1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. HSP
  3. Col003

Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC50=1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis

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Col003 Chemical Structure

Col003 Chemical Structure

CAS No. : 328565-16-8

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Based on 5 publication(s) in Google Scholar

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Description

Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC50=1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis[1]

IC50 & Target[1]

HSP47

1.8 μM (IC50)

In Vitro

Col003 (4.4-40 μM) is cleaved from Col001 (AK-778). Col003 has an inhibitory effect on the interaction of Hsp47 with collagen in Hsp47 KO / MEFs[1].
Col003 (0.01-100 μM) exhibits dose-dependent effects on the interactions of Hsp47 with collagen. The IC50 value is 1.8 μM for Hsp47[1].
Col003 (100 μM; 20-60 mins) has an nhibitory effects on collagen secretion and accumulation. It inhibits collagen secretion by wild-type MEFs and the secretion is not abolished completely[1].
Col003 (100 μM) degrades α,α′-dipyridyl collagen secretion completely by incubation with trypsin at a high temperature (50 °C for 15 min), but it resistant to trypsin digestion at 37 °C[1].
.

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

Western Blot Analysis[1]

Cell Line: Wild-type MEFs
Concentration: 100 μM
Incubation Time: After 50 °C or 37 °C for 15 min
Result: Affected correctly folded triple helix structures and α,α′-dipyridyl on collagen secretion.
Molecular Weight

257.24

Formula

C14H11NO4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=CC1=CC(CC2=CC=CC=C2)=CC([N+]([O-])=O)=C1O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (194.37 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 3.8874 mL 19.4371 mL 38.8742 mL
5 mM 0.7775 mL 3.8874 mL 7.7748 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (9.72 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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: 99.87%

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, 6 months; -20°C, 1 month (stored under nitrogen). 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 3.8874 mL 19.4371 mL 38.8742 mL 97.1855 mL
5 mM 0.7775 mL 3.8874 mL 7.7748 mL 19.4371 mL
10 mM 0.3887 mL 1.9437 mL 3.8874 mL 9.7186 mL
15 mM 0.2592 mL 1.2958 mL 2.5916 mL 6.4790 mL
20 mM 0.1944 mL 0.9719 mL 1.9437 mL 4.8593 mL
25 mM 0.1555 mL 0.7775 mL 1.5550 mL 3.8874 mL
30 mM 0.1296 mL 0.6479 mL 1.2958 mL 3.2395 mL
40 mM 0.0972 mL 0.4859 mL 0.9719 mL 2.4296 mL
50 mM 0.0777 mL 0.3887 mL 0.7775 mL 1.9437 mL
60 mM 0.0648 mL 0.3240 mL 0.6479 mL 1.6198 mL
80 mM 0.0486 mL 0.2430 mL 0.4859 mL 1.2148 mL
100 mM 0.0389 mL 0.1944 mL 0.3887 mL 0.9719 mL
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