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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
6 Results for "
AKR1C4 Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (6)
6 Results for "AKR1C4 Inhibitors" in MCE Product Catalog:
3
3 Cited Publications
Research Areas:
S07-2010 is a potent pan-AKR1C (aldo-keto reductase family 1 member C) inhibitor, with IC50 values of 0.19, 0.36, 0.47, and 0.73 μM for AKR1C3, AKR1C4, AKR1C1 and AKR1C2, respectively. S07-2010 induces apoptosis in A549/DDP cells. S07-2010 strengthens the cytotoxicity of chemotherapeutic agents in drug-resistant cells. S07-2010 significantly inhibits the proliferation of drug-resistant cells .
Cat. No.: HY-150649
CAS No.: 1826337-40-9
Research Areas:
S07-2005 racemic is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 value of 0.13 μM and 0.75 μM for AKR1C3 and AKR1C4, respectively. S07-2005 racemic has potential as a chemotherapeutic potentiator for cancer agent resistance .
Cat. No.: HY-173132
CAS No.: 3114057-78-9
Research Areas:
AKR1Cs-IN-1 (Compound 29) is a potent and broad-spectrum inhibitor targeting members of the Aldo-Keto Reductase 1C family (AKR1C1-1C4). By simultaneously occupying the SP2 and SP3 pockets, it effectively inhibits multiple isoforms and disrupts metabolic pathways associated with drug resistance. In enzymatic activity assays, AKR1Cs-IN-1 exhibited significant inhibitory potency, with IC50 values of 0.09, 0.28, 0.05, and 0.51 µM against AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. In the doxorubicin (DOX)-resistant breast cancer cell line MCF-7/ADR, AKR1Cs-IN-1 showed remarkable resensitization effects and significantly enhanced the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on overcoming drug resistance in breast cancer .
Cat. No.: HY-124432
CAS No.: 700856-05-9
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 .
Cat. No.: HY-184928
CAS No.: 3099381-90-2
S34-1040 is an AKR1C3 inhibitor with a human IC50 of 0.03 μM and exhibits no detectable inhibition of AKR1C1, AKR1C2, or AKR1C4. S34-1040 functions as a chemosensitizer and restores sensitivity of doxorubicin-resistant breast cancer cells to doxorubicin. S34-1040 can be used for the research of doxorubicin-resistant breast cancer .
Cat. No.: HY-181542
Research Areas:
SG-55 is a selective, noncompetitive and orally active AKR1C3 inhibitor with an IC50 of 5 nM and a Ki of 10 nM. SG-55 shows >2000-fold selectivity for AKR1C3 over AKR1C1, AKR1C2, and AKR1C4 (> 10 μM). SG-55 increases the ratio of reduced/oxidized nicotinamide adenine dinucleotide phosphate (NADPH/NADP +), decreases the ratio of reduced/oxidized glutathione (GSH/GSSG), and induces DNA double-strand breaks. SG-55 can overcome Osimertinib (HY-15772) resistance mediated by EGFR C797S triple mutation in non-small cell lung cancer (NSCLC) .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
