ERR
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB17185 | ZK 164015 | 177583-70-9 | ZK 164015 is an antagonist of estrogen receptor. It inhibits 17β-estradiol stimulation of luciferase activity with IC50 of 0.025 μM. |
| FB07651 | WAY200070 | 440122-66-7 | WAY200070 selectively activates ERβ (EC50 = 2 nM) receptor over ERα (EC50 = 155 nM). It shows anti-depressive and anti-anxiolytic activities. |
| FB03573 | Tracheloside | 33464-71-0 | Tracheloside, a natural product isolated and purified from the herbs of Trachelospermum jasminoides (Lindl.) Lem., significantly decreases the activity of alkaline phosphatase (AP), an estrogen-inducible marker enzyme, with an IC50 value of 0.31 mg/mL, a level of inhibition comparable to that of tamoxifen (IC50 = 0.43 mg/mL). |
| FB12102 | TR Antagonist 1 | 500794-88-7 | TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively. |
| FB11627 | Tetrahydrofluoroene 52 | 1398510-92-3 | Tetrahydrofluoroene 52 is a potent and selective estrogen receptor β agonist. |
| FB16487 | SR19881 | 2213490-89-0 | SR19881 is a ERRγ agonist. |
| FB11882 | SNIPER(ER)-110 | 2241690-03-7 | SNIPER(ER)-110 is a nongenetic IAP-dependent protein eraser (SNIPER) targeting estrogen receptor α (ERα), induces ERα degradation and induces apoptosis in MCF-7 human breast cancer cells; inhibits the growth of MCF-7 tumor xenografts in mice more potently than the previously characterized SNIPER(ER)-87, preferentially recruits XIAP, rather than cIAP1, to degrade ERα. |
| FB11759 | MPP 2HCl | 911295-24-4 | Selective, high affinity silent antagonist at ERα receptors. Displays > 200-fold selectivity for ERα over ERβ. Ki values are 2.7 and 1800 nM at ERα and ERβ receptors respectively. |
| FB12751 | Y 134 | 849662-80-2 | Selective estrogen receptor modulator (SERM), selective for ERα |
| FB19579 | PROTAC ERα Degrader-2 | 1351169-29-3 | PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs). |
| FB15482 | PROTAC ERα Degrader-1 | N/A | PROTAC ERα Degrader-1 is a PROTAC targeting ERα. |
| FB06175 | Prinaberel | 524684-52-4 | Prinaberel is an agonist of ERβ. |
| FB10920 | PHTPP | 805239-56-9 | PHTPP has selective antagonism of estrogen ERβ receptor . |
| FB11922 | PAC1 | 2158322-33-7 | PAC1 (Compound PAC1) is a PROTAC antibody conjugate, more potent estrogen receptor-alpha (ERα) degrader compared to PROTAC without antibody conjugation. |
| FB09355 | Ormeloxifene | 31477-60-8 | Ormeloxifene, an estrogen receptor regulator, suppresses prostate tumor growth and metastatic phenotypes via inhibition of oncogenic β-catenin signaling and EMT progression |
| FB07602 | Nitromifene | 10448-84-7 | Nitromifene is an antagonist of estrogen receptor (ER). |
| FB12792 | Lynestrenol | 52-76-6 | Lynestrenol is a progesterone receptor agonist. It is synthetic progestational hormone. |
| FB11535 | LSZ102 | 2135600-76-7 | LSZ102 is a potent ERα antagonist and degrader. LSZ102 showed ERα degradation IC50 = 0.2 nM. LSZ102 demonstrated IC50 for MCF-7 cells = 1.7 nM. Upon administration of LSZ102, this agent binds to the ER and induces the degradation of the receptor. This prevents ER activation and ER-mediated signaling, and inhibits the growth and survival of ER-expressing cancer cells. |
| FB12588 | GSK 4716 | 101574-65-6 | GSK4716 is an agonist of ERRβ/γ with IC50 of 2 µM with similar potency as the protein ligand PGC-1α. |
| FB11534 | GDC-0927 | 1642297-01-5 | GDC-0927, also known as SRN-927, is a next-generation oral SERD, appears to have greater potential than GDC-0810 to be a best-in-class SERD molecule. |
| FB12009 | GC 14 | 447415-34-1 | GC 14 is a selective agonist of thyroid hormone β1 activation (TRβ1) with an EC50 of 680 nM. |
| FB12197 | FERb 033 | 1111084-78-6 | FERb 033 is a potent and selective ERβ receptor agonist with Ki of 7.1 nM and EC50 of 4.8 nM. |
| FB16507 | Estrogen receptor modulator 1 | 63676-22-2 | Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. It has been found to be both estrogenic and antiproliferative in ER-positive endocrine-resistant breast cancer cell lines that overexpress protein kinase C alpha (PKCα). |
| FB17969 | ERRα antagonist-1 | 1072145-33-5 | ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1. |
| FB09862 | ERB-196 | 550997-55-2 | ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist. |
| FB02031 | Eprotirome | 355129-15-6 | Eprotirome is a liver-selective thyroid hormone receptor agonist. |
| FB01940 | Endoxifen Z-Isomer HCl | 1032008-74-4 | Endoxifen Z-isomer HCl is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen Z-isomer HCl inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM. |
| FB02267 | Endoxifen Z-Isomer | 112093-28-4 | Endoxifen is the most important tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). |
| FB10785 | Endoxifen HCl | 1197194-41-4 | Endoxifen HCl, the active metabolite of Tamoxifen, is a potent antiestrogen that targets estrogen receptor. |
| FB10107 | Endoxifen E-Isomer | 114828-90-9 | Endoxifen E-isomer is the E-isomer of (Z)-Endoxifen, which is an active metabolite generated via actions of CYP3A4/5 and CYP2D6, is a more potent selective estrogen receptor modulator (SERM) than Tamoxifen. |
| FB02338 | Endoxifen E-isomer HCl | 1197194-61-8 | Endoxifen E-isomer HCl is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM). |
| FB10879 | Elacestrant | 722533-56-4 | Elacestrant is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. |
| FB10880 | Elacestrant 2HCl | 1349723-93-8 | Elacestrant 2HCl is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. |
| FB12300 | Eeyarestatin I | 412960-54-4 | Eeyarestatin I is a potent inhibitor of endoplasmic reticulum associated protein degradation (ERAD). |
| FB17937 | Dihydroresveratrol | 58436-28-5 | Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations. |
| FB07198 | Daidzein | 486-66-8 | Daidzein can act as an inhibitor of tyrosine kinase and an activator of estrogen receptor. It is inactive analogue of genistein. |
| FB05231 | Cristacarpin | 74515-47-2 | Cristacarpin, a natural product isolated and purified from the herbs of Erythrina burana, exhibits moderate but selective activity towards DNA repair-deficient yeast mutants, and promotes endoplasmic reticulum (ER) stress, leading to sub-lethal reactive oxygen species (ROS) generation and which eventually terminates by triggering senescence in pancreatic and breast cancer cells through blocking the cell cycle in the G1 phase. |
| FB10605 | Clomiphene Citrate | 50-41-9 | Clomifene citrate is a modulator of estrogen receptor Erα (Ki = 0.9 nM) and Erβ (Ki = 1.2 nM). It has been used to treat ovulation induction. |
| FB06193 | BHPI | 56632-39-4 | BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression and elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis. |
| FB09954 | Bazedoxifene HCl | 198480-56-7 | Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). |
| FB03959 | AZD9496 Maleate | 1639042-28-6 | AZD9496 maleate is a potent and orally bioavailable selective estrogen receptor downregulator (Ki=0.7 nM) and antagonist. |
| FB03958 | AZD9496 | 1639042-08-2 | AZD9496 is a selective antagonist of estrogen receptor Erα (IC50 = 0.28 nM). |
| FB11962 | Arzoxifene HCl | 182133-27-3 | Arzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol. |
| FB18865 | ARV-471 | 2614417-52-4 | ARV-471 is the first-clinical-entered ERα PROTAC degrader with DC50 of ~1nM. It degrades clinically-relevant ESR1 variants (Y537S and D538G) and inhibits growth of cell lines expressing those variants. |
| FB11950 | Acolbifene | 182167-02-8 | Acolbifene (EM652) is a fourth-generation selective estrogen receptor antagonist with a LC50 value of 22±3 nM. |
| FB12235 | AC 186 | 1421854-16-1 | AC 186 is a potent and selective ERβ agonist with EC50 of 6 nM. |
| FB10602 | 4-Hydroxytamoxifen | 68047-06-3 | 4-Hydroxytamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. |
| FB10746 | 4,4-DDE | 72-55-9 | 4,4-DDE is an organochlorine pesticide and may behave as a potent androgen receptor antagonist. |
| FB12215 | (R,R)-THC | 138090-06-9 | (R,R)-THC is a selective estrogen receptor ligand that agonist at ERα receptor (Ki = 9.0 nM) and antagonist at ERβ receptor (Ki = 3.6 nM). |
| FB18102 | Afimoxifene | 68392-35-8 |