Col003
Based on 9 publication(s) in Google Scholar
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
For research use only. We do not sell to patients.
- Purity : 99.46%
- CAS No.: 328565-16-8
- Formula: C14H11NO4
- Molecular Weight:257.24
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications Citing Use of MedChemExpress (MCE) Col003
More- Cell Rep Med. 2024 May 21;5(5):101533. [Abstract]
- J Immunother Cancer. 2025 Nov 28;13(11):e011976. [Abstract]
- Dev Cell. 2024 Nov 4;59(21):2834-2849.e9. [Abstract]
- J Invest Dermatol. 2024 Mar;144(3):633-644. [Abstract]
- Front Pharmacol. 2022 Jan 10;12:792263. [Abstract]
- Mol Immunol. 2026 Jul:195:186-197. [Abstract]
- Thromb Res. 2026 Jun 4:263:109734. [Abstract]
- Neurol Res. 2025 Nov 4:1-12. [Abstract]
- bioRxiv. 2024 Mar 28.
Biological Activity
Description
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. Further protocols information, click here.
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Cell Line:Wild-type MEFs
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Concentration:100 μM
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Incubation Time:After 50 °C or 37 °C for 15 min
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Result:Affected correctly folded triple helix structures and α,α′-dipyridyl on collagen secretion.
Chemical Information
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CAS No. 328565-16-8
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Appearance Solid
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Molecular Weight 257.24
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Formula C14H11NO4
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Color Light yellow to yellow
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SMILES
O=CC1=CC(CC2=CC=CC=C2)=CC([N+]([O-])=O)=C1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Targeting the HSP47-collagen axis inhibits brain metastasis by reversing M2 microglial polarization and restoring anti-tumor immunity. [Abstract]2024 May 21;5(5):101533. PMID: 38744278 -
J Immunother Cancer
HSP47 inhibition-induced CD155 expression through TRAF2 deubiquitination promotes tumor immune evasion. [Abstract]2025 Nov 28;13(11):e011976. PMID: 41314980 -
Dev Cell
Hox gene activity directs physical forces to differentially shape chick small and large intestinal epithelia. [Abstract]2024 Nov 4;59(21):2834-2849.e9. PMID: 39116876 -
J Invest Dermatol
Benzbromarone Induces Targeted Degradation of HSP47 Protein and Improves Hypertrophic Scar Formation. [Abstract]2024 Mar;144(3):633-644. PMID: 37838329 -
Front Pharmacol
Hsp47 Inhibitor Col003 Attenuates Collagen-Induced Platelet Activation and Cerebral Ischemic-Reperfusion Injury in Rats. [Abstract]2022 Jan 10;12:792263. PMID: 35082674 -
Mol Immunol
HSP47 inhibitor Col003 attenuates thromboinflammation after cerebral ischemia-reperfusion by suppressing GPVI-mediated CD84 shedding in platelets. [Abstract]2026 Jul:195:186-197. PMID: 42172863 -
Thromb Res
Col003 attenuates sepsis-associated coagulation dysfunction in mice in association with reduced platelet activation and NET formation. [Abstract]2026 Jun 4:263:109734. PMID: 42250517 -
Neurol Res
HSP47 inhibitor Col003 may attenuates neurological impairment in chronic ischemic stroke rats by inhibiting LCN2. [Abstract]2025 Nov 4:1-12. PMID: 41185942 -
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
Purity & Documentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
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 |