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 (56):

Cat. No. Product Name Effect Purity
  • HY-14248
    Letrozole
    		Inhibitor 99.95%
    Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.
  • HY-N0292
    Oleuropein
    		Inhibitor 99.97%
    Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.
  • HY-13632
    Exemestane
    		Inhibitor 99.97%
    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.
  • HY-14274
    Anastrozole
    		Inhibitor 99.95%
    Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
  • HY-125833
    Alpha-Naphthoflavone
    		Inhibitor 99.76%
    Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis.
  • HY-180535
    Aromatase-IN-8
    		Inhibitor
    Aromatase-IN-8 is a selective Aromatase inhibitor against an IC50 of 0.05 µM. Aromatase-IN-8 exhibits selective antiproliferative effects against estrogen receptor-positive breast cancer cell lines, while showing no toxicity toward non-tumoral cells. Aromatase-IN-8 suppresses estrogen active, increases testosterone levels, and downregulates estrogen receptor expression and phosphorylation. Aromatase-IN-8 can be used for triple negative breast cancer research.
  • HY-180420
    Tan-931
    		Inhibitor
    Tan-931 is a non-competitive and selective inhibitor of aromatase , with an IC50 is 17.2 μM and a Ki of 40 μM for human aromatase, and an IC50 of 162 μM for rat aromatase. Tan-931 reduces plasma estradiol-17β level and weight of ovaries and uterus in PMSG (HY-N12634)-treated female rats. Tan-931 can be used for the research of estrogen-dependent metastatic breast cancer.
  • HY-182708
    CGS 18320B
    		Inhibitor
    CGS 18320B is a human placental microsomal aromatase inhibitor with a Ki of 0.16 nM. CGS 18320B interacts reversibly with the enzyme's active site to block estrogen biosynthesis from androstenedione. CGS 18320B can be used for the research of aromatase inhibition and estrogen biosynthesis regulation.
  • HY-18719E
    Endoxifen
    		Inhibitor 99.51%
    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.
  • HY-14247
    Fadrozole hydrochloride
    		Inhibitor 99.91%
    Fadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
  • HY-W007664
    (R)-4-Benzyl-2-oxazolidinone
    		Inhibitor 99.83%
    (R)-4-Benzyl-2-oxazolidinone is an oxazolidinone-type auxiliary that enables highly stereoselective asymmetric alkylation reactions. (R)-4-Benzyl-2-oxazolidinone is applied in the total synthesis of natural products and pharmaceutical preparations. Especially in pharmaceutical research and development, (R)-4-Benzyl-2-oxazolidinone not only serves as a key precursor for the synthesis of aromatase inhibitors, but also can be used in studies related to estrogen-dependent breast cancer.
  • HY-N7005
    Clitorin
    		Inhibitor 99.45%
    Clitorin is an orally active flavonoid compound that can be isolated from Carica papaya. Clitorin is an inhibitor of EGFR (IC50: 89.58 nM) and aromatase (IC50: 77.41 nM). Clitorin has antioxidant and anti-tumor activities. In the DPPH and ABTS radical scavenging assays, Clitorin has IC50 values of 91.96 ppm and 250.45 ppm, respectively. In addition, Clitorin can regulate lipogenesis and fatty acid oxidation and can be used in the research of non-alcoholic fatty liver disease.
  • HY-18719B
    Endoxifen hydrochloride
    		Inhibitor 98.04%
    Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study.
  • HY-14247A
    Fadrozole
    		Inhibitor 99.78%
    Fadrozole (CGS 16949A free base) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
  • HY-N7128
    Flavanone
    		Inhibitor 99.73%
    Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). Flavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy.
  • HY-B0237
    Aminoglutethimide
    		Inhibitor 98.87%
    Aminoglutethimide (DL-Aminoglutethimide) is an orally active anticonvulsant with various endocrine-related side effects. Aminoglutethimide blocks multiple steroid hormone synthesis pathways by inhibiting several cytochrome P-450-dependent hydroxylases, such as aromatase, cholesterol side-chain cleavage enzyme, 11-hydroxylase, and 18-hydroxylase, with IC50 values of 0.3, 3.5, 120, and 20 μM, respectively. Aminoglutethimide reduces cortisol levels. Aminoglutethimide can be used in research on Cushing's syndrome, breast cancer, and other conditions.
  • HY-133668
    Monoethyl phthalate
    		Activator 98.58%
    Monoethyl phthalate is an orally active PDX-1 activator and the major hydrolytic metabolite of Diethyl phthalate (HY-Y0284) in vivo, with reproductive toxicity. Monoethyl phthalate targets aromatase (aromatase/CYP19A1) and PPAR to induce cell proliferation. The plasma protein binding rate of Monoethyl phthalate in rats and humans is lower than that of Diethyl phthalate. It exhibits significant enterohepatic circulation in rats and mainly accumulates in liver tissues. Monoethyl phthalate shows no estrogenic activity in estrogen-dependent human breast cancer cells. Monoethyl phthalate can be used in studies of reproductive toxicity and related environmental endocrine disruption mechanisms.
  • HY-150775
    CYP19A1-IN-2
    		Inhibitor 99.31%
    CYP19A1-IN-2 (Compound 13h) is a nonsteroidal aromatase (CYP19A1) inhibitor (IC50=0.09 nM). CYP19A1-IN-2 has potential for breast cancer research. CYP19A1-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-W392925
    (R)-(+)-Aminoglutethimide
    		Inhibitor
    (R)-(+)-Aminoglutethimide is a potent and orally active aromatase inhibitor. (R)-(+)-Aminoglutethimide has the potential for the research of breast cancer.
  • HY-13632R
    Exemestane (Standard)
    		Inhibitor
    Exemestane (Standard) is the analytical standard of Exemestane. This product is intended for research and analytical applications. 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.