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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
423 Results for "
ubiquitin proteasome
" in MedChemExpress (MCE) Product Catalog:
Products (423)
423 Results for "ubiquitin proteasome" in MCE Product Catalog:
37
37 Publications Verification
Cat. No.: HY-16954
CAS No.: 1818885-28-7
Target:
PROTACs Epigenetic Reader Domain c-Myc Polo-like Kinase (PLK) CDK JAK STAT Pim Bcl-2 Family PAK Wnt β-catenin Caspase PARP Apoptosis Reactive Oxygen Species (ROS)
Research Areas:
ARV-825 is a BET protein PROTAC degrader that recruits cereblon, and it targets BRD2, BRD3, and BRD4 for degradation via the ubiquitin-proteasome pathway. ARV-825 downregulates c-MYC, PLK1, MYCN, CDK4/6, JAK2, pSTAT3/5, PIM1, and Bcl-xL, upregulates p21 and p27, and modulates H3K27Ac-mediated transcription, the G2/M checkpoint, the Wnt/β-catenin pathway, and amino acid transport pathways. ARV-825 induces G1 phase cell cycle arrest, caspase 3/PARP-mediated apoptosis, DNA damage, and reactive oxygen species (ROS) production, reduces mitochondrial respiration, and simultaneously inhibits cell proliferation, clonogenic growth, and cell migration. ARV-825 is used in research on gastric cancer, leukemia, neuroblastoma, and cholangiocarcinoma .
26
26 Cited Publications
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Endocrinology Cancer
IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
7
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Arimoclomol maleate (BRX-220) is an orally active co-inducer of heat shock proteins (HSP) . Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system .Arimoclomol maleate can be used for the study of Niemann–Pick disease type C.
7
7 Cited Publications
Synonyms: BRX-220 free base
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Arimoclomol (BRX-220 free base) is an orally active co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.Arimoclomol can be used for the study of Niemann–Pick disease type C. Arimoclomol can cross the blood-brain barrier and can be used in research on Niemann-Pick disease type C .
7
7 Cited Publications
Synonyms: BRX-220 citrate
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Arimoclomol citrate (BRX-220 citrate) is an orally active co-inducer of heat shock proteins (HSP) . Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system . Arimoclomol citrate can be used for the study of Niemann–Pick disease type C.
6
6 Cited Publications
Cat. No.: HY-145514D
CAS No.: 2451573-86-5
dTAGV-1 is a selective FKBP12 F36V PORTAC degrader. dTAGV-1 induces rapid degradation of FKBP12 F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 is applicable to functional validation studies of cancer and undegradable oncoproteins .
6
6 Cited Publications
dTAGV-1 TFA is a selective FKBP12 F36V PORTAC degrader. dTAGV-1 TFA induces rapid degradation of FKBP12 F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 TFA is applicable to functional validation studies of cancer and undegradable oncoproteins .
6
6 Cited Publications
dTAGV-1 hydrochloride is a selective FKBP12 F36V PORTAC degrader. dTAGV-1 hydrochloride induces rapid degradation of FKBP12 F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 hydrochloride is applicable to functional validation studies of cancer and undegradable oncoproteins .
4
Research Areas:
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 .
4
4 Cited Publications
Target:
Research Areas:
RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
4
4 Cited Publications
Target:
Research Areas:
KB02-JQ1 is a potent and selective BRD4 PROTAC degrader. KB02-JQ1 degrades BRD4 via the ubiquitin-proteasome pathway by bridging DCAF16 E3 ubiquitin ligase and BRD4. KB02-JQ1 can be used for cancer research .
4
4 Cited Publications
Gefitinib-based PROTAC 3 is a PROTAC degrader targeting EGFR, with a DC50 of 11.7 nM against exon 19 deletion mutants and a DC50 of 22.3 nM against EGFR L858R. Gefitinib-based PROTAC 3 selectively induces the ubiquitin-proteasome degradation of exon 19 deletion-mutant and L858R-mutant EGFR by recruiting the VHL E3 ligase. Gefitinib-based PROTAC 3 can be used for the research of EGFR mutation-positive cancers .
4
4 Cited Publications
Research Areas:
MS4078 is a ALK PROTAC degrader with a DC50 of 11 nM in SU-DHL-1 cells and a DC50 of 59 nM in NCI-H2228 cells, and its Kd value for ALK binding is 19 nM. MS4078 induces ALK degradation via the ubiquitin-proteasome pathway by recruiting cereblon, and inhibits the phosphorylation of ALK and STAT3, thereby suppressing cancer cell proliferation. MS4078 is applicable for the research of non-small cell lung cancer and anaplastic large cell non-Hodgkin's lymphoma .
4
Target:
PROTACs FKBP Epigenetic Reader Domain HDAC Histone Methyltransferase c-Myc Polo-like Kinase (PLK) Ras MHC
Research Areas:
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 .
3
3 Cited Publications
Target:
Research Areas:
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 .
3
3 Cited Publications
Research Areas:
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
Cat. No.: HY-19726
CAS No.: 803647-40-7
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 .
2
2 Cited Publications
Cat. No.: HY-P1259A
Target:
Research Areas:
2
2 Cited Publications
Target:
Research Areas:
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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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
