2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Cytochrome P450
  5. Aromatase/CYP19A1 Isoform

Aromatase/CYP19A1

Aromatase (estrogen synthetase, CYP19A1) is a unique cytochrome P450 that catalyzes the removal of the 19-methyl group and aromatization of the A-ring of androgens for the synthesis of estrogens. All human estrogens are synthesized via this enzymatic aromatization pathway. Aromatase is most widely known for its roles in reproduction and reproductive system diseases, and as a target for inhibitor therapy in estrogen-sensitive diseases including cancer, endometriosis, and leiomyoma.

The selective inhibition of estrogen production by aromatase inhibitors is an efficient strategy for breast cancer treatment. These compounds are classified as irreversible inhibitors of aromatase (type I), and comprise steroidal compounds. Reversible inhibitors of aromatase, which comprises non-steroidal compounds are type II aromatase inhibitors. Second and third generation aromatase inhibitors are considerably more potent and more specific in their ability to inhibit aromatase, as compared with first generation compounds (aminoglutethimide).

Aromatase/CYP19A1 Related Products (37):

Cat. No. Product Name Effect Purity
  • HY-14274S
    Anastrozole-d12
    		Inhibitor
    Anastrozole-d12 is the deuterium labeled Anastrozole. Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM[1][2].
  • HY-18719ES
    Endoxifen-d5
    		Inhibitor
    Endoxifen-d5 is the deuterium labeled Endoxifen. Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study[1][2].
  • HY-146688
    SYN20028567
    		Inhibitor
    SYN20028567 is an aromatase (CYP19) inhibitor with an IC50 of 9.4 nM. SYN20028567 can be used for breast cancer research.
  • HY-163680
    ERα degrader 9
    ERα degrader 9 is a dual targeting ligand for estrogen receptor α (ERα) and aromatase (ARO). ERα degrader 9 can be utilized for synthesis of PROTAC ERα Degrader-9 (HY-163679).
  • HY-151119
    Anticancer agent 78
    		Inhibitor
    Anticancer agent 78 is a potent anticancer agent. Anticancer agent 78 shows cytotoxicity. Anticancer agent 78 exhibits anti-aromatase activity with an IC50 value of 0.9 µM. Anticancer agent 78 has the potential for the research of breast cancer.
  • HY-13632S1
    Exemestane-13C3
    		Inhibitor
    Exemestane-13C3 is the 13C-labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].
  • HY-163679
    PROTAC ERα Degrader-9
    		Degrader
    PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7EGFR (IC50=0.075 μM), MCF-7D538G (IC50=0.31 μM), MCF-7Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
  • HY-13632S
    Exemestane-d2
    		Inhibitor
    Exemestane-d2 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].
  • HY-162105
    Aromatase-IN-3
    		Inhibitor
    Aromatase-IN-3 (compound 7d) is an aromatase inhibitor with an IC50 of 54 nM. Through suppressing the conversion of androstenedione to oestrogen caused by aromatase, Aromatase-IN-3 exerts an appreciable tumor growth inhibitory activities against breast cancer cell lines, suggesting its usage for ER+ cancer research.
  • HY-105184
    YM511
    		Inhibitor 99.73%
    YM511 is a highly specific non-steroidal aromatase inhibitor. YM511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM511 slightly inhibits production of other steroid hormones. YM511 has the potential for suppressing estrogen-dependent action research without affecting serum levels of other steroid hormones.
  • HY-13632S2
    Exemestane-d3
    		Inhibitor
    Exemestane-d3 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].
  • HY-152250
    Antibacterial agent 132
    		Inhibitor
    Antibacterial agent 132 has anticandidal effects against C. parapsilosis (ATCC 22019) and C. krusei (ATCC 6258) with MIC90 values of <0.06 μg/mL and 62.50 μg/mL, respectively. Antibacterial agent 132 inhibits aromatase enzyme with an IC50 of 0.047μM.
  • HY-W087008
    7-Hydroxyflavanone
    		Inhibitor 99.59%
    7-Hydroxyflavanone is a potent inhibitor of aromatase (CYP19) activity with the IC50 of 65 μM. 7-Hydroxyflavanone exerts various biological effects, including anticarcinogenic, antioxidant and (anti-)estrogenic effects, and modula
  • HY-144824
    Monoamine oxidase/Aromatase-IN-1
    		Inhibitor
    Monoamine oxidase/Aromatase-IN-1 (compound 2q) is a highly potent monoamine oxidase (MAO) and aromatase dual inhibitor with IC50s of 39 nM and 31 nM for MAO-B and aromatase, respectively. Monoamine oxidase/Aromatase-IN-1 can be used for researching neurological disorder and breast cancer.
  • HY-148430
    Aromatase-IN-2
    		Inhibitor 99.83%
    Aromatase-IN-2 is a potent aromatase inhibitor with an IC50 value of 1.5 µM.
  • HY-N8405
    Isolimonexic acid
    		Inhibitor
    Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC50=25.60 μM) properties.
  • HY-U00176
    Org30958
    		Inhibitor
    Org30958 is a potent aromatase inhibitor in vivo.