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Pathways Recommended:	PROTAC

Results for "

MDM2 PROTAC

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Ligands for Target Protein for PROTAC (2) Apoptosis (3) Casein Kinase (1) E1/E2/E3 Enzyme (5) E3 Ligase Ligand-Linker Conjugates (3) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (3) Histone Methyltransferase (2) IKZF Family (1) Ligands for E3 Ligase (3) MAGL (1) MDM-2/p53 (14) Molecular Glues (1) PARP (2) PROTACs (18) Target Protein Ligand-Linker Conjugates (9)
By Research Areas:	Cancer (37)
Click Chemistry:	PROTAC Synthesis (1) Azide (1)

Inhibitors & Agonists

Screening Libraries

Click Chemistry

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-128841

PROTAC MDM2 Degrader-2	PROTACs MDM-2/p53 E1/E2/E3 Enzyme	Cancer
PROTAC MDM2 Degrader-2 is an **MDM2 PROTAC** degrader. PROTAC MDM2 Degrader-2 can induce the self-ubiquitination and degradation of *MDM2, thereby upregulating the level of p53* protein. PROTAC MDM2 Degrader-2 has anti-tumor activity and can be used in the study of cancer . (Blue: MDM2 ligand (HY-128836); Black: linker (HY-128833))

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	Cancer
PROTAC MDM2 Degrader-1 (Compound 15a) is a **MDM2 PROTAC** degrader. The structures of both Linker ends of PROTAC MDM2 Degrader-1 are MDM2 ligands. PROTAC MDM2 Degrader-1 can not only block the binding of p53-MDM2, but also degrade the target MDM2 protein by utilizing the function of the E3 ligase of MDM2 itself, thus exerting an anti-tumor effect. (Pink: MDM2 ligand 2 (HY-128836); Black: Linker (HY-128844); Blue: E3 ligase Ligand 15 (HY-128836))

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-158684

YX-02-030	PROTACs MDM-2/p53	Cancer
YX-02-030M is a PROTAC *MDM2* degrader. YX-02-030M inhibits MDM2-p53 binding and VHL-HIF1α binding with IC₅₀s of 63 nM and 1.35 μM respectively. YX-02-030M binds MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, and effectively kills p53 mutant or deleted Triple-negative breast cancers (TNBC) cells. (Blue: VHL ligand; Black: linker; Pink: MDM2 inhibitor) .

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-174458

MD-4251	PROTACs MDM-2/p53 IKZF Family Casein Kinase	Cancer
MD-4251 is an orally active *MDM2* *PROTAC* degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC₅₀: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker

HY-170452

MDM2 ligand 4	MDM-2/p53 Ligands for Target Protein for PROTAC	Cancer
MDM2 ligand 4 is the ligand for *MDM2* that can be used for synthesis of PROTAC degrader KT-253 (HY-170451) .

HY-158685

RG7112D	MDM-2/p53	Cancer
RG7112D is a potent *MDM2* inhibitor with IC₅₀s of 11 nM and >10000 nM and for MDM2-p53 and VHL-HIF1α by binding HTRF assay, respectively. RG7112D is coupled by an amide bond to VHL-Amine, resulting in a bi-functional molecule, YX-02-030. YX-02-03, a MDM2-PROTAC, potently inhibits MDM2-p53 binding (HTRF IC₅₀=63nM). RG7112D can stabilize MDM2 protein and increase p53 protein levels .

HY-128837

Nutlin carboxylic acid MDM2 ligand 1; E3 ligase Ligand 16	Ligands for E3 Ligase	Cancer
Nutlin carboxylic acid (MDM2 ligand 1) is the Nutlin 3-based *MDM2* ligand. Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTAC .

HY-169327

MD-265	PROTACs MDM-2/p53	Cancer
MD-265 is a *PROTAC* degrader that can break down *MDM2*, leading to activation of p53 in cancer cells carrying wild-type p53. MD-265 achieves complete tumor regression and improves long-term survival of mice with leukemia. (Pink: MI-1063 (HY-133754); Black: linker; Blue: Lenalidomide (HY-A0003) .

HY-128836

(4R,5S)-Nutlin carboxylic acid MDM2 ligand 2; E3 ligase Ligand 15	Ligands for E3 Ligase	Cancer
(4R,5S)-Nutlin carboxylic acid (MDM2 ligand 2) is the Nutlin 3-based MDM2 ligand. (4R,5S)-Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTACs .

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-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-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-114312

MD-224 5 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-173369

PROTAC MAGL degrader-1	MAGL Ligands for E3 Ligase	Cancer
PROTAC MAGL degrader-1 is an orally active PROTAC agent that simultaneously targets monoacylglycerol lipase (MAGL) and E3 ubiquitin ligase *MDM2. PROTAC* MAGL degrader-1 degrades MAGL and inhibits the binding of MDM2 to p53. PROTAC MAGL degrader-1 can partially penetrate the blood-brain barrier (BBB). PROTAC MAGL degrader-1 induces glioblastoma stem cells (GSCs) apoptosis. (E3 ligase ligand: HY-128837; target protein ligand + linker: HY-173370; target protein inhibitor: HY-15249) .

HY-114324

PROTAC PARP1 degrader	PROTACs PARP	Cancer
PROTAC PARP1 degrader is a PARP1 degrader based on *MDM2* E3 ligand. PROTAC PARP1 degrader induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader consists of E3 ubiquitinase ligand MDM2 ligand (HY-128836), blue part; target protein ligand PAPR1 ligand (HY-171543), pink part; PROTAC linker N3-PEG4-C2-NH2 (HY-128834), black part .

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-162450

Antitumor agent-150	PROTACs MDM-2/p53 Apoptosis	Cancer
Antitumor agent-150 (V10), an anti-breast cancer agent, is a *PROTAC*-based *MDM2* protein degrader (Red: Ganoderic acid A; Black: 4O-PEG linker; Blue: VHL ligand) .

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-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-114305

A1874 1 Publications Verification	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-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-170451

KT-253	PROTACs MDM-2/p53 Apoptosis	Cancer
KT-253 is a p53 stabilizer and a PROTAC degrader for *MDM2* (DC₅₀=0.4 nM). KT-253 inhibits the proliferation of cancer cell RS4;11 with an IC₅₀ of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. KT-253 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927))

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-128838A

(rel)-PROTAC ERRα Degrader-1 1 Publications Verification	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-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-133754

MI-1063	MDM-2/p53 Ligands for Target Protein for PROTAC	Cancer
MI-1063 is an inhibitor for DMD-2, that blocks the MDM2-p53 interaction, and activates the tumor suppressor function of p53. MI-1063 inhibits the growth of cancer cell RS4-11 and MV4-11 with IC₅₀ of 179 nM and 93 nM. MI-1063 can be used as target protein ligand in synthesis of PROTAC degrader MD-265 (HY-169327) .

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-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-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-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-128832

Nutlin-C1-amido-PEG4-C2-N3 MDM2 Ligand-Linker Conjugates 1; E3 ligase Ligand-Linker Conjugates 48	E3 Ligase Ligand-Linker Conjugates	Cancer
Nutlin-C1-amido-PEG4-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Nutlin 3 based MDM2 ligand and 4-unit PEG linker used in *PROTAC* technology. Nutlin-C1-amido-PEG4-C2-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-159732

PRMT3-IN-4	Histone Methyltransferase	Cancer
PRMT3-IN-4 (intermediate 15) is a protein arginine methyltransferase 3 (PRMT3) inhibitor. PRMT3-IN-4 is an active control for HY-19715. PRMT3-IN-4 can be used to synthesize PROTACs targeting PRMT3. PRMT3-IN-4 can be used in leukemia-related research .

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 .

Cat. No.	Product Name

HY-L128

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.

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.

Cat. No.	Product Name		Classification

HY-114312

MD-224 5 Publications Verification		PROTAC Synthesis
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-128832

Nutlin-C1-amido-PEG4-C2-N3 MDM2 Ligand-Linker Conjugates 1; E3 ligase Ligand-Linker Conjugates 48		Azide
Nutlin-C1-amido-PEG4-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Nutlin 3 based MDM2 ligand and 4-unit PEG linker used in *PROTAC* technology. Nutlin-C1-amido-PEG4-C2-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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