Steroid Sulfatase Inhibitor

Irosustat is a potent steroid sulfatase inhibitor, with an IC₅₀ of 8 nM, and exhibits anti-breast cancer activity.

Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent steroid sulfatase (STS) inhibitor. Estrone O-sulfamate has inhibitory activity for STS in a placental microsomes (P.M.) preparation and in MCF-7 cells with IC₅₀ values of 18 nM and 0.83 nM, respectively. Estrone O-sulfamate can be used for the research of cancer.

Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) is a potent, long-acting, and orally active steroid sulfatase inhibitor; inhibits estrone sulfatase with an IC₅₀ of 251 nM and a K_i of 133 nM.

Caspase-3/7 activator 4 is a caspase-3 activator and caspase-7 activator. Caspase-3/7 activator 4 inhibits key enzymes in estrogen biosynthesis, including aromatase (IC₅₀ = 38.3 nM) and steroid sulfatase (IC₅₀ = 12.7 µM), and selectively suppresses COX-2 (IC₅₀ = 5.38 µM). Caspase-3/7 activator 4 shows strong antioxidant activity (DPPH: IC₅₀ = 16.26 µM). Caspase-3/7 activator 4 inhibits estrogen synthesis, suppresses estrogen availability, reduces prostaglandin production, increases caspase-3/7 expression, induces G0/G1 cell cycle arrest, induces apoptotic cell death, reduces circulating TNF-α and VEGFR-II levels, restores hepatorenal function markers and histoarchitecture, restores antioxidant defense enzyme activity, reduces lipid peroxidation, exerts antiproliferative activity against breast cancer cells, exerts antitumor activity in the Ehrlich ascites carcinoma models. Caspase-3/7 activator 4 can be used for the research of breast cancer, ehrlich ascites carcinoma.

Steroid sulfatase-IN-12 is a steroid sulfatase inhibitor. Steroid sulfatase-IN-12 inhibits the activity of steroid sulfatase. Steroid sulfatase-IN-12 can be used in research related to hormone receptor-positive/HER2-negative breast cancer.

KW-2581 is a steroidal selective steroid sulfatase (STS) inhibitor with an IC₅₀ of 4 nM. KW-2581 inhibits STS activity of ZR-75-1 cells with an IC₅₀ of 13 nM. KW-2581 inhibits the E1S-stimulated growth of ZR-75-1 cells with an IC₅₀ of 0.18 nM. KW-2581 inhibits sulfated-estrogen dependent growth of breast cancer cells both in vitro and in vivo. KW-2581 induced regression in E1S-induced tumor growth. KW-2581 can be studied in research on hormone receptors-positive breast cancer.

Steroid sulfatase-IN-10 (Example 216) is a Steroid sulfatase inhibitor with an IC₅₀ of 0.03-0.27 µM . Steroid sulfatase-IN-10 can be used for inflammatory diseases such as rheumatoid arthritis, type 1 and 2 diabetes and systemic lupus erythematosus research.

Steroid sulfatase-IN-6 (Compound 10c) is an irreversible inhibitor of steroid sulfatase (STS). Steroid sulfatase-IN-6 has an K_i value of 0.4 nM for human placenta STS. Steroid sulfatase-IN-6 can be used for tumor diseases research.

SR-16157 (NSC 732011; HLX-801) is a dual-action steroid sulfatase (STS) inhibitor (IC₅₀ = 0.1 uM) and selective ERα modulator. SR-16157 exhibits STS inhibitory and anti-estrogenic effects in breast cancer cells. SR-16157 may be used in breast cancer research.

Steroid sulfatase/17β-HSD1-IN-3 (compound 19) is a dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). Steroid sulfatase/17β-HSD1-IN-3 irreversibly inhibits hSTS activity with anIC₅₀ value of 27 nM. Steroid sulfatase/17β-HSD1-IN-3 can be used in the study of endometriosis and other estrogen-dependent diseases.

Steroid sulfatase -IN-2 is an active steroid sulfatase (STS) inhibitor with an IC₅₀ value of 109.5 nM. Steroid sulfatase-IN-2 can be used for the research of hormone-dependent cancers, such as estrogen-dependent breast and endometrial cancer.

Steroid sulfatase-IN-8 (7) is a STS inhibitor with PM IC₅₀ value of 1 nM, JEG-3 IC₅₀ of 0.025 nM, respecively.

DU-14 is a potent steroid sulfatase inhibitor with an IC₅₀ of 55.8 nM. DU-14 inhibits the MCF-7 cell proliferation (IC₅₀ = 38.7 nM). DU-14 has neuroprotective effects against neurotoxic Aβ, suggesting that up-regulation of endogenous DHEAS by DU-14 could be beneficial to the alleviation of Aβ-induced impairments in spatial memory and synaptic plasticity.

Steroid sulfatase-IN-4 (Compound 16) is an irreversible steroid sulfatase (STS) inhibitor with an IC₅₀ of 25 nM against human STS. Steroid sulfatase-IN-4 can be used for the research of endometriosis.

Steroid sulfatase-IN-3 (compound 1q) is a potent STS (Steroid sulfatase) inhibitor, with an IC₅₀ of 25.8 nM. Steroid sulfatase-IN-3 shows antiproliferative activity against T-47D estrogen-dependent breast cancer cells, with an IC₅₀ of 1.04 µM.

Steroid sulfatase-IN-9 (compound 54E) is a steroid sulfatase (STS) inhibitor with the inhibition rates of 87.03% at 10 μM. Steroid sulfatase-IN-9 shows no detectable toxic effects in zebrafish larvae model.

Steroid sulfatase-IN-7 is an irreversible steroid sulfatase (STS) inhibitor with an IC₅₀ value of 0.05 nM against human placental STS and can be used in cancer research.

Steroid sulfatase-IN-1 is a potent and orally active Steroid sulfatase inhibitor with an IC₅₀ of 1.71 nM. Steroid sulfatase-IN-1 shows antitumor activity in vivo. Steroid sulfatase-IN-1 has the potential for the research of breast cancer.

Steroid sulfatase/17β-HSD1-IN-5 is a irreversible inhibitor of steroid sulfatase (STS) .Steroid sulfatase/17β-HSD1-IN-5 is a reversible and selective inhibitor of 7β-hydroxysteroid dehydrogenase type1 (17β-HSD1), with IC₅₀s of 43 nM and 6.2μM for 17β-HSD1 and 17β-HSD2, respectively. Steroid sulfatase/17β-HSD1-IN-5 can be used for metabolic disease (especially for endometriosis) research.

Steroid sulfatase-IN-5 (compound 10b) is a steroid sulfatase (STS) inhibitor (IC₅₀: 0.32 nM). Steroid sulfatase-IN-5 inhibits T-47D cell proliferation with an IC₅₀ of 35.7 μM. Steroid sulfatase-IN-5 can be used for research of breast cancer.