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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
177 Results for "
proteasome complex
" in MedChemExpress (MCE) Product Catalog:
Products (177)
177 Results for "proteasome complex" in MCE Product Catalog:
2269
2269 Publications Verification
Synonyms: Z-Leu-Leu-Leu-al; MG132
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MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis .
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9 Cited Publications
Synonyms: ARV-471; PF-07850327
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Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
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PROTACs FKBP Epigenetic Reader Domain HDAC Histone Methyltransferase c-Myc Polo-like Kinase (PLK) Ras MHC
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FKBP12 PROTAC dTAG-7 (dTAG-7) is a FKBP12 F36V PROTAC degrader. FKBP12 PROTAC dTAG-7 binds FKBP12 F36V and CRBN to form a complex, mediating degradation via the ubiquitin-proteasome system. FKBP12 PROTAC dTAG-7 mediates the degradation of FKBP12 F36V-tagged nuclear and cytoplasmic proteins, including BRD4, HDAC1, EZH2, MYC, PLK1, KRAS G12V, and antigen fusion proteins. FKBP12 PROTAC dTAG-7 enhances MHC class I antigen presentation. FKBP12 PROTAC dTAG-7 is applicable to leukemia-related research .
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BETd-260 (ZBC 260) is a BET PROTAC degrader. BETd-260 recruits BRD2, BRD3, and BRD4 to the CUL4-RBX1-DDB1-CRBN E3 ubiquitin ligase complex, driving cereblon-, proteasome-, and NEDD8-activating enzyme-dependent ubiquitination and degradation, with a DC50 of approximately 30-100 pM in RS4;11 cells. BETd-260 induces cancer cell apoptosis via endogenous signaling pathways, regulates the expression of the Bcl-2 family, inhibits the oncogene c-Myc, and reduces cell viability. BETd-260 suppresses tumor growth in mouse xenograft models with good biosafety. BETd-260 can be used in research related to acute leukemia, hepatocellular carcinoma, osteosarcoma, and triple-negative breast cancer .
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3 Cited Publications
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CFT8634 is an orally active BRD9 PROTAC degrader with a DC50 of 0.003 μM (HEK293T.166). CFT8634 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, triggering CRBN-catalyzed BRD9 polyubiquitination and 26S proteasome-mediated degradation. CFT8634 induces sustained tumor regression and inhibits tumor growth in mouse models. CFT8634 can be used in research related to synovial sarcoma, SMARCB-1-deficient cancers, acute myeloid leukemia, malignant rhabdoid tumors, and multiple myeloma .
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2 Cited Publications
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MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes .
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2 Cited Publications
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MZP-54 is a PROTAC degrader that selectively targets BRD3/BRD4, with a DC50 of < 0.05 μM in AML cells. MZP-54 recruits VHL to form a ternary complex, induces BRD3/BRD4 degradation via the ubiquitin-proteasome pathway, inhibits c-Myc expression, and exerts antiproliferative activity. MZP-54 can be used for the research of acute myeloid leukemia .
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2 Cited Publications
ARV-393 is a BCL6 PROTAC degrader. ARV-393 forms a complex with BCL6 and Cereblon, induces BCL6 ubiquitination, and mediates BCL6 degradation via the ubiquitin-proteasome system. ARV-393 enhances CD20 expression, interferon pathway activity and antigen presentation. ARV-393 induces tumor growth inhibition and regression. ARV-393 can be used in research related to non-Hodgkin's lymphoma, high-grade B-cell lymphoma, diffuse large B-cell lymphoma, Burkitt's lymphoma and follicular lymphoma .
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2 Cited Publications
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PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research .
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2 Cited Publications
Cat. No.: HY-162318
CAS No.: 2946670-96-6
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MYC degrader 1 is a MYC degrader that recruits Cereblon (CRBN), with a Kd value of 145 nM and oral activity. MYC degrader 1 specifically binds MYC and GSPT1, recruits the CRBN E3 ubiquitin ligase complex, and induces MYC degradation via the ubiquitin-proteasome pathway. MYC degrader 1 downregulates KLHL42 expression, restores pRB1 protein levels, and re-establishes the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors. MYC degrader 1 combined with Palbociclib (HY-50767) shows significant inhibition of tumor growth. MYC degrader 1 can be used in studies related to bladder cancer, prostate cancer, and breast cancer .
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2 Cited Publications
Cat. No.: HY-162318A
MYC degrader 1 TFA is a MYC degrader that recruits Cereblon (CRBN), with a Kd value of 145 nM and oral activity. MYC degrader 1 TFA specifically binds MYC and GSPT1, recruits the CRBN E3 ubiquitin ligase complex, and induces MYC degradation via the ubiquitin-proteasome pathway. MYC degrader 1 TFA downregulates KLHL42 expression, restores pRB1 protein levels, and re-establishes the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors. MYC degrader 1 TFA combined with Palbociclib (HY-50767) shows significant inhibition of tumor growth. MYC degrader 1 TFA can be used in studies related to bladder cancer, prostate cancer, and breast cancer .
1
1 Cited Publications
XIAP degrader-1 is a PROTAC-like degrader with a Kd value of 1 μM for XIAP. XIAP degrader-1 is metabolized into an active aldehyde species that covalently binds to Cys326 of FBXO22, thereby forming a ternary complex with the BIR2 domain of XIAP. XIAP degrader-1 induces polyubiquitination and proteasomal degradation of XIAP via the ubiquitin-proteasome system, a process dependent on NEDD8 conjugation, the SCF FBXO22 ligase complex, as well as the functional activities of XIAP ligase, E1 and the proteasome .
1
1 Cited Publications
Homo-PROTAC pVHL30 degrader 1 is a Homo-PROTAC autodegraders targeting the von Hippel-Lindau E3 ubiquitin ligase (VHL), with Kd values of 11 nM and 25 nM for pVHL19-EloBC and pVHL30-EloBC, respectively. Homo-PROTAC pVHL30 degrader 1 induces Cullin2 depletion, promotes VHL dimerization to form a ternary complex, and drives proteasome-dependent and CRL2-VHL-like ubiquitination-dependent autodegradation. Homo-PROTAC pVHL30 degrader 1 does not trigger hypoxic responses, and only causes extremely mild stabilization of hypoxia-inducible factor α subunits. Homo-PROTAC pVHL30 degrader 1 can be used in studies related to cervical cancer and osteosarcoma .
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PROTAC IDO1 Degrader-1 is a potent IDO1 (Indoleamine 2,3-dioxygenase 1) PROTAC degrader with a DC50 of 2.84 μM. PROTAC IDO1 Degrader-1 forms a ternary complex with IDO1 and the CRBN E3 ligase, and induces polyubiquitination of IDO1 followed by proteasomal degradation via the ubiquitin-proteasome system. PROTAC IDO1 Degrader-1 is applicable for related research on cancer immunity .
Cat. No.: HY-P11306
CAS No.: 247068-92-4
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Cat. No.: HY-49444
CAS No.: 793719-01-4
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EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .
Synonyms: ASC-JM17; ALZ-003
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Keap1-Nrf2 Androgen Receptor HSP Mitophagy Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Autophagy
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Rosolutamide (ASC-JM17) is an orally active Nrf1/Nrf2 activator. Rosolutamide activates Hsf1 pathways, upregulates proteasome subunits and antioxidant enzymes, induces proteasome complex structural rearrangement, and enhances ubiquitin-proteasome system-mediated degradation. Rosolutamide reduces mutant androgen receptor and ataxin-3 aggregates, restores mitochondrial function, attenuates reactive oxygen species (ROS) levels, induces apoptosis and ferroptosis, and inhibits cancer cell growth. Rosolutamide can be used for the research of spinal and bulbar muscular atrophy, Huntington’s disease, and temozolomide-resistant glioblastoma .
Cat. No.: HY-P4284
CAS No.: 35172-59-9
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Cat. No.: HY-176792
CAS No.: 3097985-19-5
ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader, with Kd values of 141 nM against KRAS G12R. ACBI-4 forms a stable ternary complex with VHL, triggering ubiquitination and KRAS degradation via the ubiquitin-proteasome system. ACBI-4 induces antiproliferative effects in KRAS mutant-driven cancer cells. ACBI-4 can be used for the research of KRAS mutant-driven cancer .
Cat. No.: HY-159779
CAS No.: 2766608-52-8
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NR-V04 is a selective NR4A1 PROTAC degrader. NR-V04 forms a ternary complex with NR4A1 and the VHL E3 ligase, mediates proteasome-dependent degradation of NR4A1. NR-V04 induces tumor-infiltrating B cells and effector memory CD8 + T cells and reduces monocytic myeloid-derived suppressor cells in tumor microenvironments. NR-V04 can be used for the research of melanoma and colon 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
