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Cat. No.: HY-124432

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CRT0093964

CRT0093964 is an isoform-selective non-carboxylate inhibitor of AKR1C3 (IC₅₀=0.11 μM) with no activity against AKR1C1, AKR1C2, AKR1C4, COX-1, and COX-2.CRT0093964 can be used for the research of leukemia, hormone-related cancers, colon cancer.

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

CAS No.: 700856-05-9
Formula: C₁₅H₂₀ClN₃O₂
Molecular Weight:309.79

Storage:

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

CRT0093964 Chemical Structure

CAS No.: 700856-05-9

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

AKR1C3

0.11 μM (IC₅₀)

All 17β-HSD Isoforms :

17β-HSD5/AKR1C3

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.018 μM Compound: 24	Inhibition of AKR1C3 (unknown origin) expressed in human HCT116 cells assessed as formation of PR-104H from PR-104A preincubated for 2 hrs Inhibition of AKR1C3 (unknown origin) expressed in human HCT116 cells assessed as formation of PR-104H from PR-104A preincubated for 2 hrs	[PMID: 24411201]

In Vitro

CRT0093964 (0.1 nM-100 μM; 1 h) potently and selectively inhibits purified recombinant AKR1C3 with an IC₅₀ of 0.11 μM; in contrast, this compound shows no inhibitory effect on AKR1C1, AKR1C2 or AKR1C4 at concentrations up to 30 μM^[1].
CRT0093964 (1 nM-3 μM; 2 h pre-treatment) inhibits AKR1C3-dependent metabolism of PR-104A (HY-16405) in AKR1C3-overexpressing HCT-116 cells, with an IC₅₀ of 0.018 μM, and exhibits higher potency in cellular assays than in purified enzyme assays^[1].

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

Chemical Information

CAS No. 700856-05-9
Molecular Weight 309.79
Formula C₁₅H₂₀ClN₃O₂
SMILES

O=C(N1CCOCC1)N2CCN(C3=CC=C(Cl)C=C3)CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Flanagan JU, et al. Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3). Bioorg Med Chem. 2014;22(3):967-977. [Content Brief]

Calculators

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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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