1. Epigenetics
  2. Histone Demethylase
  3. 2,4-PDCA

2,4-PDCA (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-PDCA is a target chemical in the field of bio-based plastics.

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2,4-PDCA Chemical Structure

2,4-PDCA Chemical Structure

CAS No. : 499-80-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 27 In-stock
Solution
10 mM * 1 mL in DMSO USD 27 In-stock
Solid
100 mg USD 25 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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  • References

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Description

2,4-PDCA (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-PDCA is a target chemical in the field of bio-based plastics[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HeLa GI50
> 240 μM
Compound: 2, PCA
Growth inhibition of human HeLa cells after 48 hrs by MTT assay
Growth inhibition of human HeLa cells after 48 hrs by MTT assay
[PMID: 23964788]
KYSE-150 cell line GI50
> 240 μM
Compound: 2, PCA
Growth inhibition of human KYSE-150 cells after 48 hrs by MTT assay
Growth inhibition of human KYSE-150 cells after 48 hrs by MTT assay
[PMID: 23964788]
LNCaP CC50
588.7 μM
Compound: 2
Cytotoxicity against human LNCAP cells after 3 days by MTT assay
Cytotoxicity against human LNCAP cells after 3 days by MTT assay
[PMID: 24971742]
Sf21 IC50
0.76 μM
Compound: 1; 2,4-PDCA
Inhibition of KDM5A (1 to 797 residues) (unknown origin) expressed in insect sf21 cells using ARTK(Me3)QTARKSTGGKAPRK peptide/ 100 uM alpha-ketoglutarate as substrate/cofactor incubated for 45 mins by MALDI assay
Inhibition of KDM5A (1 to 797 residues) (unknown origin) expressed in insect sf21 cells using ARTK(Me3)QTARKSTGGKAPRK peptide/ 100 uM alpha-ketoglutarate as substrate/cofactor incubated for 45 mins by MALDI assay
[PMID: 26699912]
Sf9 IC50
1.5 μM
Compound: 1, PCA
Inhibition of human recombinant PHD1 expressed in Sf9 cells by time-resolved fluorescence assay
Inhibition of human recombinant PHD1 expressed in Sf9 cells by time-resolved fluorescence assay
[PMID: 20684604]
Sf9 IC50
6.1 μM
Compound: 1, PCA
Inhibition of human recombinant PHD2 expressed in Sf9 cells by time-resolved fluorescence assay
Inhibition of human recombinant PHD2 expressed in Sf9 cells by time-resolved fluorescence assay
[PMID: 20684604]
In Vitro

2,4-PDCA (2 µM (tested in purified enzyme system), 25 µM (tested in cellular system)) significantly inhibits prolyl 4-hydroxylase activity and interferes with collagen synthesis[3].
2,4-PDCA (700 µM) inhibits prolyl 4-hydroxylase activity and reduces procollagen production in the chicken calvaria model[3].

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

Molecular Weight

167.12

Formula

C7H5NO4

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=NC=CC(C(O)=O)=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (598.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.9837 mL 29.9186 mL 59.8372 mL
5 mM 1.1967 mL 5.9837 mL 11.9674 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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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 (14.96 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 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 (14.96 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.
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

Purity: 99.80%

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 5.9837 mL 29.9186 mL 59.8372 mL 149.5931 mL
5 mM 1.1967 mL 5.9837 mL 11.9674 mL 29.9186 mL
10 mM 0.5984 mL 2.9919 mL 5.9837 mL 14.9593 mL
15 mM 0.3989 mL 1.9946 mL 3.9891 mL 9.9729 mL
20 mM 0.2992 mL 1.4959 mL 2.9919 mL 7.4797 mL
25 mM 0.2393 mL 1.1967 mL 2.3935 mL 5.9837 mL
30 mM 0.1995 mL 0.9973 mL 1.9946 mL 4.9864 mL
40 mM 0.1496 mL 0.7480 mL 1.4959 mL 3.7398 mL
50 mM 0.1197 mL 0.5984 mL 1.1967 mL 2.9919 mL
60 mM 0.0997 mL 0.4986 mL 0.9973 mL 2.4932 mL
80 mM 0.0748 mL 0.3740 mL 0.7480 mL 1.8699 mL
100 mM 0.0598 mL 0.2992 mL 0.5984 mL 1.4959 mL
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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.

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Product Name:
2,4-PDCA
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HY-W017132
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