1. Metabolic Enzyme/Protease
  2. Aldose Reductase
  3. AKR1C3-IN-5

AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells.

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AKR1C3-IN-5 Chemical Structure

AKR1C3-IN-5 Chemical Structure

CAS No. : 2839142-93-5

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Description

AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells[1].

Cellular Effect
Cell Line Type Value Description References
DU-145 IC50
47.3 μM
Compound: 6e
Antiproliferative activity against human DU-145 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human DU-145 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
MCF-10A CC50
52.2 μM
Compound: 6e
Cytotoxicity against human MCF-10A cells assessed as cell viability for 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
MCF7 IC50
9.6 μM
Compound: 6e
Antiproliferative activity against human MCF7 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
MDA-MB-231 IC50
80.6 μM
Compound: 6e
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
PC-3 IC50
34 μM
Compound: 6e
Antiproliferative activity against human PC-3 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
PNT2 CC50
36.3 μM
Compound: 6e
Cytotoxicity against human PNT2 cells assessed as cell viability for 72 hrs by MTT assay
Cytotoxicity against human PNT2 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
Molecular Weight

592.72

Formula

C34H44N2O7

CAS No.
SMILES

CC(OC1=CC=C(C=C1C/C=C(C)\C)/C=C/C(N[C@H](C(OCC2=CC=CC=C2)=O)CCCCNC(OC(C)(C)C)=O)=O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • 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:
AKR1C3-IN-5
Cat. No.:
HY-144749
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