186 Results for "

proteasome pathway

" in MedChemExpress (MCE) Product Catalog:
Products (186)

186 Results for "proteasome pathway" in MCE Product Catalog:

25
25 Publications Verification
Cat. No.: HY-13817
CAS No.: 314245-33-5
Purity:  99.30%
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 .
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3
3 Cited Publications
Cat. No.: HY-P5819
Target:  

Wnt PROTACs β-catenin

Research Areas:  

Cancer

xStAx-VHLL is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL can inhibit the proliferation of colon cancer cells and has anti-tumor activity .
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3
3 Cited Publications
Cat. No.: HY-P5819A
Target:  

PROTACs β-catenin Wnt

Research Areas:  

Cancer

xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity .
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2
2 Cited Publications
Cat. No.: HY-19726
CAS No.: 803647-40-7
Target:  

MDM-2/p53

Research Areas:  

Cancer

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 .
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2
2 Cited Publications
Cat. No.: HY-N4225
CAS No.: 85547-22-4
Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects .
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2
2 Cited Publications
Cat. No.: HY-P1259A
Target:  

Proteasome Bacterial

Research Areas:  

Inflammation/Immunology

PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
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1
1 Cited Publications
Cat. No.: HY-158105
CAS No.: 2851885-95-3
Purity:  99.43%
Target:  

PROTACs BCL6 CD20 IFNAR

Research Areas:  

Cancer

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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1
1 Cited Publications
Cat. No.: HY-P10899
Target:  

PROTACs TGF-beta/Smad

Research Areas:  

Endocrinology

ETTAC-2 is a LRG1 PROTAC degrader, degrading LRG1 via the ubiquitin-proteasome pathway with a DC50 value of 8.38 μM. ETTAC-2 penetrates damaged renal cells to reduce the extracellular secretion of LRG1. ETTAC-2 effectively inhibits the TGF-β-Smad3 signaling pathway and diminishes the secretion of fibrosis-associated extracellular matrix proteins. ETTAC-2 degrades LRG1 within fibrotic kidneys and the efficacy in inhibiting the TGF-β-Smad3 pathway both in vitro and vivo. ETTAC-2 can be used for renal fibrosis research .
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1
1 Cited Publications
Cat. No.: HY-153896
CAS No.: 2764850-23-7
Purity:  98.74%
Target:  

c-Met/HGFR

Research Areas:  

Cancer

LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM),that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM .
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1
1 Cited Publications
Cat. No.: HY-W012985
CAS No.: 600-22-6
Methyl pyruvate is a p53/p21 axis inhibitor, intrinsic apoptosis inhibitor, cytotoxic agent, ATP production enhancer, proteasome function restorer, TDP-43 localization normalizer, ATP-sensitive potassium (K +ATP) channel inhibitor, depolarizer, and insulin secretagogue .Methyl pyruvate turns off apoptotic pathways, induces cancer cell death, acts as a substrate for dimeric dihydrodiol dehydrogenase, enhances TCA cycle activity, rescues proteasome impairment and TDP-43 mislocalization, inhibits K +ATP channels independent of ATP, depolarizes pancreatic β-cell membranes, modulates insulin secretion, and enters pancreatic β-cell mitochondria via a specific transporter .Methyl pyruvate can be used for the research of lung adenocarcinoma, ovarian clear cell adenocarcinoma, breast adenocarcinoma, amyotrophic lateral sclerosis, and type II diabetes .
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1
1 Cited Publications
Cat. No.: HY-N6929
CAS No.: 565-63-9
Angelic acid is a ferroptosis inducer, targeting NRF2 degradation. Angelic acid binds to NRF2 protein and promotes NRF2 degradation via ubiquitination-proteasome pathway, relieves the inhibitory effect of NRF2 on oxidative stress and lipid peroxidation. Then, Angelic acid induces ferroptosis in tumor cells. Angelic acid can enhance the accumulation of intracellular reactive oxygen species (ROS), upregulate ferroptosis-related markers CHAC1 and PTGS2, and synergize with ferroptosis inducers to enhance anti-tumor effects. Angelic acid also has the activity of scavenging UVA-induced ROS in vitro, inhibiting skin fibroblast senescence and extracellular matrix degradation. Angelic Acid helps wound healing with sedative activity .
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Cat. No.: HY-141432
CAS No.: 2573775-59-2
Purity:  99.87%
Synonyms: Cbl-b-IN-3
Target:  

E1/E2/E3 Enzyme

Research Areas:  

Cancer

NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research .
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Cat. No.: HY-145898
CAS No.: 2095780-08-6
Purity:  ≥95.0%
Synonyms: 14-D-Valine-TPL
Target:  

c-Myc Molecular Glues

Research Areas:  

Cancer

WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c-Myc molecule glue degrader. WBC100 is a c-Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c-Myc overexpressing tumors research .
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Cat. No.: HY-N6013
CAS No.: 8015-61-0
Aloin (mixture of A&B) is an orally active anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) mitigates airway impairment and exerts neuroprotective, anti-inflammatory, antioxidant, antibacterial, antifungal, antiviral and antitumor effects. Aloin (mixture of A&B) inhibits Clostridium histolyticum collagenase, granulocyte matrix metalloproteinases and human 20S proteasome. Aloin (mixture of A&B) upregulates the Nrf2/HO-1 pathway, suppresses the TGF-β/Smad2/3 pathway. Aloin (mixture of A&B) reduces IL-4/IL-5/IL-13 levels, and reverses oxidative stress markers (MDA, SOD, GSH). Aloin (mixture of A&B) can be used for research on chronic ulcers, burns, wounds, inflammatory and degenerative disorders, asthma and neuroblastoma .
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Cat. No.: HY-174864
CAS No.: 3100147-70-1
Target:  

PROTACs NF-κB Apoptosis

Research Areas:  

Cancer

JP-163-16 is a RelA/p65 PROTAC degrader. JP-163-16 selectively reduces the expression of RelA/p65 in a proteasome-dependent manner in cells. JP-163-16 can induce cell apoptosis by inhibiting the NF-κB signaling pathway. JP-163-16 can be used for research on RelA/p65-dependent tumours, such as chronic lymphocytic leukaemia (CLL) .
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Cat. No.: HY-P99672
CAS No.: 1509928-04-4
Synonyms: MM 141; MM-005

Target:  

IGF-1R EGFR

Research Areas:  

Cancer

Istiratumab (M-6495) is bispecific monoclonal antibody targeting IGF-1R and ErbB3. Istiratumab induces IGF-1R and ErbB3 receptor degradation through the proteasome pathway Istiratumab can be used for research of cancers .
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Cat. No.: HY-176528
CAS No.: 2919963-24-7
Target:  

ERK PROTACs

Research Areas:  

Cancer

PROTAC ERK5 degrader-1 (compound 2) is a bifunctional ERK5 PROTAC degrader. PROTAC ERK5 degrader-1 induces ERK5 degradation via VHL-mediated proteasome pathway in MOLT-4 cells. PROTAC ERK5 degrader-1 can be used for the study of a disease or disorder characterized by aberrant ERK5 activity, such as acute lymphoblastic leukemia .
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Cat. No.: HY-149760
CAS No.: 3032975-48-4
Research Areas:  

Cancer

PVD-06 is a selective PROTAC PTPN2 degrader with a DC50 of 217 nM (selectivity index >60-fold over PTP1B). PVD-06 induces PTPN2 degradation via a VHL-, ubiquitin, and proteasome-dependent pathway. PVD-06 can promote T cell activation and amplify IFN-γ-mediated anticancer activity. PVD-06 can be used to further investigate PTPN2 in diseases such as leukemia and melanoma .
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Cat. No.: HY-172208
CAS No.: 3118499-89-8
Research Areas:  

Inflammation/Immunology

PROTAC cGAS degrader-1 is a potent and selective cGAS PROTAC degrader, with DC50 values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 induces proteasome-mediated degradation of cGAS, inhibits the cGAS signaling pathway, and attenuates double-stranded DNA-induced activation of cGAS in human and mouse cells. PROTAC cGAS degrader-1 is applicable to research related to ulcerative colitis .
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Cat. No.: HY-136242
CAS No.: 2168525-92-4
Purity:  98.09%
Target:  

Estrogen Receptor/ERR

Research Areas:  

Endocrinology Cancer

UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
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