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
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
AKR1C3 84 nM (IC50) |
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. Further protocols information, click here.
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Cell Line:Human prostate cancer 22Rv1 cells
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Concentration:1.525, 3.05, 6.1, 12.2 and 24.4 μM
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Incubation Time:24 h
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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
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Molecular Weight 447.57
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Formula C28H33NO4
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SMILES
CC(C=C1)=CC=C1COC2=CC=C3C(OC(C=C3)=O)=C2C/C=C(C(N(CCC)CCC)=O)\C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AKR1C3-IN-16 Related Classifications
HY-184699 Related Classifications
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