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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
1184 Results for "
Targeted Degradation
" in MedChemExpress (MCE) Product Catalog:
Products (1184)
1184 Results for "Targeted Degradation" in MCE Product Catalog:
Cat. No.: HY-161804
Target:
Research Areas:
GNF-2-deg is a PROTAC degrader targeting the dengue virus envelope protein (DENV E protein), with a DC50 of 0.83 μM in Huh7.5 cells. GNF-2-deg induces CRBN- and proteasome-dependent proteolysis of intracellular E protein. GNF-2-deg inhibits E protein-mediated membrane fusion and blocks viral particle production. GNF-2-deg reduces viral yield in infected cells and retains activity against E protein βOG pocket mutant virus-like particles (VLP). GNF-2-deg can be used in the research of dengue virus infection, Zika virus infection, Japanese encephalitis, West Nile virus infection and yellow fever .
Cat. No.: HY-181655
CAS No.: 3127060-85-6
Target:
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Anti-hepatic fibrosis agent 3 is an orally active anti-hepatic fibrosis compound targeting Cathepsin D. Anti-hepatic fibrosis agent 3 shows an IC50 of 53.18 μM against COL1A1-promoter and a Kd of 8.86 μM for binding to Cathepsin D. Anti-hepatic fibrosis agent 3 directly binds to and promotes the degradation of Cathepsin D, with no significant effect on Cathepsin B or Cathepsin L. Anti-hepatic fibrosis agent 3 inhibits hepatic stellate cell activation and reduces extracellular matrix deposition and inflammatory cytokine expression. Anti-hepatic fibrosis agent 3 exhibits remarkable anti-fibrotic activity in rat BDL and mouse CDAHFD-induced hepatic fibrosis models. Anti-hepatic fibrosis agent 3 can be used for the study of hepatic fibrosis .
Cat. No.: HY-N0696R
CAS No.: 61825-98-7
Synonyms: Imperialine (Standard)
Cat. No.: HY-N20711
CAS No.: 1428417-60-0
Cat. No.: HY-P5377
CAS No.: 221055-89-6
Synonyms: Cathepsin K substrate
Target:
Research Areas:
Cat. No.: HY-P991381
Synonyms: PPMX-T003; TSP-A18
Research Areas:
Cat. No.: HY-W100287
CAS No.: 4532-33-6
Cat. No.: HY-184501
CAS No.: 486440-74-8
UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2. UE01 activates hULK1 with an EC50 of 695.30 nM and a KD of 114.3 nM for ULK1; it inhibits hERK1 with an IC50 of 179.90 nM and a KD of 114 nM for ERK1; it shows weak binding to ERK2 with a KD of 2.8 mM. UE01 induces the conformational transition of ULK1 from an inactive to an active state, enhances the phosphorylation of ULK1 Ser317 and mAtg13 Ser355, and reduces the phosphorylation of ULK1 Ser757. UE01 competitively occupies the ATP-binding pocket of ERK1, inhibits ERK1 kinase activity, and reduces the activity of the ERK1/2 signaling pathway. UE01 induces complete autophagy flux and apoptosis, upregulates Atg5, Atg7, LC3-II/LC3-I, Bax, cytochrome C (Cyt c), Cleaved-Caspase 3, Cleaved-PARP1 and E-cadherin, downregulates p62, Bcl-2, MMP-2 and MMP-9, reduces the phosphorylation of Exo70 Ser250, and promotes the proteasome-dependent degradation of Cav-1, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation. UE01 can be used in studies related to triple-negative breast cancer .
Target:
Cat. No.: HY-163944
CAS No.: 3081311-94-3
Research Areas:
LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer .
Cat. No.: HY-168996
CAS No.: 3032908-44-1
LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer .
Cat. No.: HY-187388
Research Areas:
HDAC6/ERα ligand-1 is a dual-target ligand with inhibitory activity against both estrogen receptor α (ERα) and histone deacetylase 6 (HDAC6). HDAC6/ERα ligand-1 can be used to synthesize PROTACs, such as PROTAC HDAC6/ERα degrader 1 (HY-187387). HDAC6/ERα ligand-1 binds to the ligand-binding pocket of ERα and forms hydrogen bonds with specific residues in helices 10, 11 and 12. HDAC6/ERα ligand-1 binds stably to HDAC6 and forms hydrogen bonds with specific residues of this protein. HDAC6/ERα ligand-1 can be used in breast cancer research .
Cat. No.: HY-P990690
CAS No.: 2407760-40-9
Synonyms: MEDI-5752
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Cat. No.: HY-W100287R
CAS No.: 4532-33-6
Cat. No.: HY-139997
CAS No.: 2140806-84-2
DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer .
Research Areas:
5'-ODMT cEt N-Bz A Phosphoramidite (Amidite) is a nucleoside phosphoramidite monomer used to synthesize locked nucleic acid (LNA) analog oligonucleotides. It can be used as a building block of antisense oligonucleotides (ASOs) to target complementary RNA sequences. 5'-ODMT cEt N-Bz A Phosphoramidite (Amidite) locks the furanose ring into an N-type conformation through 2',4'-constrained ethyl (cEt) modification, enhancing hybridization affinity and mismatch discrimination with RNA, while significantly improving the resistance of oligonucleotides to exonuclease digestion. 5'-ODMT cEt N-Bz A Phosphoramidite (Amidite) mediates RNase H-dependent mRNA degradation or inhibits translation by forming a stable hybrid with RNA, thereby achieving gene expression regulation. 5'-ODMT cEt N-Bz A Phosphoramidite (Amidite) is mainly used in the development of antisense drugs, gene function research and oligonucleotide synthesis related to disease treatment .
Cat. No.: HY-182044
MRTX849-amide-C4-(o)-carborane is a KRAS G12C inhibitor with mutation selectivity for cells expressing KRAS G12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRAS G12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRAS G12C-positive cancers .
Cat. No.: HY-P10159
CAS No.: 1809102-71-3
Target:
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DJK-5 is an antimicrobial peptide that targets and degrades guanosine pentaphosphate and tetraphosphate (pppGpp and ppGpp). DJK-5 kills bacteria within dentinal tubules, dental plaque and preformed oral biofilms, delays biofilm recovery, reduces the abundance of extracellular polysaccharides and the structural integrity of biofilm matrices, and inhibits the formation and biomass accumulation of dental plaque biofilms. DJK-5 permeabilizes bacterial membranes, induces bacterial morphological changes, inhibits bacterial growth, and exerts a synergistic effect on bacterial biofilms when used in combination with traditional antibiotics and Colistin (HY-113678). DJK-5 exhibits protease resistance and broad-spectrum antibiofilm activity, though its activity decreases in fetal bovine serum. DJK-5 can be used in studies of pulpitis, mixed biofilm infections, skin abscesses, dental caries, infections associated with failed root canal therapy, and Pseudomonas aeruginosa biofilm-related respiratory tract infections .
Cat. No.: HY-W250120
CAS No.: 37220-17-0
Cat. No.: HY-L050
507 compounds
Protein ubiquitination is an enzymatic post-translational modification in which an ubiquitin protein is attached to a substrate protein. Ubiquitination involves three main steps: activation, conjugation, and ligation, performed by ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s), and ubiquitin ligases (E3s), respectively. Ubiquitination affects cellular processes such as apoptosis, cell cycle, DNA damage repair, and membrane transportation, etc. by regulating the degradation of proteins (via the proteasome and lysosome), altering the cellular localization of proteins, affecting proteins activity, and promoting or preventing protein-protein interactions. Deregulation of ubiquitin pathway leads to many diseases such as neurodegeneration, cancer, infection and immunity, etc.
MCE offers a unique collection of 507 small molecule modulators with biological activity used for ubiquitination research. Compounds in this library target the key enzymes in ubiquitin pathway. MCE Ubiquitination Compound Library is a useful tool for the research of ubiquitination regulation and the corresponding diseases.
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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
