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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
86 Results for "
PROTAC ER
" in MedChemExpress (MCE) Product Catalog:
Products (86)
86 Results for "PROTAC ER" in MCE Product Catalog:
9
9 Publications Verification
Synonyms: ARV-471; PF-07850327
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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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BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC) .
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1 Cited Publications
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PROTAC ERα Degrader-2 is a ERα PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of ERα in MCF-7 cells .
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1 Cited Publications
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ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC50 values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity .
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PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
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1 Cited Publications
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PROTAC ERα Degrader-6 is a ERα PROTAC degrader. PROTAC ERα Degrader-6 recruits the VHL E3 ubiquitin ligase to induce the ubiquitination and proteasomal degradation of ERα. PROTAC ERα Degrader-6 can be applied in the research of ERα + breast cancer .
Cat. No.: HY-30756
CAS No.: 236406-55-6
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tert-Butyl 2,7-diazaspiro[3.5]nonane-2-carboxylate is a PROTAC linker. tert-Butyl 2,7-diazaspiro[3.5]nonane-2-carboxylate can be used in the synthesis of PROTAC ER Degrader-12 (HY-160264) and PROTAC AR Degrader-9 (HY-170332) .
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MC-Val-Cit-PAB-PROTAC ERα Degrader-1 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. MC-Val-Cit-PAB-PROTAC ERα Degrader-1 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
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PROTAC ER Degrader-4 is a potent ERα PROTAC degrader, with an IC50 of 0.8 nM against human ERα. PROTAC ER Degrader-4 recruits the VHL E3 ligase to ERα, and triggers the ubiquitination modification and degradation of ERα via the UP/26S proteasome system. PROTAC ER Degrader-4 can be used in related research on breast cancer .
Cat. No.: HY-U00425
CAS No.: 1264754-13-3
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PROTAC ERRα ligand 1 is a PROTAC target protein ligand. PROTAC ERRα ligand 1 is an orally active ERRα inverse agonist with IC50 values of 0.6 μM for ERRα. PROTAC ERRα ligand 1 shows no significant activity against a panel of other nuclear receptors, including ERα c, ERRγ, ERβ, PPARα, PPARγ, PPARδ, and RXRα. PROTAC ERRα ligand 1 can provide enhanced insulin sensitivity in vivo. PROTAC ERRα ligand 1 can be used for metabolic diseases research, such as type 2 diabetes and obesity .
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ERD-3111 is an orally active PROTAC degrader targeting estrogen receptor α (ERα), with a DC50 of 0.5 nM. ERD-3111 induces ERα degradation in breast cancer cells, and triggers tumor regression or complete inhibition of tumor growth in ER-positive breast cancer xenograft models. ERD-3111 can be used in breast cancer-related research .
Cat. No.: HY-43962
CAS No.: 693227-00-8
Synonyms: Androgen receptor ligand 3
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CS-1-65 is an androgen receptor (AR) ligand. CS-1-65 is linked to an IAP ligand via a linker to form an ERα PROTAC degrader.
Cat. No.: HY-P10446
CAS No.: 3036046-04-2
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PROTAC ERα Degrader-4 (Compound ZD12) 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.
Cat. No.: HY-W088749
CAS No.: 52221-07-5
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tert-Butyl-hexanedioic acid is a PROTAC linker. tert-Butyl-hexanedioic acid can be used to synthesize PROTAC molecules, such as PROTAC ERα Degrader-12 (HY-174453) .
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AZ'6421 is an orally active ERα PROTAC degrader with a DC50 of 0.4 nM. AZ'6421 recruits the VHL E3 ligase to form a ternary complex, inducing proteasome-mediated polyubiquitination and degradation of ERα. AZ'6421 inhibits the growth of ER + cancer cells. AZ'6421 can be used in studies related to ER + breast cancer .
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VHL Ligand 14 (Compound 11) is a VHL ligand for design of PROTAC estrogen receptor α (ERα) degraders, with a binding affinity IC50 of 196 nM .
Cat. No.: HY-176386
CAS No.: 1466558-44-0
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E3 ligase Ligand 68 is an E3 ligase ligand that can be used in the synthesis of PROTACs, such as PROTAC ER Degrader-3 (HY-128527) .
Cat. No.: HY-179433
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PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .
Cat. No.: HY-128527
CAS No.: 2158322-29-1
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PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
