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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
246 Results for "
Proteasome pathway
" in MedChemExpress (MCE) Product Catalog:
Products (246)
246 Results for "Proteasome pathway" 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 .
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
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
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 .
3
3 Cited Publications
Cat. No.: HY-P5819
3
3 Cited Publications
Cat. No.: HY-P5819A
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:
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2
2 Cited Publications
Cat. No.: HY-N4225
CAS No.: 85547-22-4
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 .
1
1 Cited Publications
Cat. No.: HY-P10899
Target:
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1
1 Cited Publications
Target:
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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 .
1
1 Cited Publications
Cat. No.: HY-W012985
CAS No.: 600-22-6
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Research Areas:
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 .
1
1
1 Cited Publications
Cat. No.: HY-162318
CAS No.: 2946670-96-6
Research Areas:
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 .
1
1 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 .
Synonyms: Cbl-b-IN-3
Target:
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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 .
Synonyms: 14-D-Valine-TPL
Target:
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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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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
