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17β-Hydroxysteroid dehydrogenase (17β-HSD) inhibitors in this category mostly target one aldo-keto reductase. Aldo-keto reductase family 1 member C3 (AKR1C3), also called type 5 17β-HSD, reduces androstenedione to testosterone in peripheral tissues. Its close relatives AKR1C1 and AKR1C2 act mainly on other steroids, inactivating progesterone and 5α-dihydrotestosterone. These isoforms share high sequence identity, so selectivity between them is a central question in inhibitor research. AKR1C3-IN-1 and AKR1C2/3-IN-1 address AKR1C3, while AKR1C1-IN-1 is directed at AKR1C1. Stylopine, a protoberberine alkaloid, is also listed as an AKR1C3 inhibitor. AKR1B10-IN-1 targets AKR1B10, a reductase of a neighboring subfamily that is studied in retinoid and lipid metabolism.
HSD17B13-IN-77 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC50 value of less than 0.1 μM for estradiol. This compound is valuable for research related to liver diseases and metabolic disorders, providing insight into the role of HSD17B13 in various physiological and pathological processes. Its application may enhance understanding of steroid metabolism and its implications in health and disease.
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HSD17B13-IN-20 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13). This compound plays a crucial role in the modulation of estrogen metabolism and is particularly relevant in the study of liver diseases, including hepatitis, liver fibrosis, liver cirrhosis, and hepatocellular carcinoma. HSD17B13-IN-20 provides valuable insights into the therapeutic targeting of HSD17B13 for the treatment and understanding of hepatic disorders.
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HSD17B13-IN-68 is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), demonstrating an IC50 value of less than 0.1 μM for estradiol. This compound is valuable for investigating the role of HSD17B13 in liver diseases and metabolic disorders, providing insights into potential therapeutic targets and mechanisms of action in these conditions. Its potency and specificity make it a useful tool for research in endocrinology and metabolic pathways.
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HSD17B13-IN-64 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC50 value of ≤ 0.1 μM for estradiol. This compound is valuable for research focused on liver diseases, including non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH), as well as metabolic disorders and drug-induced liver injury (DILI). Its selective inhibition of HSD17B13 may provide insights into therapeutic strategies for these conditions.
ESC1002755 is a selective inhibitor of 17β-HSD10, exhibiting an IC50 of 19 nM and demonstrating non-competitive inhibition against the cofactor NADH. This compound shows minimal cytotoxicity in HEK293 cells at a concentration of 50 μM, making it a promising tool for studies related to Alzheimer’s disease and hormone-dependent cancers, including prostate, bone, and colorectal cancer. Research applications include exploring the enzymatic mechanisms and therapeutic interventions associated with these conditions.
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HSD17B13-IN-11 is a selective inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting potent activity with an IC50 of ≤ 1 μM for leukotriene B3 and ≤ 0.1 μM for estradiol. This compound is valuable for investigating liver pathologies, including non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and drug-induced liver injury (DILI). Its role in metabolic and cardiovascular research also supports its utility in exploring potential therapeutic interventions.
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HSD17B13-IN-38 is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13). This compound plays a significant role in the regulation of steroid metabolism and has potential implications in the study of liver and metabolic diseases, including non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH). Researchers can utilize HSD17B13-IN-38 to explore its impact on cardiovascular diseases and related metabolic pathways.
HSD17B13-IN-23 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC50 of less than 0.1 μM for estradiol and below 1 μM for leukotriene B3. This compound is significant in the study of nonalcoholic fatty liver diseases (NAFLDs), particularly in relation to nonalcoholic steatohepatitis (NASH). Its capacity to modulate HSD17B13 activity makes it a valuable tool for investigating the biochemical pathways involved in hepatic lipid metabolism and related disorders.
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HSD17B13-IN-88 is a potent inhibitor of 17β-Hydroxysteroid dehydrogenase 13 (HSD17B13), exhibiting an IC50 value of ≤0.1 μM for estradiol. This compound selectively modulates steroid hormone metabolism and has significant implications for research in metabolic disorders and liver diseases. Its ability to influence estradiol levels makes it a valuable tool for studying hormone-related pathways and therapeutic strategies.
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HSD17B13-IN-99 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC50 value of less than 0.1 μM for estradiol. This compound demonstrates significant potential for investigating liver diseases, metabolic disorders, and cardiovascular conditions, including non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and drug-induced liver injury (DILI). Researchers can utilize HSD17B13-IN-99 to explore therapeutic strategies and mechanisms related to these health issues.
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HSD17B13-IN-22 is a selective inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13). This compound demonstrates significant biological activity in modulating lipid metabolism and is relevant in the study of liver-related disorders, including hepatitis, liver fibrosis, liver cirrhosis, and hepatocellular carcinoma. Its application in research enables a deeper understanding of HSD17B13's role in these conditions, potentially paving the way for therapeutic advancements.
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HSD17B13-IN-60 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC50 value of ≤ 0.1 μM for estradiol. This compound is primarily utilized in research related to liver and metabolic diseases, including non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and drug-induced liver injury (DILI). Its inhibition of HSD17B13 makes it a valuable tool for understanding the underlying mechanisms of these disorders and developing potential therapeutic strategies.
HSD17B13-IN-18 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC50 of less than 0.1 μM for estradiol and less than 1 μM for Leukotriene B3. This compound is significant in the context of nonalcoholic fatty liver diseases (NAFLDs), particularly in the study of nonalcoholic steatohepatitis (NASH). HSD17B13-IN-18 facilitates research aimed at understanding and potentially therapeutically targeting metabolic disorders related to liver function.
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3-Acetyl-7-Hydroxycoumarin is a selective inhibitor of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1). It exhibits significant biological activity, demonstrating 57% inhibition of 17β-HSD1 at a concentration of 6 μM. This compound is valuable for research applications focused on hormone-dependent diseases, including breast cancer and endometriosis.
HSD17B13-IN-94 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC50 value of ≤ 0.1 μM for estradiol. This compound is instrumental in the investigation of liver diseases, metabolic disorders, and cardiovascular conditions, including non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and drug-induced liver injury (DILI). Its selective inhibition of HSD17B13 provides valuable insights into the underlying mechanisms of these diseases.
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HSD17B13-IN-78 is a selective inhibitor of 17β-Hydroxysteroid dehydrogenase 13 (HSD17B13), exhibiting an IC50 of less than 0.1 μM for estradiol. This compound is primarily utilized in research focused on nonalcoholic fatty liver disease (NAFLD), aiding in the understanding of lipid metabolism and associated metabolic disorders. HSD17B13-IN-78 serves as an important tool for studying the therapeutic potential of targeting HSD17B13 in liver-related pathologies.
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S07-2005 (racemic) is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor, exhibiting an IC50 value of 0.13 μM for AKR1C3 and 0.75 μM for AKR1C4. This compound demonstrates significant potential as a chemotherapeutic potentiator, particularly in overcoming resistance mechanisms in cancer treatment. Its selectivity and efficacy make it a valuable tool for research applications focused on cancer biology and drug resistance mechanisms.
HSD17B13-IN-56-d3 is a selective inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC50 value of ≤ 0.1 μM for estradiol. This compound is valuable for investigating the role of HSD17B13 in liver diseases, metabolic disorders, and cardiovascular conditions, including non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and drug-induced liver injury (DILI). Its inhibitory action makes it a significant tool for exploring therapeutic strategies targeting these conditions.
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HSD17B13-IN-36 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC50 of less than 0.1 μM for estradiol as a substrate. This compound is significant in the study of nonalcoholic fatty liver diseases (NAFLDs), including nonalcoholic steatohepatitis (NASH), making it valuable for research concerning metabolic disorders and liver health. Its selective inhibition of HSD17B13 may provide insights into therapeutic interventions for liver-related diseases.
HSD17B13-IN-85 is a potent inhibitor of 17β-Hydroxysteroid dehydrogenase 13 (HSD17B13), exhibiting an IC50 of less than 0.1 μM for estradiol. This compound is primarily employed in the study of nonalcoholic fatty liver disease (NAFLD) and offers significant insights into the role of HSD17B13 in metabolic regulation and liver physiology. Its specific inhibition enhances understanding of the enzyme's contribution to various biological processes and potential therapeutic targets in liver-related disorders.
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HSD17B13-IN-84 is a potent inhibitor of the enzyme 17β-Hydroxysteroid dehydrogenase type 13 (HSD17B13), demonstrating an IC50 of less than 0.1 μM for estradiol. This compound is primarily utilized in research concerning nonalcoholic fatty liver disease (NAFLD), providing valuable insights into the role of HSD17B13 in lipid metabolism and liver pathophysiology. Its effective inhibition of HSD17B13 supports studies aimed at understanding disease mechanisms and potential therapeutic interventions.
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HSD17B13-IN-98 is a potent inhibitor of 17 β-hydroxysteroid dehydrogenase (HSD17B13), demonstrating an IC50 value for estradiol of less than 0.1 μM. This compound is particularly relevant in the investigation of nonalcoholic fatty liver disease, providing valuable insights into the biochemical pathways involved in lipid metabolism and liver function. Its specificity and efficacy make it an essential tool for research focused on metabolic disorders and related therapeutic strategies.
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HSD17B13-IN-59 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibiting an IC50 value of ≤ 0.1 μM for estradiol. This compound is valuable for research focused on liver diseases, metabolic disorders, and cardiovascular conditions, including non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and drug-induced liver injury (DILI). Its specific mechanism of action makes it an essential tool in elucidating the role of HSD17B13 in various pathophysiological contexts.
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7-Coumaryl triflate is a selective inhibitor of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1), demonstrating an IC₅₀ of 360 nM and a Kᵢ of 173 nM. This compound selectively targets 17β-HSD2 while displaying no significant affinity for estrogen receptors ERα or ERβ. 7-Coumaryl triflate is valuable for research focused on hormone-dependent breast cancer and the modulation of estrogen metabolism.
HSD17B13-IN-26 is a potent inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13). This compound exhibits significant activity in the modulation of steroid metabolism and demonstrates potential therapeutic applications in liver diseases, including hepatitis, liver fibrosis, liver cirrhosis, and hepatocellular carcinoma. Researchers can utilize HSD17B13-IN-26 to further investigate the role of HSD17B13 in liver pathology and associated metabolic disorders.
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