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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
7 Results for "
dimerization interface
" in MedChemExpress (MCE) Product Catalog:
Products (7)
7 Results for "dimerization interface" in MCE Product Catalog:
Cat. No.: HY-146812
CAS No.: 2675490-72-7
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DIZ-3 is a selective multimeric G4 ligand based on a G4-ligand-dimerizing strategy. DIZ-3 intercalates into the G4-G4 interface, stabilizing the higher-order structure. DIZ-3 induces cell cycle arrest and apoptosis, and thus inhibits cell proliferation in alternative lengthening of telomere (ALT) cancer cells .
Cat. No.: HY-175435
CAS No.: 3094183-98-6
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CST905 is a potent BRAF-V600E PROTAC degrader with a DC50 of 18 nM. CST905 recruits the VHL E3 ligase to form a ternary complex, mediating the degradation of BRAF-V600E via the ubiquitin-proteasome pathway. The ligand of CST905 disrupts the RAF dimerization interface, thereby preventing the aberrant activation of the harmful MAPK/ERK pathway in RAS-mutated cells while degrading the target protein. CST905 can be used in studies related to malignant melanoma and neuroblastoma .
Cat. No.: HY-131570
CAS No.: 1997359-63-3
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JZ-4109 is a β-Glucocerebrosidase (GCase) modulator with an IC50 of 8 nM for wild-type recombinant GCase. JZ-4109 binds to an allosteric site at the GCase dimer interface, stabilizes wild-type and GCase N370S mutant GCase, induces GCase dimerization. JZ-4109 increases GCase protein abundance. JZ-4109 can be used for the research of Parkinson's diseas .
Cat. No.: HY-181062
VWK147 is a second-generation HSP90 C-terminal domain (CTD) inhibitor. VWK147 targets the CTD dimerization interface, prevents HSP90 CTD dimerization, disrupts co-chaperone PPID binding to HSP90 CTD, and inhibits HSP90 chaperone function dependent on dimerization. VWK147 reduces protein levels of HSP90 client proteins ULK1, RIPK1, and CDK4 without inducing a heat shock response. VWK147 induces cell death, including apoptosis, in Cisplatin (HY-17394)-sensitive and -resistant urothelial carcinoma cells. VWK147 induces LC3-II accumulation, inhibits autophagosome-lysosome fusion to block canonical autophagy, and induces non-canonical LC3 lipidation independent of ULK1 and PIK3C3 complexes. VWK147 can be used for the research of urothelial carcinoma .
Cat. No.: HY-183988
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OICR409946 is a self-dimerization-induced proximity-targeting chimera (SDIPTAC) targeting DCAF1, with a Kd value of 6200 nM. OICR409946 binds to DCAF1, induces head-to-tail homodimerization, sterically blocks the Vpr binding interface, prevents the recruitment of Vpr to the CRL4DCAF1 complex, and inhibits Vpr-dependent HIV replication. OICR409946 can be used in studies related to HIV infection (DCAF1 ligand: (HY-169390); Linker: (HY-130659)) .
Cat. No.: HY-187584
CAS No.: 1044664-73-4
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LQZ-7 is a survivin inhibitor and molecular glue degrader (Kd=0.24 μM). LQZ-7 binds to the dimerization interface of survivin, disrupting homodimerization and dissociating dimeric survivin into monomers, thereby accelerating its proteasome-dependent degradation. LQZ-7 does not affect the structurally similar dimeric proteins 14-3-3σ and 14-3-3δ, and can induce apoptosis, exhibiting cytotoxicity against cancer cells .
Cat. No.: HY-183583
CAS No.: 2709068-47-1
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HIF-2α-IN-18 is a selective HIF-2α inhibitor with a human IC50 of 8.1 nM. HIF-2α-IN-18 binds to the HIF-2α PAS-B domain, induces conformational perturbations at the HIF-2α/ARNT dimerization interface, destabilizes the HIF-2α/ARNT heterodimer, and blocks HIF-2α-mediated transcriptional activity. HIF-2α-IN-18 inhibits hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1, without inhibiting HIF-1α target genes PGK1 and PDK1. HIF-2α-IN-18 can be used for the research of clear cell renal cell carcinoma, hepatocellular carcinoma[1].
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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
