Search Result

Results for "

MDM2 Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	MDM-2/p53 (135) Akt (2) AMPK (1) Apoptosis (50) Autophagy (7) Bcl-2 Family (2) Biochemical Assay Reagents (1) c-Myc (5) Calcium Channel (1) Caspase (7) CDK (2) COX (1) Cyclin G-associated Kinase (GAK) (1) Cyclophilin (1) Cytochrome P450 (2) DAPK (1) Deubiquitinase (8) Dihydroorotate Dehydrogenase (1) DNA Methyltransferase (1) Drug Derivative (1) Drug Intermediate (2) Drug Isomer (3) Drug-Linker Conjugates for ADC (1) DYRK (1) E1/E2/E3 Enzyme (41) Early 2 Factor (E2F) (1) Epigenetic Reader Domain (1) Ferroptosis (1) Fungal (3) HDAC (3) Herbicide (2) Histone Methyltransferase (1) IAP (3) IGF-1R (1) Interleukin Related (3) Isotope-Labeled Compounds (4) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (1) Lipoxygenase (1) LPL Receptor (1) MAGL (1) NF-κB (3) Notch (1) Parasite (1) PARP (4) PDK-1 (1) Pim (1) PROTACs (8) PTEN (1) Reactive Oxygen Species (ROS) (3) Reference Standards (7) Sirtuin (1) STAT (1) TGF-beta/Smad (1) TNF Receptor (1) Topoisomerase (3) Wnt (1) β-catenin (2)
By Research Areas:	Cancer (150) Cardiovascular Disease (2) Endocrinology (1) Infection (3) Inflammation/Immunology (7) Neurological Disease (7)

By Targets:

MDM-2/p53 (135)

Akt (2)

AMPK (1)

Apoptosis (50)

Autophagy (7)

Bcl-2 Family (2)

Biochemical Assay Reagents (1)

c-Myc (5)

Calcium Channel (1)

Caspase (7)

CDK (2)

COX (1)

Cyclin G-associated Kinase (GAK) (1)

Cyclophilin (1)

Cytochrome P450 (2)

DAPK (1)

Deubiquitinase (8)

Dihydroorotate Dehydrogenase (1)

DNA Methyltransferase (1)

Drug Derivative (1)

Drug Intermediate (2)

Drug Isomer (3)

Drug-Linker Conjugates for ADC (1)

DYRK (1)

E1/E2/E3 Enzyme (41)

Early 2 Factor (E2F) (1)

Epigenetic Reader Domain (1)

Ferroptosis (1)

Fungal (3)

HDAC (3)

Herbicide (2)

Histone Methyltransferase (1)

IAP (3)

IGF-1R (1)

Interleukin Related (3)

Isotope-Labeled Compounds (4)

Ligands for E3 Ligase (2)

Ligands for Target Protein for PROTAC (1)

Lipoxygenase (1)

LPL Receptor (1)

MAGL (1)

NF-κB (3)

Notch (1)

Parasite (1)

PARP (4)

PDK-1 (1)

Pim (1)

PROTACs (8)

PTEN (1)

Reactive Oxygen Species (ROS) (3)

Reference Standards (7)

Sirtuin (1)

STAT (1)

TGF-beta/Smad (1)

TNF Receptor (1)

Topoisomerase (3)

Wnt (1)

β-catenin (2)

By Research Areas:

Cancer (150)

Cardiovascular Disease (2)

Endocrinology (1)

Infection (3)

Inflammation/Immunology (7)

Neurological Disease (7)

159

Inhibitors & Agonists

Screening-Bibliotheken

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: MDM-2/p53

Art. -Nr.	Produktname	Target	Forschungsgebiete	Chemical Structure

HY-50696

Nutlin-3 40+ Cited Publications	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
Nutlin-3 is a commercial available *p53-MDM2* inhibitor, with K_i of 90 nM.

HY-15676

Idasanutlin 50+ Cited Publications RG7388	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
Idasanutlin (RG7388) is a potent and selective *MDM2* antagonist, inhibiting p53-MDM2 binding, with an IC₅₀ of 6 nM.

HY-10029

Nutlin-3a Maximum Cited Publications 66 Publications Verification Rebemadlin	MDM-2/p53 E1/E2/E3 Enzyme Autophagy Apoptosis	Cancer
Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC₅₀=90 nM). Nutlin-3a inhibits *MDM2-p53* interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas .

HY-152859

Brigimadlin BI 907828	E1/E2/E3 Enzyme MDM-2/p53	Cancer
Brigimadlin (BI 907828) is an orally active E3 ubiquitin-protein ligase *MDM-2* inhibitor, preventing MDM-2 from negatively regulating the tumor suppressor p53. Brigimadlin can be used for antineoplastic research .

HY-10959

RG7112 20+ Cited Publications RO5045337	MDM-2/p53 E1/E2/E3 Enzyme	Neurological Disease Cancer
RG7112 is a potent, selective, orally active and blood-brain barrier crossed *MDM2-p53* inhibitor, with an IC₅₀ of 18 nM and a K_D of 11 nM for binding to MDM2 .

HY-12296

Navtemadlin 20+ Cited Publications AMG 232; KRT-232	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of *p53-MDM2* interaction, with an IC₅₀ of 0.6 nM. Navtemadlin binds to MDM2 with a K_d of 0.045 nM .

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-101518

Alrizomadlin 4 Publications Verification APG-115; AA-115	MDM-2/p53 E1/E2/E3 Enzyme Apoptosis	Cancer
Alrizomadlin (APG-115) is an orally active *MDM2* protein inhibitor binding to MDM2 protein with IC₅₀ and K_i values of 3.8 nM and 1 nM, respectively . Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner .

HY-100892

MX69 2 Publications Verification	MDM-2/p53 IAP E1/E2/E3 Enzyme	Cancer
MX69 is an inhibitor of *MDM2/XIAP*, used for cancer treatment.

HY-18986

SAR405838 3 Publications Verification MI-77301	MDM-2/p53 E1/E2/E3 Enzyme Apoptosis	Cancer
SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective *MDM2-p53* interaction inhibitor. SAR405838 binds to MDM2 with a K_i of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity .

HY-18658

Siremadlin 10+ Cited Publications NVP-HDM201; HDM201	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
Siremadlin (NVP-HDM201) is a potent, orally bioavailable and highly specific *p53-MDM2* interaction inhibitor.

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-P4210

Sulanemadlin 1 Publications Verification ALRN-6924; MP-4897	MDM-2/p53	Cancer
Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research .

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-15954

NVP-CGM097 3 Publications Verification CGM097	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
NVP-CGM097 is a potent and selective *MDM2* inhibitor with IC₅₀ of 1.7±0.1 nM for hMDM2.

HY-15335

Nutlin-3b 1 Publications Verification	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
Nutlin-3b, the inactive form of Nutlin-3 (HY-50696), is a *p53/MDM2* inhibitor with an IC₅₀ of 13.6 μM. Nutlin-3b is 150 times less potent in binding to *MDM2* than Nutlin-3a (HY-10029). Nutlin-3b is promising for research of cancers .

HY-176083

ASTX295	MDM-2/p53 Caspase Apoptosis	Cancer
ASTX295 is an orally active and selective *MDM2* antagonist with an IC₅₀ of <1 nM. ASTX295 inhibits the *MDM2-p53* interaction, activates wild-type TP53, and thereby induces the expression of relevant transcriptional targets, leading to cell death. ASTX295 drives the transition of pancreatic cancer cells from senescence to apoptosis and regulates p53 and DNA damage biomarkers. ASTX295 can be used for the research of hematologic malignancies and pancreatic cancer .

HY-70027A

*p53 and MDM2* proteins-interaction-inhibitor dihydrochloride**	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
p53 and MDM2 proteins-interaction-inhibitor dihydrochloride (Compound 32) is an inhibitor of the interaction between p53 and *MDM2. p53 and MDM2* proteins-interaction-inhibitor dihydrochloride has potential applications in cancer research .

HY-17493

MI-773 5+ Cited Publications	MDM-2/p53 Apoptosis	Neurological Disease Cancer
MI-773 is an orally active, selective *MDM2-p53* interaction inhibitor with a K_i of 0.88 nM for MDM2. MI-773 blocks the *MDM2*-TP53 interaction. MI-773 potently activates p53. MI-773 induces Apoptosis. MI-773 causes tumor regression in xenograft models of adenoid cystic carcinoma. MI-773 exhibits anticancer effects in neuroblastoma. MI-773 TFA can be used for the research of adenoid cystic carcinoma .

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-125858

MI-1061 3 Publications Verification	MDM-2/p53 E1/E2/E3 Enzyme Apoptosis	Cancer
MI-1061 is a potent, orally bioavailable, and chemically stable *MDM2* (MDM2-p53 interaction) inhibitor (IC₅₀=4.4 nM; K_i=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity .

HY-120086

RO-5963 1 Publications Verification	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
RO-5963 is a dual *p53-MDM2* and p53-MDMX inhibitor with IC₅₀s of ~17 nM and ~24 nM, respectively .

HY-70027

*p53 and MDM2* proteins-interaction-inhibitor (chiral)**	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
p53 and MDM2 protein-interaction inhibitor (chiral) (Compound 32) is an inhibitor of the interaction between p53 and *MDM2. p53 and MDM2* protein-interaction inhibitor (chiral) has potential applications in cancer research .

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-163357

CDK2/MDM2-IN-1	CDK MDM-2/p53	Cancer
CDK2/MDM2-IN-1 (III-13) is a dual inhibitor of CDK2/MDM2 with an IC₅₀ value of 2.60 nM for CDK2. CDK2/MDM2-IN-1 has antitumor activity .

HY-148833

MDM2-p53-IN-16	MDM-2/p53	Cancer
MDM2-p53-IN-16 is a *MDM2-p53* complex inhibitor with an IC₅₀ value of 4.3 nM to dissociate human p53/MDM2 complex. MDM2-p53-IN-16 reactivates p53, and induces Glioblastoma Multiforme (GBM) cell apoptosis and cell-cycle arrest. MDM2-p53-IN-16 can be used for the cancer research .

HY-15676A

Idasanutlin (enantiomer) RG7388 (enantiomer)	MDM-2/p53 Drug Isomer Apoptosis	Cancer
Idasanutlin enantiomer is the isomer of Idasanutlin (HY-15676), and can be used as an experimental control. Idasanutlin (RG7388) is a potent and selective *MDM2* antagonist, inhibiting p53-MDM2 binding, with an IC₅₀ of 6 nM.

HY-15954B

NVP-CGM097 sulfate 3 Publications Verification CGM097 sulfate	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
NVP-CGM097 sulfate is a potent and selective *MDM2* inhibitor with IC₅₀ of 1.7±0.1 nM for hMDM2.

HY-76667

3-(Boc-amino)propyl bromide	MDM-2/p53 Biochemical Assay Reagents Drug Intermediate	Others
3-(Boc-amino) propyl bromide is an alkylating reagent used for the N-alkylation of benzopyranotriazolopyrimidine-based *MDM2-p53* protein-protein inhibitor 4 to prepare Compound 13 .

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-148106

MEL23	Ligands for E3 Ligase	Cancer
MEL23 is a MDM2 E3 ligase inhibitor that blocks the E3 ligase activity of the MDM2-MDMX complex. MEL23 inhibits Mdm2 and p53 ubiquitination in cells, reduce viability of cells with wild-type p53. MEL23 stabilizes MDM2 via a mechanism independent of p53 transcription .

HY-W340839

p53-MDM2-IN-1	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
p53-MDM2-IN-1 (Example 30) is an inhibitor of *p53-MDM2/X* protein interaction with an K_i value of 23.35 µM. p53-MDM2-IN-1 can be used for anti-tumor research .

HY-W340313

p53-MDM2-IN-4	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
p53-MDM2-IN-4 (Example 4) is an inhibitor of *p53-MDM2/X* protein interaction, with a K_i value of 3.079 μM. p53-MDM2-IN-4 can be used in anti-tumor research .

HY-12296A

(3S,5S,6R)-Navtemadlin (3S,5S,6R)-AMG 232; (3S,5S,6R)-KRT-232	MDM-2/p53	Cancer
(3S,5S,6R)-Navtemadlin is the isomer of Navtemadlin (HY-12296), and can be used as an experimental control. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of *p53-MDM2* interaction, with an IC₅₀ of 0.6 nM. Navtemadlin binds to MDM2 with a K_d of 0.045 nM .

HY-14967

NSC 66811 1 Publications Verification	MDM-2/p53	Cancer
NSC 66811 is a *MDM2-p53* inhibitor, with a K_i of 120 nM for binding to MDM2 .

HY-70028

*p53 and MDM2* proteins-interaction-inhibitor (racemic)**	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
p53 and MDM2 proteins-interaction-inhibitor (racemic) (Compound 2j) is an inhibitor of the interaction between p53 and MDM2 proteins.

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-133760

MI-888	MDM-2/p53	Cancer
MI-888 is an orally active *MDM2* inhibitor with a K_i of 0.44 nM. MI-888 can inhibit the *MDM2-p53* interaction. MI-888 has favorable pharmacokinetic properties and anti-tumor activity .

HY-124791

MMRi6	MDM-2/p53 PARP	Cancer
MMRi6 is a Mdm2-MdmX RING domain inhibitor that can disrupt Mdm2-MdmX RING-RING interaction in vitro. MMRi6 inhibits MdmX-stimulated *Mdm2* autoubiquitination and Mdm2-MdmX-mediated p53 polyubiquitination in vitro without affecting NEDD4-1 autoubiquitination. MMRi6 induces p53 stabilization and accumulation and induces PARP cleavage in wt-p53 Emu-myc lymphoma cells. MMRi6 inhibits the growth of wt-p53 and p53-null Emu-myc lymphoma cells with IC₅₀s of approximately 0.5 μM and 3 μM, respectively. MMRi6 can be used for the study of leukemia/lymphoma .

HY-149988

UNP-6457	MDM-2/p53	Cancer
UNP-6457 is a potent active *MDM2-p53* interaction inhibitor with an IC₅₀ values of 8.9 nM .

HY-10029A

(Rac)-Nutlin-3 (Rac)-Rebemadlin	MDM-2/p53 Autophagy Apoptosis E1/E2/E3 Enzyme	Cancer
(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC₅₀=90 nM). (Rac)-Nutlin-3 inhibits *MDM2-p53* interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas .

HY-P11256

pDI	MDM-2/p53	Cancer
pDI is a peptide. pDI inhibits *MDM2-p53* and MDMX-p53 interactions with IC₅₀s of 10 and 100 nM respectively. pDI can be used in the research of colorectal cancer .

HY-149250

MDMX/MDM2-IN-2	MDM-2/p53 Apoptosis	Cancer
MDMX/MDM2-IN-2 is a potent *p53-MDM2/MDMX* dual inhibitors with K_is of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively. MDMX/MDM2-IN-2 inhibits the binding of p53 and MDM2 proteins. MDMX/MDM2-IN-2 restores the function of p53 and enables cell cycle arrest and apoptosis. MDMX/MDM2-IN-2 inhibits cell migration and invasion. MDMX/MDM2-IN-2 has antitumor activity .

HY-18052

AM-8553	MDM-2/p53	Cancer
AM-8553 is a *MDM2/p53* inhibitor (K_D: 0.4 nM for MDM2). AM-8553 has anti-tumor activity

HY-18331

MI-219	MDM-2/p53	Cancer
MI-219 is an antagonist for *MDM2* with a K_i of 13.3 μM. MI-219 inhibits the *MDM2-p53* interaction, inhibits thus the proliferation of FSCCL cells, with an IC₅₀ of 2.5 μM .

HY-123544

RDR03871	MDM-2/p53	Cancer
RDR03871 (compound 2) is a potent dual *MDM2/MDM4* inhibitor with IC₅₀ values of 35.4 nM and 10.4 nM for MDM2-p53 and MDM4-p53, respectively .

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-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-12941

AM-7209	MDM-2/p53	Cancer
AM-7209 is a potent and selective *MDM2-p53* interaction inhibitor with a K_d of 38 pM. AM-7209 inhibits the MDM2 amplified SJSA-1 osteosarcoma cell line with an IC₅₀ of 1.6 nM. AM-7209 shows antitumor activities .

Art. -Nr.	Produktname

HY-L109

Protein-protein Interaction Inhibitor Library

797 compounds

Protein protein interactions (PPI) have pivotal roles in life processes. The studies showed that aberrant PPI are associated with various diseases, including cancer, infectious diseases, and neurodegenerative diseases. The classic drug targets are usually enzymes, ion channels, or receptors, the PPI indicate new potential therapeutic targets. Therefore, targeting PPI is a new direction in treating diseases and an essential strategy for the development of new drugs.

However, the design of modulators targeting PPI still faces tremendous challenges, such the difficult PPI interfaces for the drug design, lack of ligands reference, lack of guidance rules for the PPI modulators development and high-resolution PPI proteins structures.

With the development of high-throughput technology, high-throughput screening is also gradually used for the identification of PPI inhibitors, but the compound library used for conventional target screening is not very effective in screening PPI inhibitors. To improve screening efficiency, MCE carefully selected 797 PPI inhibitors and mainly targeting MDM2-p53, Keap1-Nrf2, PD-1/PD-L1, Myc-Max, etc. MCE Protein-protein Interaction Inhibitor Library is a useful tool for PPI drug discovery and related research.

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.

Art. -Nr.	Produktname	Target	Research Area

HY-P4210

Sulanemadlin 1 Publications Verification ALRN-6924; MP-4897	MDM-2/p53	Cancer
Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research .

HY-141584

ATSP-7041	MDM-2/p53	Cancer
ATSP-7041, a selective dual peptide inhibitor of *MDM2* and MDMX, effectively reactivates the p53 tumor suppressor pathway in a mechanism-dependent manner in p53-positive cancers .

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-P11256

pDI	MDM-2/p53	Cancer
pDI is a peptide. pDI inhibits *MDM2-p53* and MDMX-p53 interactions with IC₅₀s of 10 and 100 nM respectively. pDI can be used in the research of colorectal cancer .

HY-P10914

D-CopA3	MDM-2/p53 Autophagy	Inflammation/Immunology Cancer
D-CopA3 is the inhibitor for *MDM2* and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC₅₀=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .

HY-P11490

DPMI-ω	MDM-2/p53	Inflammation/Immunology Cancer
DPMI-ω is a dual-specificity d-peptide antagonist of oncogenic proteins *MDM2* and MDMX. DPMI-ω, upon fabrication on gold nanoparticles, efficiently traverses tumor cells and kills them by reactivating the p53 signaling pathway. DPMI-ω can disrupte the p53-MDM2/MDMX complex. DPMI-ω can inhibit B16 melanoma growth and induce cells G0/G1 phase arrest. DPMI-ω can augment the efficacy of immunotherapy by expanding CD3 ⁺/CD8 ⁺ cytotoxic T cells and suppressing CD4 ⁺/CD25 ⁺ regulatory T cells companied with anti-PD1 antibody. DPMI-ω can be used for research of melanoma .

Art. -Nr.	Produktname	Category	Target	Chemical Structure

HY-N0068

Solasodine 5 Publications Verification Purapuridine; Solancarpidine; Solasodin	Infection Cardiovascular Disease Alkaloids Piperidine Alkaloids Neurological Disease Classification of Application Fields Solanum nigrum Linn. Solanaceae Plants Inflammation/Immunology Disease Research Fields Source Classification	MDM-2/p53 Fungal E1/E2/E3 Enzyme Apoptosis
Solasodine (Purapuridine) is a steroidal alkaloid that occurs in plants of the Solanaceae family. Solasodine induces apoptosis by inhibiting the *p53-MDM2* complex**, p21Waf1/Cip1, and Bcl-2 proteins. Solasodine has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities .

HY-N7012

7,3',4'-Tri-O-methylluteolin 1 Publications Verification 5-Hydroxy-3',4',7-trimethoxyflavone	Monophenols Flavonoids Classification of Application Fields Flavones Labiatae Phenols Plants Swartzia polyphylla DC. Inflammation/Immunology Disease Research Fields Source Classification	Lipoxygenase TNF Receptor Interleukin Related COX Fungal Parasite Apoptosis
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid with multiple biological activities. 7,3',4'-Tri-O-methylluteolin inhibits soybean lipoxygenase (LOX), with an IC₅₀ value of 23.97 µg/mL. 7,3',4'-Tri-O-methylluteolin possesses anti-inflammatory effects in Lipopolysaccharides (HY-D1056) (LPS)-induced RAW 264.7 macrophages. 7,3',4'-Tri-O-methylluteolin inhibits the binding of MDM2 with p53 and induces apoptosis in MCF-7 breast cancer cells. 7,3',4'-Tri-O-methylluteolin also has antioxidant, antifungal and antitrypanosomal activities sup>[4]sup>[5].

HY-N12768

Rhodojaponin VI	Structural Classification Terpenoids Diterpenoids Pieris japonica (Thunb.) D. Don ex G. Don Ericaceae Plants Source Classification	MDM-2/p53 Notch Calcium Channel
Rhodojaponin VI is an orally active diterpenoid compound found in hododendron molle G. Don (Ericaceae) (RM). Rhodojaponin VI binds rat N-Ethylmaleimide-sensitive fusion (NSF) with a Kd of 1.03 μM. Rhodojaponin VI blocks the *MDM2-Notch1* signalling pathway by reducing *MDM2* and Notch1 expression. Rhodojaponin VI indirectly reduces Cav_2.2 current intensity by inhibiting NSF-mediated Cav2.2 trafficking. Rhodojaponin VI alleviates glomerulonephritis progression and podocyte injury in passive heymann nephritis rats. Rhodojaponin VI also has antinociceptive effects. Rhodojaponin VI can be used for the researches of heymann nephritis and pain .

Art. -Nr.	Produktname	Chemical Structure

HY-153939S

Idasanutlin-d3-1
Idasanutlin-d₃-1 (RG7388-d₃-1) is the deuterium labeled Idasanutlin. Idasanutlin is a potent antagonist of *MDM2/p53*. Idasanutlin inhibits relapsed or refractory acute myeloid leukemia .

HY-12296S

Navtemadlin-d7
Navtemadlin-d₇ is the deuterium labeled Navtemadlin. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC₅₀ of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM .

HY-18986S

SAR405838-d10
SAR405838-d₁₀ (MI-77301-d₁₀) is the deuterium labeled SAR405838 (HY-18986). SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective *MDM2-p53* interaction inhibitor. SAR405838 binds to MDM2 with a K_i of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity .

HY-W704348

Diphenyltin Dichloride-d10
Diphenyltin Dichloride-d₁₀ is the deuterium labeled NSC405640 (HY-144105). NSC405640 is a potent inhibitor of the MDM2-p53 interaction. NSC405640 rescues structural p53 mutations. NSC405640 selectively inhibits the growth of cell lines with wild-type p53 .

Online-Anfrage

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Anrede			Country or Region *
Name des Antragstellers *			Name der Organisation *
Department *
E-Mail-Addresse *			Produktname *
Art. -Nr.			Requested quantity *
Telefonnummer *
Bemerkungen