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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
371 Results for "
proteasomal degradation
" in MedChemExpress (MCE) Product Catalog:
Products (371)
371 Results for "proteasomal degradation" in MCE Product Catalog:
494
494 Publications Verification
Target:
Research Areas:
MK-2206 is an orally active pan-AKT inhibitor, with IC50 values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia .
494
494 Publications Verification
Synonyms: MK-2206 (2HCl)
Target:
Research Areas:
MK-2206 dihydrochloride (MK-2206 2HCl) is an orally active pan-AKT inhibitor, with IC50 values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 dihydrochloride inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 dihydrochloride induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 dihydrochloride causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 dihydrochloride can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia .
70
70 Cited Publications
Synonyms: VPA; 2-Propylpentanoic acid; Dipropylacetic acid
70
70 Cited Publications
Synonyms: Sodium Valproate; VPA sodium; 2-Propylpentanoic acid sodium
45
Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
20
20 Cited Publications
Research Areas:
CC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer .
16
16 Cited Publications
Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects .
16
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Indisulam (E 7070) is a carbonic anhydrase inhibitor and RBM39 molecular glue degrader, with Ki values of 31, 15, and 24 nM against human carbonic anhydrase I, II, and IX, respectively, and a Ki value of 65 nM against bovine carbonic anhydrase IV. Indisulam promotes the recruitment of RBM39 to the CUL4-DCAF15 E3 ubiquitin ligase complex, triggering polyubiquitination and proteasomal degradation of RBM39. Indisulam induces aberrant pre-mRNA splicing, G1 cell cycle arrest, and cell death in cancer cells. As an anticancer agent, Indisulam drives tumor regression and growth inhibition in xenograft models. Indisulam can be used in research related to solid tumors, hematologic and lymphoid malignancies, colorectal cancer, and non-small cell lung cancer .
12
12 Cited Publications
Synonyms: GX15-070 Mesylate
Target:
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity .
12
Target:
Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity .
11
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Research Areas:
FKBP12 PROTAC dTAG-13 (dTAG-13) is a FKBP12 F36V PROTAC degrader and a PXR partial agonist. FKBP12 PROTAC dTAG-13 induces ubiquitination and proteasomal degradation of proteins tagged with FKBP12 F36V, without degrading wild-type FKBP12 or un-fused PXR. It weakly promotes the recruitment of SRC-1, strongly inhibits the interaction between NCoR and PXR, and upregulates the expression of CYP3A4 and other drug metabolism-related genes. FKBP12 PROTAC dTAG-13 is applicable to research related to breast cancer and leukemia [1] .
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10 Cited Publications
THAL-SNS-032 is a selective CDK9 PROTAC degrader. THAL-SNS-032 recruits CRBN to form a ternary complex with CDK9, thereby triggering ubiquitination and proteasomal degradation of CDK9. THAL-SNS-032 also induces the degradation of CDK1, CDK2 and CDK7. THAL-SNS-032 elevates pH2AX levels, reduces MCL1s expression, and activates caspase-3. THAL-SNS-032 induces cancer cell apoptosis, regulates transcription, and inhibits the replication of human cytomegalovirus (CMV) and SARS-CoV-2. THAL-SNS-032 can be used in research related to breast cancer, leukemia, cytomegalovirus infection and SARS-CoV-2 infection .
10
10 Cited Publications
Research Areas:
AGX51 is a pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist that disrupts ID-E protein interactions, thereby triggering ubiquitin-mediated proteasomal degradation of ID1, ID2, ID3 and ID4. AGX51 induces ROS production, G0/G1 cell cycle arrest, non-apoptotic cell death, and regulates EMT-related proteins. AGX51 reduces the proliferation, migration and myofibroblast differentiation of lung fibroblasts, alleviates pulmonary fibrosis, inhibits cancer cell viability and tumor growth, impairs neovascularization, and shows no obvious toxicity in mice. AGX51 can be used in research related to idiopathic pulmonary fibrosis, triple-negative breast cancer, breast cancer, pancreatic ductal adenocarcinoma, colorectal tumors, wet age-related macular degeneration and retinopathy of prematurity .
7
7 Cited Publications
Cat. No.: HY-19979
CAS No.: 339163-65-4
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Research Areas:
RCM-1 is a forkhead box M1 (FOXM1) inhibitor with an EC50 of 0.72 μM in U2OS cells. RCM-1 blocks the nuclear localization and increased the proteasomal degradation of FOXM1. RCM-1 can be used for asthma and other chronic airway diseases research .
7
Research Areas:
Eragidomide (CC-90009) is a GSPT1 Molecular Glue degrader. Eragidomide exhibits antiproliferative and pro-apoptotic (apoptosis) activities against acute myeloid leukemia cells. Eragidomide recruits the CRL4CRBN E3 ubiquitin ligase complex to selectively target GSPT1 for ubiquitination and proteasomal degradation. Eragidomide reduces leukemia cell engraftment and eliminates leukemia stem cells. Eragidomide promotes the activation of the GCN1/GCN2/ATF4 pathway and the integrated stress response pathway, inhibits global protein translation, promotes preferential translation of ATF4, and induces the accumulation of ATF4, CHOP and ATF3. The response to Eragidomide is regulated by the ILF2/ILF3 heterodimer complex, the mTOR signaling pathway and the integrated stress response. Eragidomide can be used in research related to acute myeloid leukemia and relapsed/refractory acute myeloid leukemia .
5
5 Cited Publications
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UNC6852 is a PRC2 PROTAC degrader, with a DC50 value of 0.79 μM for EED (HeLa), 0.3 μM for EZH2 (HeLa), and 0.59 μM for SUZ12 (DLBCL). UNC6852 binds to the WD40 aromatic cage of EED and CRL2-VHL, inducing proteasomal degradation of EED, EZH2 and SUZ12. UNC6852 reduces the level of H3K27me3 and exerts antiproliferative effects in cancer cells. UNC6852 can be used in studies related to diffuse large B-cell lymphoma, triple-negative breast cancer and prostate cancer .
4
Category:
Antifungal Marine natural products Anti-parasitic Disease Research Infection Microorganisms Macrolide Antibiotics Antibiotics Phenols Polyphenols Disease Research Fields Marine microorganism
Target:
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 .
2
2 Cited Publications
JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19 .
2
2 Cited Publications
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JQAD1 is a EP300 PROTAC degrader. JQAD1 selectively targets EP300 and induces its degradation via the CRBN-dependent proteasomal pathway. JQAD1 reduces the levels of H3K27ac and the expression of MYCN. JQAD1 induces apoptosis (apoptosis) and inhibits cancer cell growth. JQAD1 exerts anti-neuroblastoma effects in vivo in a CRBN-dependent manner. JQAD1 can be used for the research of neuroblastoma .
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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
