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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
309 Results for "
ubiquitin-proteasome systems
" in MedChemExpress (MCE) Product Catalog:
Products (309)
309 Results for "ubiquitin-proteasome systems" in MCE Product Catalog:
4
Target:
PROTACs FKBP Epigenetic Reader Domain HDAC Histone Methyltransferase c-Myc Polo-like Kinase (PLK) Ras MHC
Forschungsgebiete:
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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3 Cited Publications
Forschungsgebiete:
A1874 is an orally active BRD4 PROTAC degrader with a DC50 of 32 nM. A1874 degrades BRD4 via the ubiquitin-proteasome system by recruiting the MDM2 E3 ligase, while disrupting the MDM2-p53 interaction to stabilize p53 and upregulate p21, thereby inducing cell cycle arrest and apoptosis. A1874 exhibits selectivity for wild-type p53 cells and MDM2-amplified tumors, and it can be used in research on breast cancer, colorectal cancer, melanoma, lung cancer, lymphoma, myeloid leukemia, osteosarcoma, and glioblastoma .
2
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 .
2
2 Cited Publications
Target:
Forschungsgebiete:
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 .
2
2 Cited Publications
Target:
Forschungsgebiete:
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 .
2
2 Cited Publications
Art. -Nr.: HY-163410
CAS. Nr.: 3084244-26-5
Target:
Forschungsgebiete:
AU-24118 is an orally active PROTAC degrader that recruits cereblon to target the degradation of SMARCA2, SMARCA4 and PBRM1. AU-24118 impairs the chromatin accessibility of oncogenic transcription factors, inhibits colony formation, dislodges chromatin-bound transcription factors, attenuates downstream signal transduction, induces apoptosis, and exerts antiproliferative and cytotoxic effects. AU-24118 can be used in research related to castration-resistant prostate cancer, colorectal cancer, small cell lung cancer and multiple myeloma (including the t (4;14) subtype) .
1
1 Cited Publications
XZ739 is a potent and selective BCL-XL PROTAC degrader with a DC50 of 2.5 nM. XZ739 recruits CRBN to ubiquitinate and degrade BCL-XL via the ubiquitin-proteasome system. XZ739 also induces cell cycle arrest and caspase-mediated apoptosis. XZ739 can be used in research related to T-cell acute lymphoblastic leukemia and cholangiocarcinoma .
1
1 Cited Publications
Target:
Forschungsgebiete:
PROTAC B-Raf degrader 1 is a PROTAC degrader targeting B-Raf, which recruits the ubiquitin-proteasome system to accelerate B-Raf degradation and reduce the expression of downstream Mcl-1. PROTAC B-Raf degrader 1 inhibits cancer cell proliferation, arrests cell cycle and induces apoptosis. PROTAC B-Raf degrader 1 can be used in breast cancer-related research .
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
Art. -Nr.: HY-139606
CAS. Nr.: 2630950-38-6
VCP/p97 inhibitor-1 is a potent inhibitor of VCP/p97 (also called Cdc48, CDC-. 48, or Ter94) with an IC50 of 54.7 nM. VCP/p97 inhibitor-1 causes the dysregulation of protein homeostasis and disturbs the degradation of misfolded polypeptides by the ubiquitin-proteasome system (UPS) .
1
1 Cited Publications
Art. -Nr.: HY-W054146
CAS. Nr.: 145888-79-5
Target:
Forschungsgebiete:
RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity .
1
Forschungsgebiete:
Zomiradomide (KT-413) is an orally active IRAK4 PROTAC degrader with a DC50 of 6 nM. Zomiradomide inhibits the NF-κB signaling pathway, while its molecular glue function mediates the degradation of Ikaros and Aiolos (with a DC50 of 1 nM for both), activates the IFN-I signaling pathway, and selectively degrades IMiD substrates. Zomiradomide inhibits cancer cell proliferation and tumor growth. Zomiradomide can be used in research related to B-cell non-Hodgkin's lymphoma and diffuse large B-cell lymphoma .
1
1 Cited Publications
Target:
Forschungsgebiete:
AD4 is a PROTAC that induces the degradation of PCLAF by recruiting cereblon. AD4 is also an artemisinin derivative. AD4 directly binds to PCLAF with a KD of 6.1 μM, and induces apoptosis and G1-phase cell cycle arrest. By degrading PCLAF, AD4 upregulates p21, reduces Rb phosphorylation, downregulates Bcl-2 and upregulates Bax, thereby activating the p21/Rb axis. AD4 can be used in studies related to acute B-lymphoblastic leukemia and PCLAF-dependent anticancer mechanisms .
Art. -Nr.: HY-172162
Target:
Forschungsgebiete:
LC-04-045 is a selective NIMA-related kinase 7 (NEK7) molecular glue degrader. LC-04-045 induces NEK7 degradation via the CRBN-based ubiquitin-proteasome system, dependent on the glycine 57-containing degron motif. LC-04-045 inhibits secretion of downstream cytokines IL-1β and IL-18. LC-04-045 can be used for the research of lymphoblastic leukemia .
Target:
Forschungsgebiete:
HQ005 is a potent CCNK degrader with an DC50 value of 0.041 µM. HQ005 is a molecular-glue degrader that mediates interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation .
Art. -Nr.: HY-162250
CAS. Nr.: 3050872-59-5
Target:
Forschungsgebiete:
MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC50=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer .
Art. -Nr.: HY-176792
CAS. Nr.: 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 .
Target:
Forschungsgebiete:
USP28-IN-4 is a USP28 inhibitor (IC50=0.04 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-4 also decreases the ankyrase-1/2 level in vitro. USP28-IN-4 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331) .
Synonyms: ASC-JM17; ALZ-003
Target:
Keap1-Nrf2 Androgen Receptor HSP Mitophagy Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Autophagy
Forschungsgebiete:
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 .
PROTAC BCR-ABL Degrader-1 is a PROTAC degrader targeting BCR-ABL, and also selectively inhibits cancer cell proliferation. PROTAC BCR-ABL Degrader-1 induces degradation via the ubiquitin-proteasome system to reduce protein levels. PROTAC BCR-ABL Degrader-1 can be used for research on chronic myeloid leukemia .
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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
