1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. 1,4-DPCA

1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.

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

1,4-DPCA Chemical Structure

1,4-DPCA Chemical Structure

CAS No. : 331830-20-7

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 95 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE 1,4-DPCA

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM[1][2].

IC50 & Target

IC50: 2.4 µM (Collagen hydroxylation); 60 μM (Factor inhibiting HIF (FIH))[2]

In Vitro

1,4-DPCA (24 hours) treatment specifically increases the expression of multiple target genes, including the proangiogenic target genes Vegfa and Hmox1 and proglycolytic targets Ldh-a, Pgk1, Pdk1, and Glut1 in mouse B6 cells[1].
1,4-DPCA treatment significantly reduces the colony sizes of T4-2 (10 μM 1,4-DPCA) and ZR-75-1 cells (20 μM 1,4-DPCA). 1,4-DPCA-treated T4-2 cells form polarized spheroids in 3D culture. 1,4-DPCA treatment significantly reduces invasive branches in DA-MB-157 (20 μM 1,4-DPCA) and MDA-MB-231 (10 μM 1,4-DPCA) cells.1,4-DPCA inhibits the proliferation of T4-2, ZR-75-1, MDA-MB-157 and MDA-MB-231 cells[3].

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

In Vivo

1,4-DPCA treatment suppresses connective tissue ingrowth in porous porous poly (lactic-co-glycolic acid) (PLGA) discs implanted in the peritoneal cavity for 28 days in mice. 1,4-DPCA is found to be effective at inhibiting collagen deposition within and on the outer surface of the disc, and also limited connective tissue ingrowth, but not to the extent of glucocorticoid inhibition[2].

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

Molecular Weight

240.21

Formula

C13H8N2O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN=C2C3=NC=CC=C3C=CC2C1=O)O

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 : 12.5 mg/mL (52.04 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 4.1630 mL 20.8151 mL 41.6302 mL
5 mM 0.8326 mL 4.1630 mL 8.3260 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% Corn Oil

    Solubility: ≥ 0.92 mg/mL (3.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.92 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 (9.2 mg/mL) to 900 μL Corn oil, and mix evenly.

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:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (41.63 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

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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 4.1630 mL 20.8151 mL 41.6302 mL 104.0756 mL
5 mM 0.8326 mL 4.1630 mL 8.3260 mL 20.8151 mL
10 mM 0.4163 mL 2.0815 mL 4.1630 mL 10.4076 mL
15 mM 0.2775 mL 1.3877 mL 2.7753 mL 6.9384 mL
20 mM 0.2082 mL 1.0408 mL 2.0815 mL 5.2038 mL
25 mM 0.1665 mL 0.8326 mL 1.6652 mL 4.1630 mL
30 mM 0.1388 mL 0.6938 mL 1.3877 mL 3.4692 mL
40 mM 0.1041 mL 0.5204 mL 1.0408 mL 2.6019 mL
50 mM 0.0833 mL 0.4163 mL 0.8326 mL 2.0815 mL
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1,4-DPCA 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.

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1,4-DPCA
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