er modulator

27-Hydroxycholesterol (25(R)-27-hydroxy Cholesterol) is a selective modulator of estrogen receptor and an agonist of the liver X receptor.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Tamoxifen Citrate is an orally active selective estrogen receptor modulator (SERM) that blocks estrogen activity in breast cells while activating estrogen signaling in cells such as those of the bone, liver, and uterus. As an Hsp90 activator, it enhances the ATPase activity of the Hsp90 chaperone complex, induces autophagy and apoptosis, and can be used to generate gene knockout models in CreER(T2) transgenic mice as well as liver injury models.

Nur77 modulator 1 is an effective Nur77 binder (KD = 3.58 μM) that up-regulates Nur77 expression, mediates its sub-cellular localization, induces Nur77-dependent ER stress and autophagy, and leads to cell apoptosis, demonstrating anti-hepatoma activity.

TAS-108 (also known as SR-16234) is a selective estrogen receptor modulator (SERM) reported to exhibit antagonistic activity towards estrogen receptor (ER) α, while demonstrating high affinity and weak partial agonistic activity for the ERβ receptor.

(E/Z)-Droloxifene is a mixture comprising (E)-Droloxifene, known as a selective estrogen receptor modulator, and (Z)-Droloxifene. (E)-Droloxifene binds to estrogen receptors (ER) in rabbit uterine homogenate with an IC50 of 24 nM. It increases uterine weight in immature rats and reduces the uterine weight increase caused by estradiol in juvenile rats. Additionally, (E)-Droloxifene inhibits the growth of human breast cancer cells MCF-7, ZR-75-1, and T47D stimulated by 17β-estradiol. In contrast, (Z)-Droloxifene shows weak binding to ER and exhibits neither estrogenic nor anti-estrogenic activity.

Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. It significantly promotes Nur77 expression and apoptosis, exhibiting excellent growth inhibitory effects on HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, leading to apoptosis. This compound is applicable in cancer research.

TFR4OHT is a selective ER modulator (SERM).

KUS121 is a valosin-containing protein modulator that inhibits VCP ATPase activity with an IC50 of 330 nM, suppresses tunicamycin-induced ATP depletion, cell death, and CHOP upregulation in HeLa cells, protects primary cortical neurons from oxygen-glucose deprivation injury in vitro, reduces infarct volume and improves motor performance in mouse models of focal cerebral ischemia, and preserves retinal structure and visual function in rd10 retinitis pigmentosa models, supporting its investigation in neuroprotection and ischemic disease research.

Estrogen receptor modulator 6 (compound 3a) is a highly specific and potent agonist of the estrogen receptor (ER) β, exhibiting remarkable affinity (K i = 0.44 nM) and impressive 19-fold selectivity for ERβ over ERα, as evidenced by its affinity (K i = 8.4 nM).

SNG-1153 is a estrogen receptor ER-alpha36 modulator.

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.

D 15414 is a nonsteroidal weak estrogen of the 2-phenylindole group which was never marketed. It is the major metabolite of the selective estrogen receptor modulator zindoxifene. D-15414 has high affinity for the estrogen receptor and inhibits the growth of ER-positive MCF-7 breast cancer cells in vitro.

ER degrader 6 (compound 35s) is a potent selective estrogen receptor modulator (SERM) with the capacity to degrade Estrogen Receptor (ER)α. It disrupts the microtubule network, inhibits tubulin polymerization, and effectively suppresses tumor growth with minimal toxicity [1].

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer research [1].

ER proteostasis regulator-1 is an effective modulator of ER proteostasis. It balances the UPR pathway to reduce misfolded protein accumulation, protecting cells from proteotoxicity in neurodegenerative disease research.

CT-08 (CT8, Compound 3) is a macrolide Sec61 modulator that inhibits protein secretion in a signal sequence-dependent manner. It prevents the Sec61-mediated translocation of VCAMss-GLuc to the ER, resulting in the loss of luciferase activity. Additionally, CT-08 suppresses the expression of VCAM in transfected cells.