cells KB-8511 by 50 percent (72 hr exposure)	[PMID: 11133086]
KB 3-1	IC₅₀	2.15 nM Compound: Epothilone A	Concentration required to inhibit the growth of paclitaxel-sensitive human epidermoid carcinoma cells KB-31 by 50 percent (72 hr exposure) Concentration required to inhibit the growth of paclitaxel-sensitive human epidermoid carcinoma cells KB-31 by 50 percent (72 hr exposure)	[PMID: 11133086]
KB 3-1	IC₅₀	0.0096 μM Compound: Epothilone A	Cytotoxicity against human KB3-1 cells by MTT assay Cytotoxicity against human KB3-1 cells by MTT assay	[PMID: 25397992]
L929	IC₅₀	4 ng/mL Compound: 1	Cytotoxicity against mouse L929 cells Cytotoxicity against mouse L929 cells	[PMID: 11473410]
L929	IC₅₀	0.0077 μM Compound: Epothilone A	Cytotoxicity against mouse L929 cells by MTT assay Cytotoxicity against mouse L929 cells by MTT assay	[PMID: 25397992]
L929	IC₅₀	0.0038 μM Compound: Epothilone A	Cytotoxicity against mouse L929 cells after 5 days by MTT assay Cytotoxicity against mouse L929 cells after 5 days by MTT assay	[PMID: 27231731]
MCF7	IC₅₀	2.9 nM Compound: 1a, epothilone A	Antiproliferative activity against human MCF7 cells after 72 hrs by methylene blue staining Antiproliferative activity against human MCF7 cells after 72 hrs by methylene blue staining	[PMID: 18271516]
MCF7	IC₅₀	2.6 nM Compound: Epo A	Antiproliferative activity against human MCF7 cells after 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs	[PMID: 19433359]
MCF7	IC₅₀	2.5 nM Compound: EpoA	Cytotoxicity against human MCF7 cells after 72 hrs by methylene blue assay Cytotoxicity against human MCF7 cells after 72 hrs by methylene blue assay	[PMID: 19804980]
MCF7	IC₅₀	0.0008 μM Compound: 4	Cytotoxicity against human MCF7 cells in presence of 10 mM DTT after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells in presence of 10 mM DTT after 48 hrs by SRB assay	[PMID: 25084144]
MCF7	IC₅₀	0.0009 μM Compound: 4	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 25084144]
MCF7	IC₅₀	0.8 nM Compound: 4	Cytotoxicity against human MCF7 cells in presence of 10 mM DTT after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells in presence of 10 mM DTT after 48 hrs by SRB assay	[PMID: 25084144]
MCF7	IC₅₀	0.9 nM Compound: 4	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 25084144]
MCF7	IC₅₀	0.0022 μM Compound: Epothilone A	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 25397992]
PC-3	IC₅₀	0.0024 μM Compound: Epothilone A	Cytotoxicity against human PC3 cells by MTT assay Cytotoxicity against human PC3 cells by MTT assay	[PMID: 25397992]
PC-3M	IC₅₀	6.4 nM Compound: 1a, epothilone A	Antiproliferative activity against human PC3M cells after 72 hrs by methylene blue staining Antiproliferative activity against human PC3M cells after 72 hrs by methylene blue staining	[PMID: 18271516]
SK-OV-3	IC₅₀	0.0013 μM Compound: Epothilone A	Cytotoxicity against human SKOV3 cells by MTT assay Cytotoxicity against human SKOV3 cells by MTT assay	[PMID: 25397992]

In Vitro

Epothilone A is a competitive inhibitor of the binding of [³H] paclitaxel to tubulin polymers. The apparent K_i value for Epothilone A is 1.4 μM by Hanes analysis and 0.6 μM by Dixon analysis^[1]. Epothilone A, is noted to be highly cytotoxic (IC₅₀=0.05 μM) in vitro when applied to the human T-24 bladder carcinoma cell line. The binding affinity of Epothilone A to tubulin is of the same order of magnitude as the binding affinity of paclitaxel to tubulin based on competition assays. The IC₅₀ for displacement of 100 nM of (³H) paclitaxel from the tubulin binding site is 3.6 μM for paclitaxel, 2.3 μM for Epothilone A, and 3.3 μM for patupilone^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 152044-53-6
Appearance Solid
Molecular Weight 493.66
Formel C₂₆H₃₉NO₆S
Color White to off-white
SMILES

O=C(C[C@H](O)C1(C)C)O[C@H](/C(C)=C/C2=CSC(C)=N2)C[C@]3([H])O[C@]3([H])CCC[C@H](C)[C@H](O)[C@@H](C)C1=O
Synonyms

Epo A
Structure Classification
- Antibiotics
- Macrolide Antibiotics
Initial Source
- Microorganisms
Sorangium cellulosum
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

Clin Transl Med

Mechanism of Gzma-mediated GEF-H1 activation in intestinal epithelial cells leading to intestinal barrier dysfunction in sepsis. [Abstract]

2026 Apr;16(4):e70651. PMID: 41943423
bioRxiv

2025 Nov 12.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (253.21 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

2.0257 mL

10.1284 mL

20.2569 mL

5 mM

0.4051 mL

2.0257 mL

4.0514 mL

10 mM

0.2026 mL

1.0128 mL

2.0257 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. 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: ≥ 2.08 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, 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 (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Kowalski RJ, et al. Activities of the microtubule-stabilizing agents epothilones A and B with purified tubulin and in cells resistant to paclitaxel (Taxol(R)). J Biol Chem. 1997 Jan 24;272(4):2534-41. [Content Brief]

[2]. Cheng KL, et al. Novel microtubule-targeting agents - the epothilones. Biologics. 2008 Dec;2(4):789-811. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0257 mL	10.1284 mL	20.2569 mL	50.6421 mL
	5 mM	0.4051 mL	2.0257 mL	4.0514 mL	10.1284 mL
	10 mM	0.2026 mL	1.0128 mL	2.0257 mL	5.0642 mL
	15 mM	0.1350 mL	0.6752 mL	1.3505 mL	3.3761 mL
	20 mM	0.1013 mL	0.5064 mL	1.0128 mL	2.5321 mL
	25 mM	0.0810 mL	0.4051 mL	0.8103 mL	2.0257 mL
	30 mM	0.0675 mL	0.3376 mL	0.6752 mL	1.6881 mL
	40 mM	0.0506 mL	0.2532 mL	0.5064 mL	1.2661 mL
	50 mM	0.0405 mL	0.2026 mL	0.4051 mL	1.0128 mL
	60 mM	0.0338 mL	0.1688 mL	0.3376 mL	0.8440 mL
	80 mM	0.0253 mL	0.1266 mL	0.2532 mL	0.6330 mL
	100 mM	0.0203 mL	0.1013 mL	0.2026 mL	0.5064 mL

Keywords

Epothilone A

2 Cited Publications

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Epothilone A

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Mass Spectrometry Natural Product Library

Publications Citing Use of MedChemExpress (MCE) Epothilone A

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Epothilone A

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Natural Product Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Lipid Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Microbial Metabolite Library

Anti-Cancer Natural Product Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Cysteine Targeted Covalent Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Natural Product Library Plus

Natural Product and Natural Product-Like Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

RO5 Drug-like Natural Product Library

High-Throughput Bioactive Compound Library

High-Throughput Natural Product Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Natural Product Diversity Scaffold Library

Bacteria-Sourced Compound Library

Mass Spectrometry Natural Product Library

Publications Citing Use of MedChemExpress (MCE) Epothilone A

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Epothilone A Related Classifications

HY-13503 Related Classifications