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Cat. No.: HY-184699

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AKR1C3-IN-16

AKR1C3-IN-16 is a selective AKR1C3 inhibitor with a human IC₅₀ of 0.084 μM. AKR1C3-IN-16 features a coumarin core that anchors to the oxyanion site and substituents that interact with the SP1 pocket. AKR1C3-IN-16 acts as an antiproliferative agent in prostate cancer cells. AKR1C3-IN-16 can be used for the research of castration-resistant prostate cancer.

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

Formula: C₂₈H₃₃NO₄
Molecular Weight:447.57

Storage:

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

AKR1C3-IN-16 Chemical Structure

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Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

AKR1C3

84 nM (IC₅₀)

All 17β-HSD Isoforms :

17β-HSD5/AKR1C3

In Vitro

AKR1C3-IN-16 (Compound 7k) potently inhibits the proliferation of 22Rv1 prostate cancer cells at 72 h, with an IC₅₀ value of 3.05 μM^[1].
AKR1C3-IN-16 (1.525-24.4 μM; 24 h) downregulates the expression of PSA protein in 22Rv1 prostate cancer cells after 24 h of treatment at concentrations of 6.1 μM and above, indicating that the androgen signaling axis is involved in its antiproliferative activity^[1].

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

Western Blot Analysis^[1]

Cell Line:

Human prostate cancer 22Rv1 cells
Concentration:

1.525, 3.05, 6.1, 12.2 and 24.4 μM
Incubation Time:

24 h
Result:

Downregulated PSA protein expression at concentrations of 6.1 μM and above, compared to the control group.
Caused no substantial cell viability loss at these concentrations at the 24 h time point.

Chemical Information

Molecular Weight 447.57
Formula C₂₈H₃₃NO₄
SMILES

CC(C=C1)=CC=C1COC2=CC=C3C(OC(C=C3)=O)=C2C/C=C(C(N(CCC)CCC)=O)\C
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]. Zheng X, et al. Rational design and structural insights of osthole-derived selective AKR1C3 inhibitors with cellular activity. Bioorganic chemistry. 2026 Jun 17;180:110123. [Content Brief]

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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.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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AKR1C3-IN-16

All 17β-HSD Isoforms