Search Result
Results for "
ER cancer
" in MedChemExpress (MCE) Product Catalog:
11
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-103457
-
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Estrogen Receptor/ERR
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Cancer
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Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .
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-
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- HY-141551
-
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Estrogen Receptor/ERR
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Cancer
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GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
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- HY-19822A
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RAD1901 dihydrochloride
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Estrogen Receptor/ERR
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Cancer
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Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo .
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-
-
- HY-19822
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RAD1901
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Estrogen Receptor/ERR
|
Cancer
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Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo .
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-
-
- HY-133017
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SAR439859
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Estrogen Receptor/ERR
|
Cancer
|
SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC50 of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER + breast cancer.
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-
-
- HY-128707
-
|
Caspase
Apoptosis
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Cancer
|
Z-LEVD-FMK is a cell-permeable caspase-4 inhibitor. Z-LEVD-FMK blocks ER stress-induced apoptosis in cancer cells .
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-
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- HY-168101
-
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Estrogen Receptor/ERR
|
Cancer
|
ERα degrader 11 (compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to investigate ER status in ER-positive breast cancer cells .
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-
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- HY-163812
-
|
Molecular Glues
Estrogen Receptor/ERR
|
Cancer
|
ER degrader 9 (compound 1), a bifunctional molecular glue, is a potent estrogen receptor (ER) degrader with a DC50 of ≤10 nM in MCF-7 cells. ER degrader 9 can be used for the research of breast cancer .
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-
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- HY-126932
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Estrogen Receptor/ERR
|
Cancer
|
TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three TR ER+ breast cancer cell cultures in 3D. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites, mimicking the actions of E2 .
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-
-
- HY-19822S2
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RAD1901-d10
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Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Cancer
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Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
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-
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- HY-149480
-
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PROTACs
Estrogen Receptor/ERR
|
Cancer
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ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
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-
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- HY-167868
-
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TRP Channel
Apoptosis
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Neurological Disease
Cancer
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DWP-05195 is a TRPV1 antagonist that can inhibit the pain signal transduction. DWP-05195 induces ER stress-dependent apoptosis through the ROS-p38-CHOP pathway in human ovarian cancer cells .
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- HY-123024
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BL-S-640; SK&F 60771
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Apoptosis
Bacterial
Antibiotic
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Infection
Cancer
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Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection .
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- HY-136528
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Deubiquitinase
Apoptosis
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Cancer
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RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells .
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- HY-138364
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YUM70
1 Publications Verification
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HSP
Apoptosis
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Cancer
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YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model .
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- HY-155158
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Ferroptosis
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Cancer
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Anticancer agent 147 (compound 6j) is a derivative of sophoridine (HY-N1373) and is a ferroptosis inducer. Anticancer agent 147 can promote the accumulation of intracellular Fe2+, reactive oxygen species (ROS) and MDA, increase ER stress, and upregulate the expression of the activating transcription factor ATF3. Anticancer agent 147 has good anti-liver cancer effects in vitro and in vivo .
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- HY-149970
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Estrogen Receptor/ERR
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Cancer
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ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer .
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- HY-149295
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PROTACs
Estrogen Receptor/ERR
Apoptosis
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Cancer
|
PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER + breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
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- HY-42484
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Microtubule/Tubulin
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Cancer
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ER-076349 is an inhibitor of tubulin polymerization, induces G2-M cell cycle arrest, and disrupts mitotic spindles. ER-076349 inhibits cancer cell growth, and inhibits tumor growth in several human tumor xenografts. ER-076349 is an analog of Halichondrin B .
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- HY-145073
-
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PROTACs
Estrogen Receptor/ERR
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Cancer
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PROTAC ER Degrader-10 is a potent PROTAC ER degrader and can be used for cancer research. PROTAC ER Degrader-10 is extracted from patent WO2021133886, example 36.
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- HY-137144
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ZB716
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Estrogen Receptor/ERR
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Cancer
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Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells .
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- HY-168099
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Estrogen Receptor/ERR
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Cancer
|
ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer .
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- HY-145572
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LY-3484356
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Estrogen Receptor/ERR
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Cancer
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Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .
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- HY-145572A
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LY-3484356 tosylate
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Estrogen Receptor/ERR
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Cancer
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Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .
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-
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- HY-149081
-
|
Estrogen Receptor/ERR
Cytochrome P450
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Cancer
|
ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .
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- HY-14933
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ERB-041
|
Estrogen Receptor/ERR
Wnt
Apoptosis
|
Cancer
|
Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis .
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- HY-151230
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Estrogen Receptor/ERR
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Cancer
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(-)-Erteberel is a selective estrogen receptor beta (ERβ) agonist. (-)-Erteberel can be utilized in the study of diseases mediated by estrogen receptor beta (ERβ), such as prostate cancer .
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- HY-136255
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AZD-9833
|
Estrogen Receptor/ERR
|
Cancer
|
Camizestrant (AZD-9833) is a potent and orally active estrogen receptor (ER) antagonist. Camizestrant is used for the study of ER + HER2-advanced breast cancer .
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- HY-142926
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Estrogen Receptor/ERR
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Cancer
|
ER degrader 2 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 2 has the potential for the research of cancer diseases (extracted from patent CN112830919A, compound 1) .
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- HY-169903
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Apoptosis
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Cancer
|
SMIP34 is a PELP1 inhibitor. SMIP34 binds to PELP1 with a Kd of 37.4 μM. SMIP34 inhibits cancer cell proliferation and tumor progression. SMIP34 can be used for breast cancer research, and is active against wild-type (WT), mutant (MT) ER + and therapy-resistant (TR)-ER + breast cancer .
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-
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- HY-142925
-
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Estrogen Receptor/ERR
|
Cancer
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ER degrader 1 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 1 has the potential for the research of cancer diseases (extracted from patent WO2021139756A1, compound 11) .
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- HY-142927
-
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Estrogen Receptor/ERR
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Cancer
|
ER degrader 3 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 3 has the potential for the research of cancer diseases (extracted from patent WO2018233591A1, compound 1) .
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-
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- HY-144070A
-
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Estrogen Receptor/ERR
|
Cancer
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(Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP againsts ERα+ breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1) .
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- HY-131404
-
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Estrogen Receptor/ERR
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Cancer
|
TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth .
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- HY-168270
-
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PROTACs
Estrogen Receptor/ERR
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Cancer
|
PROTAC ER Degrader-11 (Example 26-1) is a potent PROTAC ER degrader, with the IC50 of 0.66 nM. PROTAC ER Degrader-11 plays an important role in cancer research(Sturcture Note:(Blue: Cereblon ligand (HY-W797329), Black: linker (HY-W262798);Pink: ER ligand (HY-168271)) .
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-
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- HY-P10393
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ERα (295-311)
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Apoptosis
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Cancer
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ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
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- HY-19822S3
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RAD1901-d6
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
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- HY-155492
-
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Estrogen Receptor/ERR
|
Cancer
|
ERα degrader 7 (compound B1) is a potent ERα degrader with an IC50 of 14.6 nM and a DC50 of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research .
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-
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- HY-128600
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ERD-308
1 Publications Verification
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PROTACs
Estrogen Receptor/ERR
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Cancer
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ERD-308 is a highly potent von Hippel-Lindau-based PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively) .
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-
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- HY-19822S
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RAD1901-d4
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
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Cancer
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Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
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-
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- HY-B0723
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FC-1271a
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Estrogen Receptor/ERR
|
Cancer
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Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer .
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-
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- HY-155197
-
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Microtubule/Tubulin
Estrogen Receptor/ERR
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Cancer
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ER degrader 7 (Compound 35t) is an ERα and ERβ degrader. ER degrader 7 inhibits tubulin polymerization. ER degrader 7 inhibits cell viability with IC50s of 0.06, 2.56, 15.84, 1.59, 1.67, 1.37 μM for MCF-7, T47D, MCF-10A, LCC2, T47D D538G, and T47D Y537S cells respectively. ER degrader 7 also inhibits breast cancer tumor growth .
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-
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- HY-146440
-
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Histone Demethylase
Estrogen Receptor/ERR
Apoptosis
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Cancer
|
LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM .
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- HY-144306
-
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Estrogen Receptor/ERR
Apoptosis
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Cancer
|
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
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- HY-132194
-
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Estrogen Receptor/ERR
|
Cancer
|
ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER + breast cancer research .
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- HY-A0281
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4-PBA; Benzenebutyric acid
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HDAC
Virus Protease
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Infection
Cancer
|
4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
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-
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- HY-15654
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4-PBA sodium; 4-Phenylbutyric acid sodium; Benzenebutyric acid sodium
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HDAC
Autophagy
Apoptosis
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Cancer
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Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research .
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-
-
- HY-132294
-
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Estrogen Receptor/ERR
|
Cancer
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GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer .
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-
-
- HY-119418
-
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Estrogen Receptor/ERR
|
Cancer
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Desketoraloxifene is an estrogen receptors alpha (ERα) activator at an AP-1 site. Desketoraloxifene can be used for the research of osteoporosis and breast cancer .
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-
-
- HY-10426
-
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Estrogen Receptor/ERR
Autophagy
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Cancer
|
XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ .
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- HY-B0412
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Estriol
4 Publications Verification
Oestriol
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Estrogen Receptor/ERR
Endogenous Metabolite
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Cancer
|
Estriol (Oestriol), an orally active estrogen, is a ERα and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .
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- HY-A0098
-
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Bacterial
Fungal
Influenza Virus
Antibiotic
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Infection
Inflammation/Immunology
Cancer
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Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity .Tunicamycin increases exosome release in cervical cancer cells .
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- HY-138642
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ARV-471
|
PROTACs
Estrogen Receptor/ERR
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Cancer
|
Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
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- HY-A0031S
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TSE-424-d4
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
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- HY-A0031S2
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TSE-424-d4 acetate
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Estrogen Receptor/ERR
|
Cancer
|
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
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- HY-132294A
-
|
Estrogen Receptor/ERR
|
Cancer
|
(1S,3R)-GNE-502 (compound 179) is a potent ERα degrader with an EC50 value of 13 nM against ERα in MCF7 HCS. (1S,3R)-GNE-502 can be used to research cancer related with estrogen receptor .
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- HY-18719A
-
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Estrogen Receptor/ERR
Potassium Channel
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Cancer
|
Endoxifen Z-isomer hydrochloride 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).
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-
- HY-N1443
-
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Endogenous Metabolite
Apoptosis
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Metabolic Disease
Cancer
|
Demethylcantharidate disodium, an endogenous metabolite, induces apoptosis in hepatocellular carcinoma cells via ER stress. Demethylcantharidate disodium shows excellent anticancer activity against multiple types of cancer .
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- HY-161253
-
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Estrogen Receptor/ERR
|
Cancer
|
OSU-ERb-12 is a ERβ agonist, and suppress ovarian cancer cell proliferation in vitro and in vivo. OSU-ERb-12 decreases the expression of Snail .
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- HY-138642A
-
(Rac)-ARV-471
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Estrogen Receptor/ERR
PROTACs
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Cancer
|
(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
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- HY-N0878
-
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation .
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-
- HY-U00141
-
α-Hydroxylinoleic acid
|
Autophagy
|
Metabolic Disease
|
ABTL-0812 (α-Hydroxylinoleic acid) induces endoplasmic reticulum (ER) stress-mediated autophagy. ABTL-0812 is a first-in-class small molecule with anti-cancer activity .
|
-
- HY-A0036
-
TSE-424 acetate
|
Estrogen Receptor/ERR
|
Cancer
|
Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
|
-
- HY-169367
-
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
ERD-1233 is a potent and orally active estrogen receptor PROTAC degrader, with the DC50 of 0.9 nM. ERD-1233 plays an important role in ER + breast cancer research .
|
-
- HY-A0031
-
TSE-424
|
Estrogen Receptor/ERR
|
Cancer
|
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
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-
- HY-147402
-
D-0502
|
Estrogen Receptor/ERR
|
Cancer
|
Taragarestrant (D-0502) is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant shows potent activity in various ER+ breast cancer cell lines and xenograft models .
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-
- HY-A0031A
-
TSE-424 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer .
|
-
- HY-112596
-
|
Estrogen Receptor/ERR
|
Cancer
|
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer .
|
-
- HY-112596A
-
|
Estrogen Receptor/ERR
|
Cancer
|
H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer .
|
-
- HY-132247
-
|
Others
|
Cancer
|
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer .
|
-
- HY-15654S
-
4-PBA-d11 sodium; 4-Phenylbutyric acid-d11 sodium; Benzenebutyric acid-d11 sodium
|
Isotope-Labeled Compounds
HDAC
Autophagy
Apoptosis
|
Cancer
|
Phenylbutyrate-d11 (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[1].
|
-
- HY-114631
-
|
Estrogen Receptor/ERR
|
Cancer
|
EM-800, an orally active anti-estrogen, serves as an antagonist to the transcriptional functions of estrogen receptors α (ERα) and β (ERβ). EM-800 possesses anticancer activity, capable of inhibiting the growth of breast cancer induced by 7,12-Dimethylbenz[a]anthracene (DMBA) (HY-W011845). Furthermore, in ovariectomized animals, EM-800 effectively slows down bone loss. Additionally, EM-800 shows potential in the research of breast and endometrial cancers, while exerting beneficial effects on bone and lipid metabolism .
|
-
- HY-162105
-
|
Cytochrome P450
|
Endocrinology
Cancer
|
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-A0281S
-
4-PBA-d11; Benzenebutyric acid-d11
|
HDAC
Virus Protease
|
Infection
Cancer
|
4-Phenylbutyric acid-d11 is the deuterium labeled 4-Phenylbutyric acid. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
|
-
- HY-143253
-
|
Estrogen Receptor/ERR
|
Cancer
|
Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities .
|
-
- HY-147402A
-
D-0502 meglumine
|
Estrogen Receptor/ERR
|
Cancer
|
Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models .
|
-
- HY-148368
-
|
Bcl-2 Family
Apoptosis
|
Cancer
|
CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis .
|
-
- HY-W011241
-
(8R,9S)-Cinchonine hydrochloride; LA40221 hydrochloride
|
Apoptosis
Parasite
|
Cancer
|
Cinchonine hydrochloride ((8R,9S)-Cinchonine hydrochloride) is a natural alkaloid present in Cinchona bark, with antimalarial activity. Cinchonine hydrochloride activates endoplasmic reticulum (ER) stress-induced apoptosis in human liver cancer cells .
|
-
- HY-162129
-
|
Photosensitizer
|
Cancer
|
Antitumor agent-131 (Compound 2-p) is an ER fluorescent probe with an IC50 value of 23 nM for HepG2 tumor cells. Antitumor agent-131 can be used as a photosensitizer for the study of cancer photodynamics .
|
-
- HY-144137
-
|
Estrogen Receptor/ERR
|
Cancer
|
Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4) .
|
-
- HY-144138
-
|
Estrogen Receptor/ERR
|
Cancer
|
Estrogen receptor antagonist 2 is a selective estrogen receptor downregulator. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3) .
|
-
- HY-18719
-
|
Estrogen Receptor/ERR
Potassium Channel
|
Cancer
|
Endoxifen Z-isomer is the most important Tamoxifen metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM.
|
-
- HY-A0031R
-
|
Estrogen Receptor/ERR
|
Cancer
|
Bazedoxifene (Standard) is the analytical standard of Bazedoxifene. This product is intended for research and analytical applications. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
|
-
- HY-A0036R
-
|
Estrogen Receptor/ERR
|
Cancer
|
Bazedoxifene (acetate) (Standard) is the analytical standard of Bazedoxifene (acetate). This product is intended for research and analytical applications. Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
|
-
- HY-15654R
-
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
Sodium 4-phenylbutyrate (Standard) is the analytical standard of Sodium 4-phenylbutyrate. This product is intended for research and analytical applications. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research .
|
-
- HY-A0281S3
-
4-PBA-d2; Benzenebutyric acid-d2
|
HDAC
Virus Protease
|
Cancer
|
4-Phenylbutyric acid-d2 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
|
-
- HY-W040270
-
|
PROTAC Linkers
|
Cancer
|
Amino-PEG10-amine, a PEG-based PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer .
|
-
- HY-N11600
-
|
Apoptosis
|
Cancer
|
β-Apopicropodophyllin is a nature product that could be isolated from Hyptis wticillata.β-Apopicropodophyllin induces apoptosis by inducing microtubule disruption, DNA damage, cell cycle arrest and ER stress. β-Apopicropodophyllin can be used in research of cancer .
|
-
- HY-16023
-
EM-652 hydrochloride; SCH 57068 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties .
|
-
- HY-103455
-
|
Others
|
Others
|
ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.
|
-
- HY-114770
-
|
Others
|
Cancer
|
(E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC50 = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604 .
|
-
- HY-155068
-
|
Reactive Oxygen Species
Apoptosis
Microtubule/Tubulin
|
Cancer
|
FC-11 is a Tubulin inhibitor that effectively inhibits tumor growth in mice. FC-11 can also induce endoplasmic reticulum (ER) stress to generate excess reactive oxygen species (ROS), leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-11 can be used in cancer research .
|
-
- HY-103454B
-
|
Estrogen Receptor/ERR
Apoptosis
|
Endocrinology
Cancer
|
MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo .
|
-
- HY-130411
-
|
PROTAC Linkers
|
Cancer
|
Amino-PEG11-amine, a PEG-based (12 units) PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer .
|
-
- HY-145341
-
|
Estrogen Receptor/ERR
|
Cancer
|
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .
|
-
- HY-A0281S2
-
4-PBA-d5; Benzenebutyric acid-d5
|
HDAC
Virus Protease
|
Cancer
|
4-Phenylbutyric acid-d5 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[2][3][4].
|
-
- HY-155406
-
|
Estrogen Receptor/ERR
Caspase
Bcl-2 Family
|
Cancer
|
Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research .
|
-
- HY-P10446
-
|
Epigenetic Reader Domain
|
Cancer
|
TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445). TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can disrupt the interaction between the breast cancer oncogene BRD4/JMJD6 and inhibit the growth of breast cancer cells. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells and is a potential inhibitor of breast cancer .
|
-
- HY-103454
-
|
Estrogen Receptor/ERR
Apoptosis
|
Endocrinology
Cancer
|
MPP dihydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP dihydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP dihydrochloride reverses the positive effects of beta-estradiol. MPP dihydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo .
|
-
- HY-110329
-
|
Others
|
Cancer
|
ML179 (SR-1309) is a inverse LRH1 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer .
|
-
- HY-50767S
-
PD 0332991-d8
|
CDK
|
Cancer
|
Palbociclib-d8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].
|
-
- HY-50767S1
-
PD 0332991-d4 hydrochloride
|
Isotope-Labeled Compounds
CDK
|
Cancer
|
Palbociclib-d4 (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].
|
-
- HY-144139
-
|
Estrogen Receptor/ERR
|
Cancer
|
Estrogen receptor antagonist 3 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 3 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 7) .
|
-
- HY-144202
-
|
Estrogen Receptor/ERR
|
Cancer
|
Estrogen receptor antagonist 4 is a potent antagonist of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. Estrogen receptor antagonist 4 has the potential for the research of cancer diseases (extracted from patent WO2021213358A1, compound 1) .
|
-
- HY-P10445
-
|
Epigenetic Reader Domain
|
Cancer
|
TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4 that disrupts the BRD4/JMJD6 interaction. BRD4/JMJD6 is a protein complex that is critical for oncogene expression and breast cancer, and TAT-PiET inhibits BRD4/JMJD6 target gene expression and breast cancer cell growth. TAT-PiET also resists endocrine resistance in ERα-positive breast cancer cells and is a potential inhibitor of breast cancer .
|
-
- HY-115901
-
|
Nuclear Hormone Receptor 4A/NR4A
Paraptosis
|
Cancer
|
4-PQBH is a potent Nur77 binder (KD=1.17 μM). 4-PQBH extensively induces caspase-independent cytoplasmic vacuolization and paraptosis through Nur77-mediated ER stress and autophagy. 4-PQBH can be used for cancer research .
|
-
- HY-101119
-
|
Estrogen Receptor/ERR
|
Cancer
|
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
|
-
- HY-127133
-
MPP
|
Estrogen Receptor/ERR
|
Endocrinology
|
Methylpiperidino pyrazole (MPP) is a potent and selective ER (estrogen receptor) modulator. Methylpiperidino pyrazole induces significant apoptosis in the endometrial cancer and oLE cell lines. Methylpiperidino pyrazole reverses the the positive effects of beta-estradiol. Methylpiperidino pyrazole has mixed agonist/antagonist action on murine uterine ERalpha in vivo .
|
-
- HY-144070
-
|
Others
|
Cancer
|
ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO.ErSO-DFP displays antitumor activity and leads to profound regression of MCF-7 tumors in mice model .
|
-
- HY-148789
-
OP-1250
|
Estrogen Receptor/ERR
|
Inflammation/Immunology
Cancer
|
Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER +/HER2 + cancer .
|
-
- HY-145823
-
|
EGFR
|
Cancer
|
EGFR-IN-42 (Compound 17b) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-42 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-42 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-42 has superior anti-cancer activity .
|
-
- HY-145824
-
|
EGFR
|
Cancer
|
EGFR-IN-43 (Compound 17c) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-43 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-43 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-43 has superior anti-cancer activity .
|
-
- HY-150505
-
|
Deubiquitinase
Apoptosis
|
Cancer
|
DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer .
|
-
- HY-144699
-
|
Estrogen Receptor/ERR
|
Cancer
|
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo .
|
-
- HY-163766
-
|
Estrogen Receptor/ERR
|
Cancer
|
Antiproliferative agent-51 (Compound 18h) exhibits inhibitory efficacy against estrogen receptor α (ERα) mediated transcription, with an IC50 of 1.6 nM. Antiproliferative agent-51 inhibits the proliferation of cancer cell ZR-75, with an IC50 of 0.031 μM. Antiproliferative agent-51 exhibits antitumor efficacy in mouse models .
|
-
- HY-146696
-
|
Epoxide Hydrolase
|
Cardiovascular Disease
Neurological Disease
Cancer
|
mEH-IN-1 (Compound 62) is a potent microsomal epoxide hydrolase (mEH) inhibitor with the IC50 of 2.2 nM. The mEH is a mammalian α/β-fold hydrolase enzyme, expressed in almost all tissues, hydrolyzes a wide range of epoxide containing molecules. The mEH is mainly localized in the endoplasmic reticulum (ER) of eukaryotic cells. mEH-IN-1 can be used for the research of preeclampsia, hypercholanemia and cancer .
|
-
- HY-162312
-
|
Deubiquitinase
Apoptosis
|
Cancer
|
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
|
-
- HY-159957
-
|
Histone Acetyltransferase
Estrogen Receptor/ERR
|
|
BAY-184 is a selective and orally active KAT6A and KAT6B inhibitor. BAY-184 inhibits KAT6A/KAT6B activity with an IC50 of 71 nM and 83 nM. respectively BAY-184 inhibits ERα transcriptional activity. BAY-184 inhibits proliferation of diverse breast cancer subtypes, and inhibits tumor growth .
|
-
- HY-19625
-
|
Reactive Oxygen Species
Paraptosis
|
Cancer
|
MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity.
MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS).
MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program .
|
-
- HY-110144
-
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .
|
-
- HY-121372
-
|
Estrogen Receptor/ERR
|
Cancer
|
Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .
|
-
- HY-103450
-
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
|
-
- HY-147165
-
|
YAP
|
Cancer
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 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-147165A
-
|
YAP
|
Cancer
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 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-114263
-
NXT629
3 Publications Verification
|
PPAR
|
Cancer
|
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively . NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models .
|
-
- HY-N1435
-
|
Apoptosis
PI3K
PTEN
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent.
Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT .
Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells .
|
-
- HY-N2025
-
|
PPAR
Glucosidase
|
Metabolic Disease
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
|
-
- HY-N0401A
-
|
Bacterial
Estrogen Receptor/ERR
FATP
|
Infection
Metabolic Disease
|
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide is orally active, it inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .
|
-
- HY-P99683
-
SGN-LIV1A
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
Ladiratuzumab vedotin (SGN-LIV1A) is a LIV-1 targeting antibody drug conjugate (ADC) (IC50: 5.6 nM for LIV-1). Ladiratuzumab vedotin consists of humanized IgG1 monoclonal antibody, MMAE and a protease-cleavable linker. Ladiratuzumab vedotin can drive immunogenic cell death (ICD) to elicit an immune response. Ladiratuzumab vedotin can be used for research of breast cancer .
|
-
- HY-168106
-
|
Eukaryotic Initiation Factor (eIF)
Apoptosis
|
Cancer
|
ZMF-24 is an anti-triple-negative breast cancer (TNBC) agent with IC50 values of 0.22 μM and 0.44 μM against TNBC proliferation in BT-549 cells and MDA-MB-231 cells, respectively. ZMF-24 inhibits Eukaryotic translation initiation factor 3 subunit D (EIF3D) that disrupts the energy supply of TNBC by inhibiting glycolysis and further induces profound TNBC apoptosis by stimulating persistent ER stress .
|
-
- HY-B0336R
-
|
COX
Apoptosis
PGE synthase
|
Inflammation/Immunology
Cancer
|
Pranoprofen (Standard) is the analytical standard of Pranoprofen. This product is intended for research and analytical applications. Pranoprofen is a non-steroidal anti-inflammatory agent (NSAID) for the research of keratitis or other ophthalmology diseases. Pranoprofen inhibit COX-1 and COX-2 enzymes, thus blocking arachidonic acid converted to eicosanoids and reducing prostaglandins synthesis .
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-
- HY-B0336
-
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COX
Apoptosis
PGE synthase
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Inflammation/Immunology
Cancer
|
Pranoprofen is a non-steroidal anti-inflammatory agent (NSAID) for the research of keratitis or other ophthalmology diseases.?Pranoprofen inhibit COX-1 and COX-2 enzymes, thus blocking arachidonic acid converted to eicosanoids and reducing prostaglandins synthesis .
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-
- HY-P4190
-
|
GnRH Receptor
|
Endocrinology
|
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries .
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-
- HY-159577
-
|
PI3K
mTOR
Akt
|
Cancer
|
Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine .
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-
- HY-122815
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Fusicoccin A
|
Apoptosis
|
Cancer
|
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity .
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- HY-N1435R
-
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Apoptosis
PI3K
PTEN
Autophagy
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Metabolic Disease
Inflammation/Immunology
Cancer
|
Oroxin B (Standard) is the analytical standard of Oroxin B. This product is intended for research and analytical applications. Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent.
Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT .
Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells .
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- HY-N2025R
-
|
PPAR
Glucosidase
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Metabolic Disease
|
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
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- HY-50767R
-
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CDK
|
Cancer
|
Palbociclib (Standard) is the analytical standard of Palbociclib. This product is intended for research and analytical applications. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
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-
- HY-50767
-
Palbociclib
Maximum Cited Publications
157 Publications Verification
PD 0332991
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
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-
- HY-50767A
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PD 0332991 monohydrochloride
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
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-
- HY-A0065
-
PD 0332991 isethionate
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-119437
-
FLTX1
2 Publications Verification
|
Estrogen Receptor/ERR
|
Cancer
|
FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus .
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-
- HY-50767B
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PD-0332991 dihydrochloride
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-50767D
-
PD 0332991 orotate
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
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-
- HY-50767C
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PD-0332991 hydrochloride
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
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-
- HY-108514
-
|
Sigma Receptor
|
Neurological Disease
Cancer
|
(±)-PPCC hemioxalate is a compound that has the ability to regulate the activity of the sigma-1 receptor. (±)-PPCC hemioxalate can selectively bind sigma-1 protein (s1), and then activate s1 receptor leading to dissociation of s1-BIP complex to regulate ER-mitochondrial calcium signaling, which plays an important role in cell bioenergy and cell survival. (±)-PPCC hemioxalate can be used to study sigma-1 receptors in cocaine addiction, forgetting, pain, depression, Alzheimer's disease, stroke, and cancer .
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-
- HY-110339
-
|
ROCK
Apoptosis
|
Cancer
|
RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively . RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis .
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-
- HY-N9174
-
|
Others
|
Cancer
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
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-
- HY-121605
-
|
Others
|
Cancer
|
RL71 is a curcuminoid anticancer agent that exhibits potent cytotoxicity against a variety of ER-negative breast cancer cells. RL71 (1 μM) induces cell cycle arrest in the G2/M phase and induces apoptosis in SKBr3 cells. RL7 also decreases HER2/neu phosphorylation and increases p27. RL71 also significantly reduced the phosphorylation of Akt and transiently increased the stress kinases JNK1/2 and p38 MAPK. Furthermore, RL71 exhibited anti-angiogenic potential in vitro, inhibiting the migration of HUVEC cells and the ability of these cells to form tubular networks .
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-
- HY-13559
-
Azaspirane
|
Apoptosis
|
Cancer
|
Atiprimod (Azaspirane) is an orally bioavailable small molecule with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) by inhibiting the phosphorylation of signal transducer and activator of transcription 3 (STAT3). Atiprimod also downregulates the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB transcription factors .
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-
- HY-N0288
-
|
Fatty Acid Synthase (FASN)
Virus Protease
Bacterial
Apoptosis
|
Inflammation/Immunology
Cancer
|
Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a Kd value 15.24 nM. Lycorine downregulates the SCAP protein level without changing its transcription . Lycorine is also a melanoma vasculogenic inhibitor . Lycorine can be used for the study of prostate cancer and metabolic diseases .
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-
-
-
HY-L054
-
|
223 compounds
|
Endoplasmic reticulum (ER) contributes to the production and folding of approximately one third of cellular proteins, and is thus inextricably linked to the maintenance of cellular homeostasis and the fine balance between health and disease. However, some adverse factors negatively impact ER functions and protein synthesis, resulting in the activation of Endoplasmic reticulum stress (ER stress, ERS) and unfolded protein response (UPR) signaling pathways. The UPR is triggered when ER protein folding capacity is overwhelmed by cellular demand and the UPR initially aims to restore ER homeostasis and normal cellular functions. However, if this fails, then the UPR triggers cell death. Chronic ER stress and defects in UPR signaling are emerging as key contributors to a growing list of human diseases, including diabetes, neurodegeneration and cancer.
MCE Endoplasmic Reticulum Stress Compound Library contains 223 ER stress-related compounds that mainly target PERK, IRE1, ATF6, etc. MCE ER stress library is a useful tool for researching ER stress and related diseases.
|
Cat. No. |
Product Name |
Type |
-
- HY-162129
-
|
Fluorescent Dyes/Probes
|
Antitumor agent-131 (Compound 2-p) is an ER fluorescent probe with an IC50 value of 23 nM for HepG2 tumor cells. Antitumor agent-131 can be used as a photosensitizer for the study of cancer photodynamics .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-129960
-
|
Peptides
|
Others
|
L-Selenocystine is a diselenide-bridged amino acid. L-Selenocystine is a redox-active selenium compound that has both anti- and pro-oxidant actions. L-Selenocystine induces an unfolded protein response, ER stress, and large cytoplasmic vacuolization in HeLa cells and has cytostatic effects in a range of cancer cell types .
|
-
- HY-P4190
-
|
GnRH Receptor
|
Endocrinology
|
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries .
|
-
- HY-P10393
-
ERα (295-311)
|
Apoptosis
|
Cancer
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
-
- HY-P10446
-
|
Epigenetic Reader Domain
|
Cancer
|
TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445). TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can disrupt the interaction between the breast cancer oncogene BRD4/JMJD6 and inhibit the growth of breast cancer cells. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells and is a potential inhibitor of breast cancer .
|
-
- HY-P10445
-
|
Epigenetic Reader Domain
|
Cancer
|
TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4 that disrupts the BRD4/JMJD6 interaction. BRD4/JMJD6 is a protein complex that is critical for oncogene expression and breast cancer, and TAT-PiET inhibits BRD4/JMJD6 target gene expression and breast cancer cell growth. TAT-PiET also resists endocrine resistance in ERα-positive breast cancer cells and is a potential inhibitor of breast cancer .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99683
-
SGN-LIV1A
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
Ladiratuzumab vedotin (SGN-LIV1A) is a LIV-1 targeting antibody drug conjugate (ADC) (IC50: 5.6 nM for LIV-1). Ladiratuzumab vedotin consists of humanized IgG1 monoclonal antibody, MMAE and a protease-cleavable linker. Ladiratuzumab vedotin can drive immunogenic cell death (ICD) to elicit an immune response. Ladiratuzumab vedotin can be used for research of breast cancer .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-B0412
-
-
-
- HY-A0098
-
-
-
- HY-N1443
-
-
-
- HY-N0878
-
-
-
- HY-U00141
-
-
-
- HY-N1435
-
-
-
- HY-N2025
-
-
-
- HY-N0401A
-
-
-
- HY-W011241
-
-
-
- HY-N11600
-
-
-
- HY-122815
-
-
-
- HY-N1435R
-
-
-
- HY-N2025R
-
|
Structural Classification
Flavonoids
Flavones
Source classification
Bignoniaceae
Plants
Oroxylum indicum (Linn.) Bentham ex Kurz
|
PPAR
Glucosidase
|
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
|
-
-
- HY-N9174
-
|
Structural Classification
Flavonoids
Flavones
Source classification
Plants
Moraceae
Broussonetia papyrifera (Linnaeus) L'Heritier ex Ventenat
|
Others
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
|
-
-
- HY-N0288
-
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-15654S
-
|
Phenylbutyrate-d11 (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[1].
|
-
-
- HY-A0281S
-
|
4-Phenylbutyric acid-d11 is the deuterium labeled 4-Phenylbutyric acid. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
|
-
-
- HY-50767S
-
|
Palbociclib-d8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].
|
-
-
- HY-19822S2
-
|
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
|
-
-
- HY-19822S3
-
|
Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
|
-
-
- HY-19822S
-
|
Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
|
-
-
- HY-A0031S
-
|
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
|
-
-
- HY-A0031S2
-
|
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
|
-
-
- HY-A0281S3
-
|
4-Phenylbutyric acid-d2 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
|
-
-
- HY-A0281S2
-
|
4-Phenylbutyric acid-d5 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[2][3][4].
|
-
-
- HY-50767S1
-
|
Palbociclib-d4 (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-162129
-
|
|
Azide
|
Antitumor agent-131 (Compound 2-p) is an ER fluorescent probe with an IC50 value of 23 nM for HepG2 tumor cells. Antitumor agent-131 can be used as a photosensitizer for the study of cancer photodynamics .
|
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