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Pathways Recommended:	PROTAC

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PROTAC ERα Degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Ligands for Target Protein for PROTAC (5) PROTAC Linkers (1) PROTAC-Linker Conjugates for PAC (3) Androgen Receptor (2) Apoptosis (8) Cytochrome P450 (2) E3 Ligase Ligand-Linker Conjugates (3) Estrogen Receptor/ERR (27) Fluorescent Dye (1) IAP (4) Ligands for E3 Ligase (2) NF-κB (1) NOD-like Receptor (NLR) (1) PROTACs (20) Src (2) TNF Receptor (1)
By Research Areas:	Cancer (34) Inflammation/Immunology (1)

Targets Recommended: PROTAC-Linker Conjugates for PAC PROTAC Linkers Ligands for Target Protein for PROTAC

Cat. No.	Nombre del producto	Target	Áreas de investigación	Chemical Structure

HY-112100

*MC-Val-Cit-PAB-PROTAC* ERα Degrader-1**	PROTAC-Linker Conjugates for PAC Estrogen Receptor/ERR	Cancer
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) .

HY-111846

PROTAC ERα Degrader-2 1 Publications Verification	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-2 (Compound 11) is a *ERα* PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of *ERα* in MCF-7 cells.(Pink: AR ligand (HY-43962), Blue: IAP Ligand (HY-177389), Black: Linker (HY-128833)) .

HY-149295

PROTAC ERα Degrader-4	PROTACs Estrogen Receptor/ERR Apoptosis	Cancer
PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC *ERα* degrader (K_i: 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.

HY-112098

PROTAC ERα Degrader-1 1 Publications Verification	PROTACs Estrogen Receptor/ERR	Cancer
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.

HY-43962

Androgen receptor ligand 3	Ligands for Target Protein for PROTAC Androgen Receptor	Cancer
Androgen receptor ligand 3 is an androgen receptor (AR) ligand. Androgen receptor ligand 3 is linked to an IAP ligand via a linker to form an **ERα PROTAC** degrader.

HY-149480

ERD-3111	PROTACs Estrogen Receptor/ERR	Cancer
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 .

HY-W088749

tert-Butyl-hexanedioic acid	PROTAC Linkers	Cancer
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) .

HY-150803

VHL Ligand 14	Ligands for E3 Ligase	Cancer
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 .

HY-178961

PROTAC ERα Degrader-13	PROTACs Estrogen Receptor/ERR Apoptosis	Cancer
PROTAC ERα Degrader-13 is an orally active *PROTAC* molecule that efficiently and selectively degrades *ERα* (DC₅₀ = 3.78 nM). PROTAC ERα Degrader-13 has the characteristics of strong anti proliferation (IC₅₀ = 0.6 nM), induction of apoptosis, and overcoming drug resistance in MCF-7 cells. PROTAC ERα Degrader-13 has good safety and no significant organ toxicity. PROTAC ERα Degrader-13 can be used for cancer research .

HY-179433

PROTAC AR Degrader-12	PROTACs Androgen Receptor Estrogen Receptor/ERR Src	Cancer
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 .

HY-174453

PROTAC ERα Degrader-12	PROTACs Estrogen Receptor/ERR Apoptosis	Cancer
PROTAC ERα Degrader-12 is a potent and selective **Erα PROTAC** degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310)) .

HY-174870

PROTAC ERα Degrader-11	PROTACs Estrogen Receptor/ERR Apoptosis Fluorescent Dye	Cancer
PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) *ERα* PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective *ERα* degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)) .

HY-128527

PROTAC ER Degrader-3	PROTAC-Linker Conjugates for PAC Estrogen Receptor/ERR	Cancer
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) .

HY-157765

PROTAC ERα Degrader-6	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-6 (compound A2) is a potent *PROTAC* degrader of *ERα, with IC₅₀* of 0.11 μM in MCE-7 cells. PROTAC ERα Degrader-6 has anti-tumor effect. PROTAC ERα Degrader-6 is a fluorescent probes with Em of 582 nm that enable real-time visualization of ERα protein degradation .

HY-160562

PROTAC ERα Degrader-7	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-7 (compound i-320) is a potent estrogen receptor alpha(ERα) PROTAC degrader with a DC₅₀ value of 0.000006 µM. PROTAC ERα Degrader-7 comprises a cereblon-binding moiety LBM linked to a ligand ERBM that binds ERα and comprises a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring .

HY-160563

PROTAC ERα Degrader-8	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-8 (compound ii-56) is a potent PROTAC degrader of *Erα, with DC₅₀* of 0.000006 μM in MCF7 cells .

HY-163679

PROTAC ERα Degrader-9	Estrogen Receptor/ERR Cytochrome P450 PROTACs Apoptosis	Cancer
PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a K_i of 0.25 μM, inhibits ARO with an IC₅₀ of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC₅₀=0.54 μM) and ERα mutants MCF-7 ^EGFR (IC₅₀=0.075 μM), MCF-7 ^D538G (IC₅₀=0.31 μM), MCF-7 ^Y537S (IC₅₀=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))

HY-170336

PROTAC ERα Degrader-10	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Degrader-10 (Compound 160a) is an orally active degrader for *ERα* with DC₅₀ of 0.37-1.1 nM, in cells MCF7, T47D and CAMA-1. PROTAC ERα Degrader-10 exhibits antitumor efficacy in mouse model . (Pink: ligand for target protein (HY-170339); Black: linker (HY-30105); Blue: ligand for E3 ligase Cereblon (HY-168055))

HY-145071

PROTAC ERα Y537S degrader-1	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 extracts from patent WO2021143822, example 12. PROTAC ERα Y537S degrader-1 is an estrogen receptor-alpha (ERα) Y537S degrader .

HY-W998310

(S,R,S)-AHPC-Me-CO-C4-COOH	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-Me-CO-C4-COOH is a conjugate of the E3 ligase VHL ligand and a linker, which can be used to synthesize PROTAC ERα Degrader-12 (HY-174453). PROTAC ERα Degrader-12 is a potent and highly selective *ERα* PROTAC degrader .

HY-176225

BY13	PROTACs Src Estrogen Receptor/ERR Apoptosis	Cancer
BY13 is a SRC-3 *PROTAC* degrader with a DC₅₀ of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model . Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)

HY-168869

Tamoxifen-PEG-Clozapine	PROTACs Estrogen Receptor/ERR	Cancer
Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. Tamoxifen-PEG-Clozapine degrades ERα via a ubiquitin-proteasome system that uses the ubiquitin protein ligase E3 component N-recognin 5. Tamoxifen-PEG-Clozapine can be used for the research of cancer . (Pink: ERα inhibitor (HY-W271653); Black: linker (HY-168870); Blue: CRBN Ligand (HY-G0021))

HY-128528

PROTAC ER Degrader-2	PROTAC-Linker Conjugates for PAC Estrogen Receptor/ERR	Cancer
PROTAC ER Degrader-2 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) .

HY-175348

XB2M54	Ligands for E3 Ligase IAP NOD-like Receptor (NLR)	Others Inflammation/Immunology Cancer
XB2M54 is a selective XIAP antagonist. XB2M54 inhibits NOD2-mediated inflammatory signaling. XB2M54 is an E3 ligase ligand. XB2M54 can be used for synthesis of PROTAC ERα Degrader-1 (HY-112098) .

HY-175448

GNE-1567	PROTACs Estrogen Receptor/ERR IAP	Cancer
GNE-1567 is a potent **ERα PROTAC** degrader and a selective XIAP antagonist with a K_d value of 0.03 μM. GNE-1567 is indicated for breast cancer research. (Pink: ligand for target protein (HY-18719); Black: linker; Blue: ligand for E3 ligase (HY-175449)) .

HY-163680

ERα degrader 9	Estrogen Receptor/ERR Cytochrome P450	Cancer
ERα degrader 9 is a dual targeting ligand for estrogen receptor α (ERα) and aromatase (ARO). ERα degrader 9 can be utilized for synthesis of PROTAC ERα Degrader-9 (HY-163679) .

HY-174475

ER ligand-11	Estrogen Receptor/ERR Ligands for Target Protein for PROTAC	Cancer
ER ligand-11 is the ligand for *ERα* and can be used for synthesis of PROTACs, such as PROTAC ERα Degrader-12 (HY-174453) .

HY-170339

ER ligand-5	Estrogen Receptor/ERR Ligands for Target Protein for PROTAC	Cancer
ER ligand-5 is the ligand for estrogen receptor, that can be used as ligand for target protein for PROTAC synthesis of PROTAC ERα Degrader-10 (HY-170336) .

HY-177389

IAP ligand 5	Ligands for Target Protein for PROTAC	Cancer
IAP ligand 5 is a IAP ligand. IAP ligand 5 can be used to synthesize PROTAC ERα Degrader-2 (HY-111846).

HY-167701

OBHSA	Ligands for Target Protein for PROTAC Apoptosis Estrogen Receptor/ERR	Cancer
OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an *ERα* ligand to synthesize PROTAC degraders .

HY-175444

XIAP ligand-Linker Conjugate 1	E3 Ligase Ligand-Linker Conjugates IAP	Cancer
XIAP ligand-Linker Conjugate 1 is an E3 ligase ligand-linker conjugate that incorporates the XIAP BIR2 ligand XB2M54 (HY-175348) and linker. XIAP ligand-Linker Conjugate 1 can be used for synthesis of PROTAC ERα Degrader-1 (HY-112098) .

HY-174880

CRBN ligand-8-O-C6-NH2	E3 Ligase Ligand-Linker Conjugates	Others
CRBN ligand-8-O-C6-NH2 is an E3 ligase ligand-linker conjugate that incorporates a CRBN ligand (HY-150831) and a linker. CRBN ligand-8-O-C6-NH2 can be used for synthesis of PROTAC ERα Degrader-11 (HY-174870) .

HY-180959

NEP168	PROTACs Estrogen Receptor/ERR	Cancer
NEP168 is an ERα PROTAC degrader designed based on the GID4 E3 ligase. NEP168 can be used for the study of breast cancer .

HY-183804

PROTAC ER Degrader-16	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ER Degrader-16 is an orally active *ERα* *PROTAC* degrader with a DC₅₀ of 1.4 nM and an IC₅₀ of 1.9 nM. PROTAC ER Degrader-16 inhibits ER-dependent breast cancer cell proliferation and exerts anti-tumor effects in mouse models. PROTAC ER Degrader-16 can be used for breast cancer research .

HY-175445

GNE-5472	PROTACs Estrogen Receptor/ERR IAP NF-κB TNF Receptor Apoptosis	Cancer
GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer .

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