1. Metabolic Enzyme/Protease
  2. Aldose Reductase
  3. AKR1B10-IN-1

AKR1B10-IN-1 is a potent inhibitor of AKR1B10 (Aldo-Keto Reductase 1B10) with an IC50 of 3.5 nM. AKR1B10-IN-1 suppresses proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells.

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

AKR1B10-IN-1 Chemical Structure

AKR1B10-IN-1 Chemical Structure

CAS No. : 2136579-33-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

AKR1B10-IN-1 is a potent inhibitor of AKR1B10 (Aldo-Keto Reductase 1B10) with an IC50 of 3.5 nM. AKR1B10-IN-1 suppresses proliferation, metastasis, and Cisplatin (CDDP) resistance of lung cancer cells[1].

IC50 & Target

3.5 nM (AKR1B10); 277 nM (AKR1B1)[1]

In Vitro

AKR1B10-IN-1 (compound 4e) (0-20 μM; 96 hours) dose-dependently suppresses the growth of both A549 and A549/1B10 cells[1].
AKR1B10-IN-1 (compound 4e) (0-20 μM; 96 hours) completely suppresses increased cell proliferation by the overexpressing AKR1B10 as well as the endogenous protein[1].
AKR1B10-IN-1 (compound 4e) (0-40 μM; 26 hours; pretreatment with AKR1B10-IN-1 for 2 hours, then incubated with CDDP for 24 hours) decreases the cell viability of CDDP-R-A549 cells in a dose-dependent manner[1].

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

Cell Viability Assay[1]

Cell Line: A549 cells, A549/1B10 cells (AKR1B10-stably overexpressing A549 cells)
Concentration: 0, 10, 20 μM
Incubation Time: 96 hours
Result: Dose-dependently suppressed the growth of both A549 and A549/1B10 cells, and statistically significant at 20 μM.

Cell Viability Assay[1]

Cell Line: CDDP-resistance (cisplatin-resisitance) of A549 cells
Concentration: 0, 10, 20, 40 μM
Incubation Time: Pretreatment with AKR1B10-IN-1 for 2 hours, then incubated with CDDP for 24 hours
Result: Decreased the cell viability of CDDP-R-A549 cells in a dose-dependent manner, and most obvious in the treatment of 40 μM.
Molecular Weight

341.33

Formula

C19H16FNO4

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CC2=CC=C(O)C=C2OC1=O)NCCCC3=CC=C(F)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (292.97 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 2.9297 mL 14.6486 mL 29.2972 mL
5 mM 0.5859 mL 2.9297 mL 5.8594 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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, 6 months; -20°C, 1 month. 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 2.9297 mL 14.6486 mL 29.2972 mL 73.2429 mL
5 mM 0.5859 mL 2.9297 mL 5.8594 mL 14.6486 mL
10 mM 0.2930 mL 1.4649 mL 2.9297 mL 7.3243 mL
15 mM 0.1953 mL 0.9766 mL 1.9531 mL 4.8829 mL
20 mM 0.1465 mL 0.7324 mL 1.4649 mL 3.6621 mL
25 mM 0.1172 mL 0.5859 mL 1.1719 mL 2.9297 mL
30 mM 0.0977 mL 0.4883 mL 0.9766 mL 2.4414 mL
40 mM 0.0732 mL 0.3662 mL 0.7324 mL 1.8311 mL
50 mM 0.0586 mL 0.2930 mL 0.5859 mL 1.4649 mL
60 mM 0.0488 mL 0.2441 mL 0.4883 mL 1.2207 mL
80 mM 0.0366 mL 0.1831 mL 0.3662 mL 0.9155 mL
100 mM 0.0293 mL 0.1465 mL 0.2930 mL 0.7324 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:
AKR1B10-IN-1
Cat. No.:
HY-139696
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