enzyme modulator

GSM-1 is a modulator of γ-Secretase.

Autotaxin modulator 1 (compound 12b) is an autotaxin (ATX) enzyme inhibitor applicable for studying demyelination and tumours.

CA-170 is an orally bioavailable dual inhibitor of VISTA and PD-L1 that selectively restores T-cell proliferation and effector function suppressed by immune checkpoint signaling, while demonstrating minimal off-target activity across a broad receptor and enzyme panel, making CA-170 a valuable compound for immuno-oncology research and immune checkpoint modulation studies.

N-Acetyl-D-proline is a reagent used in biochemical research and is often employed as an allosteric modulator of enzymes to explore the regulatory mechanism of enzyme activity.

OMJ-4 is a modulator of mutant α-mannosidase (alpha-mannosidase). It restores the catalytic function of the mutant α-mannosidase and enhances substrate binding capability by altering its compactness and active site flexibility. Acting as a substrate reactivity inducer, OMJ-4 increases the reactivity of mannose disaccharides binding to mutant α-mannosidase and lowers the activation energy required for the enzyme-catalyzed reaction. OMJ-4 is useful for research related to α-mannosidosis.

Galeterone (VN 124) is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17, 20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

Ketogestin (11-Ketoprogesterone，11KP4) is a progestational steroid used in the synthesis of hormone-related drugs.Ketogestin acts through membrane glucocorticoid receptors and is an inhibitor of enzyme 11β-hydroxysteroid dehydrogenase. It acts through membrane glucocorticoid receptors, is an inhibitor of enzyme 11β-hydroxysteroid dehydrogenase, and also acts as a weak negative modulator of GABAA receptors.

Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is a chemical that is under development for estrogen receptor-positive breast cancer. It is also being evaluated as an antipsychotic for treatment of mania and other psychotic disorders. Endoxifen is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group. It is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce afimoxifene (4-hydroxytamoxifen) and endoxifen.