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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
13 Results for "
AKR1C2 Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (13)
13 Results for "AKR1C2 Inhibitors" in MCE Product Catalog:
18
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-161839
CAS No.: 3107747-45-2
Research Areas:
AKR1C2/3-IN-1 (compound 3a) is a potent AKR1C2 and AKR1C3 inhibitor with IC50 values of 90, 50 nM, respectively. AKR1C2/3-IN-1 can be used as a radiation sensitizer and as a potentiator of chemotherapy cytotoxicity .
Cat. No.: HY-146573
CAS No.: 2137881-54-8
Research Areas:
AKR1C3-IN-6 (Compound 1) is a potent, selective AKR1C3 inhibitor with IC50 values of 0.31 μM and 73.23 μM against AKR1C3 and AKR1C2, respectively. AKR1C3-IN-6 shows antitumor activity .
Cat. No.: HY-121656
CAS No.: 56600-73-8
AKR1C2/3-IN-2 is a potential AKR1C3 inhibitor with selective AKR1C3 activity. AKR1C2/3-IN-2 is able to block AKR1C3-mediated testosterone (T) production and PSA induction, affecting the endocrine activity of prostate cancer cells. AKR1C2/3-IN-2 shows selectivity over other AKR1C enzymes, indicating its potential application in inhibiting drug-resistant prostate cancer. AKR1C2/3-IN-2 has no inhibitory activity against COX isomerases, further emphasizing its specificity as a prostate cancer inhibitory compound .
Cat. No.: HY-163609
PROTAC AKR1C3 degrader-1 is a PROTAC degrader targeting AKR1C3, with a DC50 of 52 nM. PROTAC AKR1C3 degrader-1 induces proteasome-dependent degradation of AKR1C3 and inhibits the enzymatic activities of AKR1C3, AKR1C1 and AKR1C2. PROTAC AKR1C3 degrader-1 degrades ARv7 by disrupting the stable AKR1C3/ARv7 complex. PROTAC AKR1C3 degrader-1 reduces the viability of prostate cancer cells expressing AKR1C3 and sensitizes Enzalutamide (HY-70002)-resistant prostate cancer cells. PROTAC AKR1C3 degrader-1 can be used in the research of prostate cancer .
Cat. No.: HY-B0398AR
CAS No.: 3374-05-8
Research Areas:
Liquiritin (Standard) is the analytical standard of Liquiritin. This product is intended for research and analytical applications. Liquiritin, a flavonoid isolated from Glycyrrhiza uralensis, is a potent and competitive AKR1C1 inhibitor with IC50s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo . Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity .
Target:
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-W414731
CAS No.: 16524-22-4
Synonyms: 3-MFA
Research Areas:
N-(3-Methylphenyl)anthranilic acid is an aldo-keto reductase 1C3 (AKR1C3)and AKR1C2 inhibitor with IC50 values of 0.24 μM and 0.38 μM, respectively. N-(3-Methylphenyl)anthranilic acid shows no inhibition of COX-1 or COX-2. N-(3-Methylphenyl)anthranilic acid can be used for the research of castration resistant prostate 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
