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Results for "

MDM2 degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	MDM-2/p53 (35) Akt (1) Apoptosis (13) Autophagy (4) Bcl-2 Family (1) c-Myc (1) Casein Kinase (2) Caspase (2) CDK (1) DAPK (1) Deubiquitinase (4) Dihydroorotate Dehydrogenase (3) DNA Methyltransferase (1) Drug Derivative (1) Drug Isomer (1) E1/E2/E3 Enzyme (4) E3 Ligase Ligand-Linker Conjugates (5) Early 2 Factor (E2F) (1) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (3) Ferroptosis (1) HDAC (1) Histone Methyltransferase (1) IKZF Family (1) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (2) MAGL (1) Molecular Glues (1) PARP (3) PDK-1 (1) PROTACs (21) PTEN (1) Sirtuin (3) Target Protein Ligand-Linker Conjugates (10)
By Research Areas:	Cancer (62) Neurological Disease (1)
Click Chemistry:	PROTAC Synthesis (1) Azide (2)

Inhibitors & Agonists

Bibliothèques de criblage

Peptides

Click Chemistry

Targets Recommended: MDM-2/p53

Cat. No.	Nom du produit	Target	Áreas de investigación	Chemical Structure

HY-170451

Seldegamadlin KT-253	PROTACs MDM-2/p53 Apoptosis	Cancer
Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC₅₀ = 0.4 nM). Seldegamadlin 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. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927)) .

HY-128841

*PROTAC MDM2* Degrader-2** 1 Publications Verification	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 .

HY-114312

MD-224 5+ Cited Publications	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-112816

MA242 1 Publications Verification	MDM-2/p53 Apoptosis	Cancer
MA242 is a specific dual inhibitor of *MDM2* and NFAT1. MA242 directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status .

HY-15510

Tenovin-6 5 Publications Verification	MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy	Cancer
Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC₅₀s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH) .

HY-114305

A1874 2 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-134823

MD-222 1 Publications Verification	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-110182

SP-141 4 Publications Verification	MDM-2/p53	Cancer
SP-141 is a specific inhibitor of *MDM2. SP-141 promotes MDM2* auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells .

HY-19726

NSC59984 2 Publications Verification	MDM-2/p53	Cancer
NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway . NSC59984 acts by targeting GOF-mutant p53 and stimulates p73 to restore the p53 pathway signaling .

HY-13423

Tenovin-1 5 Publications Verification	MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy	Cancer
Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor .

HY-158684

YX-02-030	PROTACs MDM-2/p53 Apoptosis	Cancer
YX-02-030 is a VHL-dependent *MDM2* PROTAC degrader with a K_d of 35 nM. YX-02-030 recruits the VHL E3 ligase to form a ternary complex, leading to ubiquitination and proteasome-mediated degradation of MDM2. YX-02-030 inhibits MDM2-p53 and VHL-HIF1α binding with IC₅₀ values of 63 and 1350 nM. YX-02-030 activates TAp73, upregulates p53 family target genes and induces apoptosis. YX-02-030 demonstrates on-target efficacy in TNBC xenograft-bearing mice, extending survival without normal cell toxicity .

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 .

HY-128842

*PROTAC MDM2* Degrader-3** 1 Publications Verification	PROTACs MDM-2/p53	Cancer
PROTAC MDM2 Degrader-3 is a *MDM2* self-degrading (dimeric) PROTAC. PROTAC MDM2 Degrader-3 can be used in cancer research .

HY-148409

MMRi62	Ferroptosis Apoptosis Autophagy MDM-2/p53	Cancer
MMRi62, a ferroptosis inducer targeting *MDM2-MDM4* (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .

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 .

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-120084

BTX161 1 Publications Verification	Casein Kinase	Cancer
BTX161, a thalidomide analog, is an effective CKIα degrader. BTX161 mediates human AML cell CKIα degradation more effectively than lenalidomide and activates the DNA damage response (DDR) and p53, while stabilizing p53 antagonist MDM2.

HY-122725B

Lenalidomide-C5-NH2 hydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
Lenalidomide-C5-NH2 hydrochloride is an E3 ligase ligand-linker conjugate. Lenalidomide-C5-NH2 hydrochloride can be coupled to a target protein ligand via a linker to form a PROTAC molecule—such as a PROTAC degrader for MDM2 .

HY-169240

MX69-102	MDM-2/p53	Cancer
MX69-102 (compound MX69-102) is an *MDM-2/p53* inhibitor, inducing *MDM2* degradation, resulting in p53 activation and cancer cell apoptosis. MX69-102 shows effective inhibition on xenografted human MDM2-overexpressing ALL in SCID mice. .

HY-15510B

Tenovin-6 Hydrochloride 5 Publications Verification	MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy	Cancer
Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC₅₀s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH) .

HY-130122

MG-277 1 Publications Verification	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 .

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-122725

Lenalidomide-C5-NH2	E3 Ligase Ligand-Linker Conjugates	Others Cancer
Lenalidomide-C5-NH2 is an E3 ligase ligand-linker conjugate. Lenalidomide-C5-NH2 can be coupled to a target protein ligand via a linker to form a PROTAC molecule—such as a PROTAC degrader for MDM2 .

HY-106263B

Tyroserleutide hydrochloride	PTEN PDK-1 MDM-2/p53 Apoptosis Akt	Cancer
Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis .

HY-179055

PROTAC DAPK1 Degrader-1	PROTACs DAPK	Neurological Disease
PROTAC DAPK1 Degrader-1 (Compound CP1) is a DAPK1 PROTAC degrader with a DC₅₀ of 119.6 nM. PROTAC DAPK1 Degrader-1 significantly increased the *MDM2* protein level. PROTAC DAPK1 Degrader-1 significantly reduced the levels of cleaved caspase-3 and cleaved PARP in a cell apoptosis model induced by the neurotoxin ceramide, indicating that it effectively inhibits neuronal apoptosis by degrading DAPK1. PROTAC DAPK1 Degrader-1 can be used to study neurological diseases such as cerebral ischemia and traumatic brain injury (pink: DAPK1 ligand (HY-179071); blue: CRBN ligand (HY-10984); black: linker (HY-40171)) .

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-159728

PROTAC PRMT3 degrader 1	PROTACs Histone Methyltransferase Apoptosis Early 2 Factor (E2F) c-Myc	Cancer
PROTAC PRMT3 degrader 1 is a selective PRMT3 PROTAC degrader with a DC₅₀ of 2.566 μM. PROTAC PRMT3 degrader 1 forms a ternary complex with MDM2 E3 ubiquitin ligase to induce proteasomal and neddylation-dependent degradation of PRMT3. PROTAC PRMT3 degrader 1 activates intrinsic apoptosis, endoplasmic reticulum stress signaling pathways. PROTAC PRMT3 degrader 1 downregulates E2F, MYC, oxidative phosphorylation pathways. PROTAC PRMT3 degrader 1 reduces cellular asymmetric dimethylarginine (ADMA) levels. PROTAC PRMT3 degrader 1 inhibits acute leukemia cell growth. PROTAC PRMT3 degrader 1 acts with glycolysis inhibitor 2-DG to reduce ATP production, induce intrinsic apoptosis, drive synergistic antiproliferative effects. PROTAC PRMT3 degrader 1 can be used for the research of acute leukemia .

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. rel-PROTAC PARP1 degrader induces significant PARP1 cleavage and programmed cell death .

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-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 .

HY-123656

Antiproliferative agent-61	Apoptosis	Cancer
Antiproliferative agent-61 is a synthetic β-carlinyl chalcone with significant antiproliferative activity. Antiproliferative agent-61 showed significant effects in a range of solid tumor cell lines, with the most prominent effects in breast cancer. Antiproliferative agent-61 showed IC50 values of 2.25 and 3.29 μM in the human breast cancer MCF-7 cell line. Antiproliferative agent-61 significantly induced DNA fragmentation and apoptosis in breast cancer cells. Antiproliferative agent-61 inhibited the interaction of MDM2 with p53 and promoted the degradation of MDM2 .

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-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-12430

SP-141 hydrochloride	MDM-2/p53	Cancer
SP-141 (hydrochloride) is a specific inhibitor of *MDM2. SP-141 (hydrochloride) promotes MDM2* auto-ubiquitination and degradation. SP-141 (hydrochloride) might be used for the research of pancreatic cancer and breast cancer cells .

HY-174266

WB156	MDM-2/p53	Cancer
WB156 is a dual *MDM2* and GSPT1 degrader. WB156 can recruit CRBN (Cereblon, a substrate receptor of the E3 ubiquitin-ligase complex) to induce the ubiquitination-proteasome pathway-mediated degradation of MDM2 and GSPT1. WB156 is promising for research of cancers, such as leukemia .

HY-112816A

MA242 free base	MDM-2/p53 Apoptosis	Cancer
MA242 free base is a specific dual inhibitor of *MDM2* and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status .

HY-124070

ISA 27	MDM-2/p53	Cancer
ISA 27 is a small-molecule *MDM2-p53* protein-protein interaction inhibitor. ISA 27 inhibits MDM2-mediated p53 ubiquitination and degradation. ISA 27 is promising for research of p53-mutant solid tumors (e.g., thyroid, breast cancer) .

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-124739

HBX 28258	Deubiquitinase	Cancer
HBX 28258 is a selective USP7 inhibitor, with an IC₅₀ of 22.6 μM. HBX 28258 can covalently binds to Cys223 located in the catalytic core of USP7, inhibits its deubiquitinating activity, promotes MDM2 protein degradation, and activates p53 .

HY-122646

USP7-IN-2	Deubiquitinase MDM-2/p53	Cancer
USP7-IN-2 (compound 4) is a non-competitive USP7 inhibitor with an IC₅₀ of 6 nM. USP7-IN-2 causes degradation of *MDM2, stabilization of p53* and induction of p21 in multiple cell lines, and can be utilized in cancer research .

HY-174301

USP7-IN-18	Deubiquitinase DNA Methyltransferase MDM-2/p53	Cancer
USP7-IN-18 is a naphthalene derivative. USP7-IN-18 is a selective USP7 inhibitor (IC₅₀ : 130.9 nM), with no or very weak inhibition of the other 8 DUBs including USP47. USP7-IN-18 specifically binds to the catalytic domain of USP7, blocking its deubiquitinase activity. USP7-IN-18 causes degradation of the oncogenic proteins *MDM2* and DNMT1, and also degrades the novel target PCLAF. USP7-IN-18 activates the p53-p21 pathway. USP7-IN-18 exerts anti-tumor effects in colon cancer animal models and reshapes the tumor immune microenvironment. USP7-IN-18 achieves both direct cytotoxic and immune-synergistic anti-tumor actions.

HY-153200

MDM2/XIAP-IN-2	MDM-2/p53	Cancer
MDM2/XIAP-IN-2 is a dual inhibitor of murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP). MDM2/XIAP-IN-2 degrades MDM2, and inhibits XIAP mRNA translation to inhibits cancer cells. Particularly, MDM2/XIAP-IN-2 inhibits acute lymphoblastic leukemia cell line EU-1 with an IC₅₀ value of 0.3 μM .

HY-122725A

Lenalidomide-C5-NH2 TFA	E3 Ligase Ligand-Linker Conjugates	Cancer
Lenalidomide-C5-NH2 TFA is an E3 ligase ligand-linker conjugate. Lenalidomide-C5-NH2 TFA can be coupled to a target protein ligand via a linker to form a PROTAC molecule—such as a PROTAC degrader for MDM2 .

HY-164550

YF438	HDAC	Cancer
YF438 is an HDAC inhibitor with effective anticancer activity both in vitro and in vivo. YF438 inhibits the growth and metastasis of triple-negative breast cancer (TNBC) cells by blocking the interaction between HDAC and *MDM2, inducing the dissociation of MDM2-MDMX, and promoting the degradation* of *MDM2* .

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-172597

YL-1-9	MDM-2/p53 CDK Apoptosis	Cancer
YL-1-9 is an inhibitor of the degradation of p53 by MDM2 through strong binding to the key hydrophobic pockets of MDM2. YL-1-9 induces cell cycle arrest and apoptosis in breast cancer cells .

HY-133754

MI-1063	MDM-2/p53 Ligands for Target Protein for PROTAC	Cancer
MI-1063 is an inhibitor for *MDM-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-173369

PROTAC MAGL degrader-1	PROTACs MAGL	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-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) .

Cat. No.	Nom du produit

HY-L128

E3 Ligase Ligand Library

177 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 177 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.	Nom du produit	Target	Research Area

HY-106263B

Tyroserleutide hydrochloride	PTEN PDK-1 MDM-2/p53 Apoptosis Akt	Cancer
Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis .

Cat. No.	Nom du produit		Classification

HY-114312

MD-224 5+ Cited Publications		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-181358

(4R,5S)-Nutlin carboxylic acid-NHC2-PEG1-N3		Azide
(4R,5S)-Nutlin carboxylic acid-NHC2-PEG1-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (4R,5S)-Nutlin carboxylic acid based MDM2 ligand and a linker used in PROTAC technology. (4R,5S)-Nutlin carboxylic acid-NHC2-PEG1-N3 can be connected to the ligand for protein by a linker to form PROTAC EZH2 Degrader-29 (HY-181357) .

HY-180924

(4R,5S)-Nutlin carboxylic acid-NHC2-PEG2-N3		Azide
(4R,5S)-Nutlin carboxylic acid-NHC2-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (4R,5S)-Nutlin carboxylic acid based MDM2 ligand and a linker used in PROTAC technology. (4R,5S)-Nutlin carboxylic acid-NHC2-PEG1-N3 can be connected to the ligand for protein by a linker to form PROTAC EZH2 Degrader-30 (HY-181359) .

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