2. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease
  3. HDAC Aminopeptidase
  4. Bufexamac

Bufexamac  (Synonyms: Bufexamic acid)

Cat. No.: HY-B0494 Purity: ≥98.0%
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Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 µM and 0.22 µM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug.

For research use only. We do not sell to patients.

Bufexamac Chemical Structure

Bufexamac Chemical Structure

CAS No. : 2438-72-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
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500 mg USD 119 In-stock
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Based on 1 publication(s) in Google Scholar

Bufexamac Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Bufexamac

View All HDAC Isoform Specific Products:

View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • Biological Activity

  • Purity & Documentation

  • References

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Description

Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 µM and 0.22 µM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug[1][2][3].

IC50 & Target[1]

HDAC6

10.7 μM (Kd app)

HDAC10

12.3 μM (Kd app)

HDAC8

235 μM (Kd app)

HDAC3

341 μM (Kd app)

In Vitro

Bufexamac (0.1-100 µM, 16 h) inhibits the secretion of IFN-α in peripheral blood mononuclear cells[1].
Bufexamac (30 µM, 6 days) inhibits HDAC10 to block autophagic flux in BE(2)-C cells and enhances the tumor-specific toxicity of DNA damage-inducing drugs[2].
Bufexamac (50-100 µM, 30 min) inhibits calcium ionophore A23187 stimulation of neutrophil chemotaxis via the inhibition of LTA4H-mediated endogenous LTB4 biosynthesis, with an IC50 of 12.91±4.02 μM for LTB4[3].
Bufexamac (0-500 µM, 4 h) inhibits lysine deacetylases (KDACs) at lower concentrations (>5 µM) and induces hypoxia-like responses in Hela cells by chelating cellular iron at higher concentrations (>200 µM) in Hela cells[4].

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

Bufexamac Related Antibodies

Cell Viability Assay[2]

Cell Line: BE(2)-C cells
Concentration: 30 µM
Incubation Time: 6 days
Result: Enhanced cell death of tumor cells.

Cell Migration Assay [3]

Cell Line: mouse neutrophils
Concentration: 50-100 µM
Incubation Time: 30 min
Result: Reduced fMLP (5μM) induced neutrophil migration.

Western Blot Analysis[4]

Cell Line: Hela cells (ATCC: CCL-2)
Concentration: 1 mM
Incubation Time: 4-16 h
Result: Induced HIF1-α protein and increased HIF1-α levels.

Immunofluorescence[4]

Cell Line: Hela cells (ATCC: CCL-2)
Concentration: 50-250 µM
Incubation Time: 4 h
Result: Stabilized HIF1-α and accumulated in the nucleus.
In Vivo

Bufexamac (50-100 mg/kg, p.o., seven days) ameliorates LPS-induced acute lung injury in mice by targeting LTA4H[3].
Bufexamac (20-100 mg, Intraarticular (IA) injection, weekly, 6 times) don’t cause any untoward systemic or local effects in healthy horse[5].

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

Animal Model: Six-to-eight weeks old female C57BL/6 mice[3]
Dosage: 50-100 mg/kg
Administration: Oral gavage (p.o.), seven days
Result: Ameliorated the infiltration of lung inflammatory cells and injury to the lung in a dose-dependent manner.
Relieved LPS-induced lung injury.
Reduced LTB4 level and MPO activity.
Reduced cytokine mRNA expressions in lung tissue and cytokine levels in BALF in LPS-induced ALI in mice.
Animal Model: horses aged 2 to 7 years old and weighing 302 to 522 kg [5]
Dosage: 20-100 mg
Administration: Intraarticular (IA) injection, weekly, 6 times
Result: Didn't effect on general health, hematological or serum biochemical variables, or organs.
Molecular Weight

223.27

Formula

C12H17NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NO)CC1=CC=C(OCCCC)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (447.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4789 mL 22.3944 mL 44.7888 mL
5 mM 0.8958 mL 4.4789 mL 8.9578 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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: 2.5 mg/mL (11.20 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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)

    Solubility: ≥ 2.5 mg/mL (11.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 10 mg/mL (44.79 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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).
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.
 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.
Purity & Documentation
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.4789 mL 22.3944 mL 44.7888 mL 111.9720 mL
5 mM 0.8958 mL 4.4789 mL 8.9578 mL 22.3944 mL
10 mM 0.4479 mL 2.2394 mL 4.4789 mL 11.1972 mL
15 mM 0.2986 mL 1.4930 mL 2.9859 mL 7.4648 mL
20 mM 0.2239 mL 1.1197 mL 2.2394 mL 5.5986 mL
25 mM 0.1792 mL 0.8958 mL 1.7916 mL 4.4789 mL
30 mM 0.1493 mL 0.7465 mL 1.4930 mL 3.7324 mL
40 mM 0.1120 mL 0.5599 mL 1.1197 mL 2.7993 mL
50 mM 0.0896 mL 0.4479 mL 0.8958 mL 2.2394 mL
60 mM 0.0746 mL 0.3732 mL 0.7465 mL 1.8662 mL
80 mM 0.0560 mL 0.2799 mL 0.5599 mL 1.3997 mL
100 mM 0.0448 mL 0.2239 mL 0.4479 mL 1.1197 mL
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Bufexamac 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.

Keywords:

Bufexamac2438-72-4Bufexamic acidHDACAminopeptidaseHistone deacetylasesHDAC6 Inhibitoranti-inflammatoryLTA4H InhibitorInhibitorinhibitorinhibit

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