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Cat. No.: HY-123732

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CRT0083914

CRT0083914 is a subtype-selective non-carboxylate inhibitor of AKR1C3. CRT0083914 is applicable to the research of colon cancer.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 932495-16-4
Formule: C₁₆H₂₂N₂O₃S
Masse moléculaire:322.42

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

CRT0083914 Chemical Structure

CAS No.: 932495-16-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

CRT0083914 is a subtype-selective non-carboxylate inhibitor of AKR1C3. CRT0083914 is applicable to the research of colon cancer^[1].

IC₅₀ & Target

AKR1C3

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	11 nM Compound: 12	Inhibition of recombinant AKR1C3 (unknown origin) overexpressed in human HCT116 cells assessed as inhibition of aerobic reduction of dinitrobenzamide PR-104A to its hydroxylamine metabolite by LC-MS/MS assay Inhibition of recombinant AKR1C3 (unknown origin) overexpressed in human HCT116 cells assessed as inhibition of aerobic reduction of dinitrobenzamide PR-104A to its hydroxylamine metabolite by LC-MS/MS assay	[PMID: 23454516]

In Vitro

CRT0083914 (0.1 nM-100 μM) potently and selectively inhibits recombinant human AKR1C3 enzyme with an IC₅₀ of 0.094 μM, while showing no activity against AKR1C1, AKR1C2, AKR1C4, COX-1, or COX-2 at the tested concentrations^[1].
CRT0083914 inhibits AKR1C3-dependent PR-104A metabolism in AKR1C3-overexpressing HCT-116 cells with an IC₅₀ of 11 nM^[1].
CRT0083914 binds to AKR1C3 with its 2-pyrrolidinone in the SP3 pocket and its sulfonamide-containing group in the SP1 pocket, making no direct contact with the enzyme's oxyanion hole residues^[1].

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

Chemical Information

CAS No. 932495-16-4
Masse moléculaire 322.42
Formule C₁₆H₂₂N₂O₃S
SMILES

O=C1N(C2=CC=C(C=C2)S(=O)(=O)N3CCCCC3C)CCC1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Heinrich DM, et al. Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3. Eur J Med Chem. 2013;62:738-744. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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