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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
42 Results for "
MDM2 PROTAC Degrader
" in MedChemExpress (MCE) Product Catalog:
Products (42)
42 Results for "MDM2 PROTAC Degrader" in MCE Product Catalog:
8
8 Publications Verification
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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.
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2 Cited Publications
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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 .
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1 Cited Publications
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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 .
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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) .
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1 Cited Publications
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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 .
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1 Cited Publications
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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 .
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1 Cited Publications
Cat. No.: HY-128838A
Purity: 98.18%
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(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 .
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 .
YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a Kd 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 .
Cat. No.: HY-128843
CAS No.: 2249750-24-9
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PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology .
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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 .
PROTAC PARP1 degrader is a PROTAC PARP1 degrader. PROTAC PARP1 degrader mediates the interaction between PARP1 and MDM2 E3 ubiquitin ligase, thereby inducing ubiquitination of PARP1 and subsequent proteasome-mediated degradation. PROTAC PARP1 degrader selectively inhibits the growth of breast cancer cells. PROTAC PARP1 degrader induces cell apoptosis by activating caspase-3 and phosphatidylserine externalization. PROTAC PARP1 degrader can be used in the research of triple-negative breast cancer .
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MCL-1/BCL-2-IN-2 is a Mcl-1 and Bcl-2 inhibitor with IC50 values of 5.4 and 7.66 μM. MCL-1/BCL-2-IN-2 is applicable to the research of Mcl-1-dependent cancers .
Cat. No.: HY-130991
CAS No.: 2378261-89-1
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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 .
Cat. No.: HY-179055
CAS No.: 3063030-38-3
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PROTAC DAPK1 Degrader-1 is a death-associated protein kinase 1 (DAPK1) degrader with a DC50 of 119.6 nM. PROTAC DAPK1 Degrader-1 significantly increases MDM2 protein levels and inhibits neuronal apoptosis in ceramide-induced cells. PROTAC DAPK1 Degrader-1 can be used to study neurological disorders such as cerebral ischemia and traumatic brain injury .
Cat. No.: HY-122725
CAS No.: 2093388-45-3
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 .
Cat. No.: HY-159728
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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 .
Cat. No.: HY-174458
MD-4251 is an orally active MDM2 PROTAC degrader with a DC50 of 0.2 nM in RS4;11 cells. MD-4251 induces cereblon-dependent depletion and degradation of MDM2 protein, elevates p53 protein levels and activates p53. MD-4251 inhibits the proliferation of wild-type p53 acute leukemia cells, induces complete and durable tumor regression in xenograft models, and upregulates the protein levels of DSC1, NBEA and CASP14. MD-4251 can be used in studies related to acute leukemia .
Cat. No.: HY-114324A
Purity: 98.99%
rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). PROTAC PARP1 degrader is a PROTAC PARP1 degrader. PROTAC PARP1 degrader mediates the interaction between PARP1 and MDM2 E3 ubiquitin ligase, thereby inducing ubiquitination of PARP1 and subsequent proteasome-mediated degradation. PROTAC PARP1 degrader selectively inhibits the growth of breast cancer cells. PROTAC PARP1 degrader induces cell apoptosis by activating caspase-3 and phosphatidylserine externalization. PROTAC PARP1 degrader can be used in the research of triple-negative breast cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
