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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
76 Results for "
proteasomal pathway
" in MedChemExpress (MCE) Product Catalog:
Products (76)
76 Results for "proteasomal pathway" in MCE Product Catalog:
Cat. No.: HY-189001
PROTEC NAMPT Degrader-1 is a NAMPT PROTEC degrader. PROTEC NAMPT Degrader-1 binds to NAMPT via non-covalent interactions and degrades this protein through a proximity-induced radical oxidation mechanism mediated by cyclopropane radical clock, independent of proteasomal or lysosomal pathways. PROTEC NAMPT Degrader-1 exhibits anticancer activity against ovarian cancer. It can be used in relevant studies on ovarian cancer (Pink: NAMPT ligand: (HY-188123); Linker: (HY-188124)) .
Cat. No.: HY-182087
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ALK degrader 3 is a ALK HyT degrader with an IC50 of 1.2 nM. ALK degrader 3 inhibits ALK kinase activity, increases the solvent-accessible surface area of hydrophobic residues near the ALK binding pocket, promotes ALK to form a partially unfolded conformation, and drives ALK degradation via the proteasomal pathway. ALK degrader 3 inhibits the proliferation of tumor cells. ALK degrader 3 can be used for the research of non-small cell lung cancer. (ALK ligand: Brigatinib (HY-12857); hydrophobic tag: Tetraasterane (HY-W1139353)) .
Cat. No.: HY-184321
LC-MG-5 is a selective molecular glue degrader targeting FGFR2, with a DC50 of 231.7 nM in KATO III cells. LC-MG-5 induces proteasomal degradation of FGFR2 in a DCAF16-dependent manner via a covalent molecular glue mechanism. LC-MG-5 inhibits cancer cell proliferation. LC-MG-5 suppresses PI3K/AKT and MAPK/ERK signaling pathways mediated by FGFR2. LC-MG-5 can be used in the research of gastric cancer .
Cat. No.: HY-184322
LC-MG-10 is a selective molecular glue degrader targeting FGFR2, with a DC50 of 230.2 nM in KATO III cells. LC-MG-10 induces proteasomal degradation of FGFR2 via a covalent molecular glue mechanism. LC-MG-10 inhibits cancer cell proliferation. LC-MG-10 suppresses FGFR2-mediated PI3K/AKT and MAPK/ERK signaling pathways. LC-MG-10 can be used in studies related to gastric cancer .
Cat. No.: HY-N19738
CAS No.: 21105-15-7
Cat. No.: HY-P11828
Cat. No.: HY-184179
CAS No.: 3103984-17-1
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TEAD degrader-1 is a potent FBXO22-mediated molecular glue degrader of TEAD, with a 24 h DC50 of 1.0 nM. TEAD degrader-1 binds reversibly and covalently to FBXO22 C326, assembles a functional ternary complex, and mediates proteasomal degradation of TEAD. TEAD degrader-1 exhibits high selectivity for the Hippo pathway and specifically downregulates only TEAD and its downstream target proteins. TEAD degrader-1 is applicable to research related to malignant pleural mesothelioma and non-small cell lung cancer .
Cat. No.: HY-189201
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PinA1 is a selective Molecular glue degrader of CK1α with an EC50 of 2.09 µM. PinA1 induces the formation of a stable CRBN-PinA1-CK1α ternary complex to promote the polyubiquitination and subsequent proteasomal degradation of CK1α. PinA1 activates the p53 signaling pathway. PinA1 induces G1 cell cycle arrest. PinA1 induces p53-dependent Apoptosis. PinA1 can be used in studies related to acute myeloid leukemia .
Cat. No.: HY-189468
CAS No.: 3128784-74-4
PROTAC SHP2 degrader-1 is a potent SHP2 PROTAC degrader with a DC50 of 7.406 μM. PROTAC SHP2 degrader-1 recruits DCAF16 E3 ligase to induce ubiquitination and proteasomal degradation of SHP2, thereby inhibiting the RAS/MAPK and PI3K/AKT/mTOR signaling pathways while simultaneously inducing IFN-γ/JAK/STAT1, apoptosis, and cell cycle arrest. PROTAC SHP2 degrader-1 can be used for cancer research .
Cat. No.: HY-182008
CAS No.: 3068938-30-4
Target:
Molecular Glues E1/E2/E3 Enzyme Apoptosis Notch PARP Caspase Bcl-2 Family Ligands for E3 Ligase
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NEURL1B-IN-1 is a molecular glue-like NEURL1B degrader with a Kd value of 46.2 nM. NEURL1B-IN-1 binds to Arg422 within the NHR2 domain of NEURL1B, triggers its autoubiquitination and proteasomal degradation, disrupts its interaction with DLL1, and attenuates the Notch signaling pathway. NEURL1B-IN-1 induces cell cycle arrest and apoptosis, and inhibits migration of hepatocellular carcinoma cells. NEURL1B-IN-1 is applicable to research related to hepatocellular carcinoma .
Cat. No.: HY-184470
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MyD88 degrader-1 is an orally active molecular glue degrader targeting MyD88, with a DC50 of 0.74 μM, and exhibits potent anti-inflammatory activity. MyD88 degrader-1 promotes ubiquitination and proteasomal degradation of MyD88, blocks the activation of the NF-κB signaling pathway, and downregulates the transcription of pro-inflammatory genes such as IL-6 and IL-1β. MyD88 degrader-1 alleviates symptoms in acute lung injury models. MyD88 degrader-1 can be used in studies related to acute lung injury .
Cat. No.: HY-183604
CAS No.: 3129176-25-3
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T-10531 is a selective USP25/USP28 inhibitor. T-10531 exhibits an IC50 of 0.03 μM and a Kd of 0.2 μM against human USP25, as well as an IC50 of 0.12 μM and a Kd of 0.06 μM against human USP28. T-10531 inhibits USP25/USP28 activity and induces the degradation of USP25 via the proteasomal pathway, without inhibiting other deubiquitinases. T-10531 can be used in the research of squamous cell carcinoma, colorectal cancer, gastric cancer, triple-negative breast cancer and pancreatic cancer .
Cat. No.: HY-187387
CAS No.: 3092711-76-4
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PROTAC HDAC6/ERα degrader 1 is a dual-target PROTAC that targets HDAC6/ERα, with DC50 values of 1.21 μM (HDAC6), 0.28 μM (ERα) in MCF-7 cells and 0.67 μM (HDAC6), 0.14 μM (ERα) in LCC2 cells, respectively. PROTAC HDAC6/ERα degrader 1 selectively degrades ERα and HDAC6 via the proteasomal pathway, inhibits the transcriptional activation of ERα and blocks the estrogen signaling pathway. PROTAC HDAC6/ERα degrader 1 inhibits the function of HDAC6, attenuates hormone responses, and disrupts autophagy-lysosome function. PROTAC HDAC6/ERα degrader 1 induces cell cycle arrest, apoptosis and ferroptosis, and exhibits antiproliferative activity in breast cancer cells. PROTAC HDAC6/ERα degrader 1 can be used for breast cancer research .
Cat. No.: HY-10358R
CAS No.: 1032350-13-2
Synonyms: MK-2206 (2HCl) (Standard)
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MK-2206 dihydrochloride (MK-2206 2HCl) (Standard) is the analytical standard of MK-2206 dihydrochloride (HY-10358). This product is intended for research and analytical applications. MK-2206 dihydrochloride 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 .
Cat. No.: HY-189146
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HDTAC EGFR Degrader-1 is an EGFR HDTAC (hypoxia-activated targeted protein degradation chimera) degrader with a DC50 of 1.76 μM. HDTAC EGFR Degrader-1 consists of a linker, a tumor hypoxia-activated group (HAG, a group that generates ROS under tumor hypoxic conditions), and an EGFR ligand. HDTAC EGFR Degrader-1 drives EGFR degradation through the proteasomal pathway. HDTAC EGFR Degrader-1 downregulates Caspase-3 under hypoxic conditions. HDTAC EGFR Degrader-1 can be used in research on non-small cell lung cancer harboring EGFR mutations (EGFR ligand: FAAH-IN-2 (HY-79511); HAG: Thalidomide-O-COOH (HY-103597); linker: NH2-PEG3 (HY-W007545)) .
Cat. No.: HY-184337
CAS No.: 143111-84-6
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Dihydroparadol is a iNOS inhibitor with an IC50 of 7.24 μM, and it is found in ginger. Dihydroparadol partially inhibits the catalytic activity of iNOS, blocks the nuclear translocation of NF-κB p65, reduces NF-κB activity, and attenuates lipopolysaccharide-induced degradation of IκB-α, thereby inhibiting NF-κB-mediated iNOS gene expression and protein production. Dihydroparadol inhibits lipopolysaccharide-induced nitric oxide production in macrophages and exhibits anti-inflammatory activity. Dihydroparadol increases ABCA1 protein abundance by elevating mRNA levels and reducing proteasomal degradation, and also increases ABCG1 protein abundance by enhancing protein stability. Dihydroparadol promotes cholesterol efflux from cholesterol-loaded macrophages via apolipoprotein A1-mediated and plasma-mediated pathways. Dihydroparadol inhibits PDGF-induced vascular smooth muscle cell proliferation, shows no cytotoxicity to vascular smooth muscle cells within the tested concentration range, and does not interfere with endothelial cell proliferation. Dihydroparadol can be used in the research of inflammatory diseases, atherosclerosis and cardiovascular 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
