Selective Inhibitor of Aldo-Keto Reductase family member 1B10 (AKR1B10) HCCFA | Funakoshi
Date:January 23 2018Web Page No:80996
Funakoshi Co.,Ltd.
Selective Inhibitor of AKR1B10
HCCFA

HCCFA is a potent and selective Inhibitor of Aldo-Keto Reductase family member 1B10 (AKR1B10).
AKR1B10 is a NADPH dependent reductase, and involved in metabolism of retinoid and isoprenoid.
After high expression of AKR1B10 in non-small cell lung cancer (NSCLC) was reported in 2005, such high expression was also found liver cancer, uterus cancer and bile duct cancer.
Therefore, AKR1B10 inhibitor was noted as a new target of anti-cancer drug development.
AKR1B10 shows 70.6% homology in amino-acid sequence to aldose reductase (AKR1B1, or AR), and both have similar structure and substrate specificity.
As a result, conventional inhibitors for AKR1B10 also inhibit AR to the same degree, selective inhibtor against AKR1B10 or AR has been searched.
HCCFA is a new compound which inhibits AKR1B10 selectively and strongly.
This product has been commercialized with the support of both the University of Toyama and Gifu Pharmaceutical University.
Features
- Selective and strong inhibitor of AKR1B10.
- Low inhibitory potency to AKR1B1 (AR, aldose reductase)
Chemical Information
- Chemical Name: 7-Hydroxy-2-oxo-2H-chromene-3-carboxylic acid [3-(4-fluorophenyl)propyl] amide
- Alternate Name: N-[3-(4-fluorophenyl)propyl]-7-hydroxy-2-oxo-2H-1-Benzopyran-3-carboxamide
- CAS No.: 2136579-33-2
- Molecular Formula: C19H16FNO4
- Molecular Weight: 341.33
- Melting Point: 207-209 °C (Recrystallization Solvent: Ethanol)
- Solubility: Soluble in DMSO
- Purity: >98% by HPLC
Product Data

Fig.1 Inhibitory activity of HCCFA was measured by using recombinant AKR1B10 or AR. Data shows HCCFA inhibits AKR1B10 strongly and selectively.

Fig.2 A549 cells or CDDP-R-A549 cells (cisplatin-resistant A549 cells) were treated with 0 to 40 μM of HCCFA for 2 hours and cultured for 24 hours under culture media containing CDDP (cisplatin) 40 μM.
Data shows that HCCFA recovers CDDP susceptibility of CDDP-R-A549 cells in a dose-dependent manner.

Fig.3 Luciferase transduced A549-Luc cells were cultured in DMSO (control) or 20 μM HCCFA containing medium for 24 hours, and transfered to BALB/c nude mouse by tail vein injection.
4 days after, luminescent in lung was observed. Data shows that HCCFA inhibits proliferation and metastasis of A549 cells in vivo.
Reference
Endo S., et al., J. Med. Chem., 60:8441-8455 (2017).
[Date : February 09 2025 00:06]
Detail | Product Name | Product Code | Supplier | Size | Price | ||||||||||||||||||||||||||||||
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HCCFA, AKR1B10 inhibitor DatasheetThis may not be the latest data sheet. |
FDV-0016 | FNAFunakoshi Co.,Ltd. | 1 mg | $300 | |||||||||||||||||||||||||||||||
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[Date : February 09 2025 00:06]
HCCFA, AKR1B10 inhibitor
DatasheetThis may not be the latest data sheet.
- Product Code: FDV-0016
- Supplier: FNA
- Size: 1mg
- Price: $300
Description |
HCCFA is a potent and selective Inhibitor of Aldo-Keto Reductase family member 1B10 (AKR1B10). |
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Storage | -20°C | CAS | 2136579-33-2 |
Link |
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CONTACT
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