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Results for "

AKR1C3 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	17β-HSD (3) Aldose Reductase (14) Androgen Receptor (1) Endogenous Metabolite (1) Ligands for Target Protein for PROTAC (1) PPAR (1) PROTACs (1) RAR/RXR (1) Reactive Oxygen Species (2)
By Research Areas:	Cancer (27) Inflammation/Immunology (3) Neurological Disease (2)

Inhibitors & Agonists

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-107379

AKR1C3-IN-1 1 Publications Verification	Others	Others
AKR1C3-IN-1 is a potent, highly selective inhibitor of *AKR1C3, with an IC₅₀* of 13 nM.

HY-138557

AKR1C3-IN-4	17β-HSD	Cancer
AKR1C3-IN-4 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC₅₀ of 0.56 μM. AKR1C3-IN-4 has the potential for castrate resistant prostate cancer (CRPC) research .

HY-163323

AKR1C3-IN-12	Aldose Reductase	Cancer
AKR1C3-IN-12 (compound 2j) is an aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC₅₀ of 27 nM. AKR1C3-IN-12 enhances the efficacy of Gemcitabine and Cisplatin in bladder cancer .

HY-163610

AKR1C3-IN-13	Ligands for Target Protein for PROTAC Aldose Reductase	Cancer
AKR1C3-IN-13 (Compound 4) is an *AKR1C3* inhibitor. AKR1C3-IN-13 degrades AKR1C3 in prostate cancer cells .

HY-146574

AKR1C3-IN-7	Others	Cancer
AKR1C3-IN-7 (Compound 13) is a potent, selective *AKR1C3* inhibitor with an IC₅₀ of 0.19 μM. AKR1C3-IN-7 shows antitumor activity .

HY-146575

AKR1C3-IN-8	Aldose Reductase 17β-HSD	Cancer
AKR1C3-IN-8 (Compound 5) is a potent, selective *AKR1C3* inhibitor with an IC₅₀ of 0.069 μM. AKR1C3-IN-8 shows antitumor activity .

HY-146573

AKR1C3-IN-6	Others	Cancer
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 .

HY-157810

AKR1C3-IN-11	Aldose Reductase	Cancer
AKR1C3-IN-11 (Compound 6e) is a Aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC₅₀ of 2.0 μM. AKR1C3-IN-11 inhibit cell proliferation in combination with abiraterone (HY-70013). AKR1C3-IN-11 can be used for the research of prostate cancer .

HY-163784

AKR1C3-IN-14	Aldose Reductase	Cancer
AKR1C3-IN-14 (compound 4) is an *AKR1C3* inhibitor (IC₅₀=0.122 μM) that reduces the overproduction of androgens by inhibiting the activity of the *AKR1C3* enzyme, thereby regulating hormone-mediated signaling. AKR1C3-IN-14 also plays a role in the biosynthesis of the prostaglandin PGF2α, regulating cell proliferation by affecting this pathway. AKR1C3-IN-14 can be used in the study of prostate cancer .

HY-155502

AKR1C3-IN-10	Aldose Reductase	Cancer
AKR1C3-IN-10 (compound 5r) is a selective *AKR1C3* inhibitor (IC₅₀=51 nM). AKR1C3-IN-10 shows good activity in a prostate cancer xenograft model .

HY-144749

AKR1C3-IN-5	Aldose Reductase	Cancer
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 .

HY-152188

AKR1C3-IN-9	Aldose Reductase	Cancer
AKR1C3-IN-9 is a selective inhibitor of Aldo-keto Reductase 1C3 (AKR1C3) with an IC₅₀ value of 8.92 nM. AKR1C3-IN-9 significantly reverses the Doxorubicin (HY-15142A) (DOX) resistance in a resistant breast cancer cell line .

HY-19903

ASP-9521 2 Publications Verification	Others	Cancer
ASP-9521 is a potent, selective and orally available *AKR1C3* inhibitor with an IC₅₀ of 11 nM for human AKR1C3.

HY-163609

PROTAC AKR1C3 degrader-1	PROTACs Aldose Reductase	Cancer
PROTAC AKR1C3 degrader-1 (compound 5) is a potent *AKR1C3* PROTAC degrader. PROTAC AKR1C3 degrader-1 decreases the protein expression of AKR1C3, AKR1C1/2, and ARv7. PROTAC AKR1C3 degrader-1 has the potential for the research of prostate cancer. (Blue:ubiquitin E3 ligase cereblon ligand (HY-A0003), Black: linker (HY-163647); Pink: AKR1C3 inhibitor (HY-163610)) .

HY-155035

S07-1066	Others	Cancer
S07-1066 is an aldo-keto reductase 1C3 (AKR1C3) inhibitor, synergizing doxorubicin (DOX) cytotoxicity. S07-1066 selectively blocks AKR1C3-mediated reduction of DOX, and reverses the DOX resistance in overexpressing AKR1C3 cells .

HY-109154

Obafistat	Others	Inflammation/Immunology
Obafistat is a potent aldo-keto reductase *AKR1C3* inhibitor with an IC₅₀ of 1.2 nM for human AKR1C3 (patent WO2017202817A1, example 4) .

HY-116170

SN34037	Aldose Reductase	Cancer
SN34037 is a specific inhibitor of Aldo-keto reductase 1C3 (AKR1C3, EC 1.1.1.188) with the ability to inhibit the cytotoxic activity of PR-104A. SN34037-sensitive coumberone reduction provides a rapid and specific assay for AKR1C3 activity. SN34037 inhibits the aerobic cytotoxicity of PR-104A in TF1 erythroleukemia cells with high AKR1C3 expression, but not in Nalm6 pre-B acute lymphoblastic leukemia cells with low AKR1C3 expression .

HY-152189

S19-1035	Others	Cancer
S19-1035 is a highly potent and specific aldo-keto reductase 1C3 (AKR1C3) inhibitor. S19-1035 inhibits AKR1C3 with an IC₅₀ value of 3.04 nM. S19-1035 can be used for the research of tumor .

HY-150649

S07-2005 (racemic)	17β-HSD	Cancer
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 .

HY-121656

AKR1C2/3-IN-2	Endogenous Metabolite	Cancer
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 .

HY-150646

S07-2009	Others	Cancer
S07-2009 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC₅₀ value of 0.20 μM .

HY-163940

LX1	Aldose Reductase Androgen Receptor	Cancer
LX1 is an anti-prostate cancer compound that targets androgen receptor (AR), AR variants and steroidogenic enzyme *AKR1C3. LX1 inhibits* the enzymatic activity of *AKR1C3, reduces the conversion of androstenedione to testosterone and reduces the expression of AR and AR-V7* and downregulates their target genes. LX1 overcomes the resistance of tumor cells to Enzalutamide (HY-70002), and the combination with Enzalutamide (HY-70002) further inhibits tumor growth .

HY-150648

S07-2008	Others	Cancer
S07-2008 is a selective aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with an IC₅₀ of 0.16 μM. S07-2008 shows anticancer activities .

HY-150644

S07-2010 1 Publications Verification	Aldose Reductase	Cancer
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 .

HY-150650

S07-2001	Others	Cancer
S07-2001 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC₅₀ value of 2.08 μM. S07-2001 enhances the activity of Doxorubicin against cancer cells. S07-2001 has potential as a chemotherapeutic potentiator for cancer agent resistance .

HY-161839

AKR1C2/3-IN-1	Aldose Reductase	Cancer
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 .

HY-N10361

Drupanin	RAR/RXR PPAR Aldose Reductase	Cancer
Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC₅₀ value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers .

HY-N0376

Liquiritin Maximum Cited Publications 6 Publications Verification	Reactive Oxygen Species	Neurological Disease Inflammation/Immunology Cancer
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 .

HY-N0376R

Liquiritin (Standard)	Reactive Oxygen Species	Neurological Disease Inflammation/Immunology Cancer
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 .

Drupanin	Monophenols Animals Classification of Application Fields Source classification Phenols Disease Research Fields Cancer	RAR/RXR PPAR Aldose Reductase
Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC₅₀ value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers .

Liquiritin 5+ Cited Publications	Structural Classification Neurological Disease Classification of Application Fields Source classification Plants Monophenols Flavonoids Leguminosae Flavonones Phenols Glycyrrhiza uralensis Fisch. Inflammation/Immunology Disease Research Fields	Reactive Oxygen Species
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 .

Liquiritin (Standard)	Structural Classification Monophenols Flavonoids Leguminosae Flavonones Source classification Phenols Plants Glycyrrhiza uralensis Fisch.	Reactive Oxygen Species
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 .

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AKR1C3 inhibitor

Inhibitors & Agonists

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Natural
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