HSD17B13-IN-2 is a selective inhibitor of HSD17B13, demonstrating human IC50 values of 0.18 μM with β-estradiol and 0.25 μM with Leukotriene B4. This compound binds to the active site of HSD17B13 in an NAD+-dependent manner, interacting with the bound NAD+ cofactor to stabilize the HSD17B13 protein and prevent its aggregation. HSD17B13-IN-2 effectively reduces the conversion of β-estradiol to estrone in cellular assays, making it a valuable tool for investigating nonalcoholic fatty liver disease and related metabolic disorders.
HSD17B13-IN-2 is a selective inhibitor of HSD17B13, demonstrating human IC50 values of 0.18 μM with β-estradiol and 0.25 μM with Leukotriene B4. This compound binds to the active site of HSD17B13 in an NAD+-dependent manner, interacting with the bound NAD+ cofactor to stabilize the HSD17B13 protein and prevent its aggregation. HSD17B13-IN-2 effectively reduces the conversion of β-estradiol to estrone in cellular assays, making it a valuable tool for investigating nonalcoholic fatty liver disease and related metabolic disorders.
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