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Pathways Recommended:	PROTAC

Results for "

MDM2 PROTAC degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) E1/E2/E3 Enzyme (6) E3 Ligase Ligand-Linker Conjugates (2) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (3) Histone Methyltransferase (1) MDM-2/p53 (6) Molecular Glues (1) PARP (2) PROTACs (13) Target Protein Ligand-Linker Conjugates (9)
By Research Areas:	Cancer (24)

Inhibitors & Agonists

Screening Libraries

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

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-128842

PROTAC MDM2 Degrader-3	PROTACs MDM-2/p53 E1/E2/E3 Enzyme	Cancer
PROTAC MDM2 Degrader-3 is a *MDM2* degrader based on *PROTAC* technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase .

HY-128840

PROTAC MDM2 Degrader-1	PROTACs MDM-2/p53 E1/E2/E3 Enzyme	Cancer
PROTAC MDM2 Degrader-1 is a *MDM2* degrader based on *PROTAC* technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase (CN108610333A) .

HY-128841

PROTAC MDM2 Degrader-2	PROTACs MDM-2/p53 E1/E2/E3 Enzyme	Cancer
PROTAC MDM2 Degrader-2 is a *MDM2* degrader based on *PROTAC* technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase (CN108610333A) .

HY-128843

PROTAC MDM2 Degrader-4	PROTACs MDM-2/p53 E1/E2/E3 Enzyme	Cancer
PROTAC MDM2 Degrader-4 is a *MDM2* degrader based on *PROTAC* technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase .

HY-122725A

Lenalidomide-C5-NH2 TFA	E3 Ligase Ligand-Linker Conjugates	Cancer
Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader .

HY-129775

K-Ras ligand-Linker Conjugate 1	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-129776

K-Ras ligand-Linker Conjugate 2	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-130991

K-Ras ligand-Linker Conjugate 6	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-134823

MD-222	MDM-2/p53 PROTACs E1/E2/E3 Enzyme	Cancer
MD-222 is the first-in-class highly potent PROTAC degrader of *MDM2. MD-222 consists of ligands for Cereblon* and *MDM2. MD-222 induces rapid degradation* of the *MDM2* protein and activation of wild-type p53 in cells. MD-222 has anticancer effects .

HY-128838

PROTAC ERRα Degrader-1	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERRα Degrader-1 comprises a *MDM2* ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader .

HY-128839

PROTAC ERRα Degrader-2	PROTACs Estrogen Receptor/ERR	Cancer
PROTAC ERRα Degrader-2 comprises a *MDM2* ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader .

HY-114305

A1874	PROTACs Epigenetic Reader Domain	Cancer
A1874 is a nutlin-based (MDM2 ligand) and *BRD4*-degrading PROTAC with a DC₅₀ of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation .

HY-128838A

(rel)-PROTAC ERRα Degrader-1	Estrogen Receptor/ERR	Others
(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a *MDM2* ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader .

HY-114312

MD-224 4 Publications Verification	PROTACs MDM-2/p53 E1/E2/E3 Enzyme	Cancer
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and *MDM2. MD-224 induces rapid degradation* of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC₅₀ value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 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-114324

PROTAC PARP1 degrader	PROTACs PARP	Cancer
PROTAC PARP1 degrader is a PARP1 degrader based on *MDM2* E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC₅₀ of 6.12 μM.

HY-44148

FAK ligand-Linker Conjugate 1	Target Protein Ligand-Linker Conjugates	Cancer
FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation .

HY-130499

ERRα Ligand-Linker Conjugates 1	Target Protein Ligand-Linker Conjugates	Cancer
ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases *MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC* ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader .

HY-122725B

Lenalidomide-C5-NH2 hydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
Lenalidomide-C5-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader .

HY-114324A

rel-PROTAC PARP1 degrader	PROTACs PARP	Cancer
rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on *MDM2* E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC₅₀ of 6.12 μM.

HY-141486

(Rac)-PROTAC PARP/EGFR ligand 1	Target Protein Ligand-Linker Conjugates	Cancer
(Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP .

HY-130707

K-Ras ligand-Linker Conjugate 3	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-130822

K-Ras ligand-Linker Conjugate 4	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 4 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 4 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-130823

K-Ras ligand-Linker Conjugate 5	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 5 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 5 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-157164

PROTAC EZH2 Degrader-2	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .

HY-130122

MG-277	Molecular Glues PROTACs Apoptosis	Cancer
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC₅₀ of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC₅₀s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity .

E3 Ligase Ligand Library	88 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2). MCE carefully prepared a unique collection of 88 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

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