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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
119 Results for "
destabilizing
" in MedChemExpress (MCE) Product Catalog:
Products (119)
119 Results for "destabilizing" in MCE Product Catalog:
Cat. No.: HY-160126
CAS No.: 2154373-60-9
27-Norcholestenoic acid is an inverse agonist of LXRβ and LXRα that decreases basal luciferase activity and inhibits agonist-induced transactivation. 27-Norcholestenoic acid induces conformational changes in the AF-2 domain that favor corepressor over coactivator recruitment, thereby destabilizing the active receptor conformation. 27-Norcholestenoic acid downregulates FASN and SREBP-1a/c gene expression .
Cat. No.: HY-183115
CAS No.: 3127009-52-0
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TNG961 is a selective and orally active CRBN-mediated HBS1L molecular glue degrader. TNG961 induces formation of an HBS1L-TNG961-CRBN ternary complex, leading to potent degradation of HBS1L and secondary destabilization of its binding partner PELO. TNG961 can reduce HBS1L protein levels, thereby disrupting the PELO region involved in ribosome rescue. TNG961 can be used for the study of FOCAD-deficient cancers, such as pancreatic cancer .
Cat. No.: HY-101931R
CAS No.: 1637443-98-1
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hVEGF-IN-1 (Standard) is the analytical standard of hVEGF-IN-1 (HY-101931). This product is intended for research and analytical applications. hVEGF-IN-1, a quinazoline derivative, could specifically bind to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilize the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression .
Cat. No.: HY-103257R
CAS No.: 154554-41-3
Synonyms: NSC656158 (Standard)
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CHM-1 (Standard) is the analytical standard of CHM-1 (HY-103257). This product is intended for research and analytical applications. CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity .
Cat. No.: HY-179577
CAS No.: 3101950-55-1
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PIN1 degrader-3 is a Pin1 (peptidyl-prolyl isomerase protein) (IC50=4.65 nM) molecular glue degrader. PIN1 degrader-3 bound covalently to Pin1. PIN1 degrader-3-induced Pin1 degradation reduced cell viability. PIN1 degrader-3 can destabilize Pin1 in vitro, causing its degradation in cells. PIN1 degrader-3 can be used for the study of pancreatic cancer .
Cat. No.: HY-187211
TYK2 activator-2 (Compound 6g) is a selective TYK2 activator and JAK3 inhibitor, with an EC50 of 0.21 μM against TYK2 and an IC50 of 1.2 μM against JAK3. TYK2 activator-2 destabilizes the JH2-JH1 autoinhibitory complex of TYK2, enhances the catalytic activity of TYK2, and inhibits the JH1 kinase domain activity of JAK3. TYK2 activator-2 can be used in cancer-related research .
Cat. No.: HY-182399
CAS No.: 2421117-94-2
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BC-DXI-495 is a AIMP2-DX2 inhibitor. BC-DXI-495 disrupts the interaction of HSP70 and destabilizes DX2. BC-DXI-495 induces DX2 degradation via Siah1-mediated ubiquitination. BC-DXI-495 exerts tumor suppressive activity in cancer cells. BC-DXI-495 serves as a chemical probe to elucidate the mechanism of action of arylsulfonamide-based DX2 inhibitors. BC-DXI-495 can be used in lung cancer research .
Cat. No.: HY-181963
ZINC-1000507824 is a non-covalent reversible RNA cytosine-5 methyltransferase NSUN2 inhibitor. ZINC-1000507824 targets the SAM cofactor binding pocket of NSUN2 and forms stable NSUN2-ligand complexes. ZINC-1000507824 destabilizes oncogenic mRNAs encoding PI3K/AKT and MAPK/ERK pathway components, attenuates growth signals, reduces proliferative drive, and restores therapy sensitivity in cancer cells. ZINC-1000507824 can be used for the research of NSUN2-driven malignancies .
Cat. No.: HY-182242
AGB-374 is an orally active NDUFS7 inhibitor. AGB-374 destabilizes NDUFS7 protein and inhibits oxidative phosphorylation by targeting mitochondrial complex I. AGB-374 reduces MYC protein levels in colon cancer cells in vivo and delays tumor growth in syngeneic mouse models of colon cancer. AGB-374 synergistically enhances the cytotoxicity of copper chelators against cancer cells. AGB-374 cooperates with copper chelators to downregulate MYC and NDUFS7 protein levels in cancer cells. AGB-374 can be used for the research of colon cancer .
Cat. No.: HY-183115A
CAS No.: 3127008-95-8
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(Rac)-TNG961 is the rac isomer of TNG961 (HY-183115). TNG961 is a selective and orally active CRBN-mediated HBS1L molecular glue degrader. TNG961 induces formation of an HBS1L-TNG961-CRBN ternary complex, leading to potent degradation of HBS1L and secondary destabilization of its binding partner PELO. TNG961 can reduce HBS1L protein levels, thereby disrupting the PELO region involved in ribosome rescue. TNG961 can be used for the study of FOCAD-deficient cancers, such as pancreatic cancer .
Cat. No.: HY-185699A
Antibacterial agent 350 TFA is a membrane stabilizer/disruptor with antibacterial activity. Antibacterial agent 350 TFA reduces glucose-induced efflux efficiency and slightly impairs outer membrane stability. Antibacterial agent 350 TFA significantly decreases the bacteriostatic MIC50 of Ceftazidime (HY-B0593) or Ciprofloxacin (HY-B0356), but increases the MIC50 of Amikacin (HY-B0509A). Antibacterial agent 350 TFA can be used for the research of Pseudomonas aeruginosa infections .
Cat. No.: HY-185699B
Antibacterial agent 350 hydrochloride is a membrane stabilizer/disruptor with antibacterial activity. Antibacterial agent 350 hydrochloride reduces glucose-induced efflux efficiency and slightly impairs outer membrane stability. Antibacterial agent 350 hydrochloride significantly decreases the bacteriostatic MIC50 of Ceftazidime (HY-B0593) or Ciprofloxacin (HY-B0356), but increases the MIC50 of Amikacin (HY-B0509A). Antibacterial agent 350 hydrochloride can be used for the research of Pseudomonas aeruginosa infections .
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Nitrosulfathiazole (Nisulfazole; p-Nitrosulfathiazole) is a sulfonamide antibacterial agent and also a key chemical intermediate for the hematotoxicity of Chloramphenicol (HY-B0239). Nitrosulfathiazole induces DNA helix instability, strand breakage and aplastic anemia. Nitrosulfathiazole can be used in research related to bacterial infections and aplastic anemia .
Cat. No.: HY-185699
CAS No.: 1394833-44-3
Antibacterial agent 350 is a membrane stabilizer/disruptor with antibacterial activity. Antibacterial agent 350 reduces glucose-induced efflux efficiency and slightly impairs outer membrane stability. Antibacterial agent 350 significantly decreases the bacteriostatic MIC50 of Ceftazidime (HY-B0593) or Ciprofloxacin (HY-B0356), but increases the MIC50 of Amikacin (HY-B0509A). Antibacterial agent 350 can be used for the research of Pseudomonas aeruginosa infections .
Cat. No.: HY-100591R
CAS No.: 709002-46-0
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SirReal2 (Standard) is the analytical standard of SirReal2 (HY-100591). This product is intended for research and analytical applications. SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
Cat. No.: HY-184178A
HF-125 is an orally active, highly selective small-molecule inhibitor of Tribbles 2 (TRIB2). HF-125 promotes the destabilization and degradation of TRIB2 protein via the proteasome pathway. HF-125 downregulates neuroendocrine markers, induces cell cycle arrest and apoptosis, inhibits tumor cell colony formation and invasion, and reverses tumor cell resistance to Enzalutamide (HY-70002). HF-125 significantly inhibits tumor growth in SCID mouse xenograft models, and exerts synergistic inhibitory effects when combined with Enzalutamide. HF-125 can be used in research related to prostate cancer .
Cat. No.: HY-179635
CAS No.: 3114128-67-2
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GSTO1-IN-6 is an allosteric and covalent GSTO1 inhibitor with an IC50 of 457 nM. GSTO1-IN-6 markedly reduces Lipopolysaccharides (LPS) (HY-D1056)-induced IL-1β (IC50 of 1.9 μM) and IL-18 (IC50 of 10. μM) secretion in human monocyte-derived macrophages. GSTO1-IN-6 covalently modifies GSTO1-Cys32, inducing conformational changes and protein destabilization. GSTO1-IN-6 can be used for the research of inflammatory diseases .
Cat. No.: HY-181074
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Tubulin polymerization-IN-88 is a tubulin inhibitor that blocks tubulin polymerization, leading to microtubule destabilization and disruption of the mitotic spindle. Tubulin polymerization-IN-88 induces G2/M phase arrest and apoptosis in cancer cells, and inhibits cancer cell migration and self-renewal of cancer stem cells. It exhibits in vitro anti-proliferative activity against cancer cells with selectivity over normal cells. Tubulin polymerization-IN-88 also demonstrates in vivo anti-cancer activity without significant toxicity. Tubulin polymerization-IN-88 is applicable for research on glioblastoma, lung cancer, endometrial cancer, ovarian cancer, and leukemia .
Cat. No.: HY-183763
CAS No.: 3134806-34-8
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RORγt inverse agonist 37 is an orally active RORγt inverse agonist with an IC50 of 10.8 nM against human targets. RORγt inverse agonist 37 destabilizes helix 12 of RORγt in the agonist-bound conformation, thereby inhibiting transcriptional activity. RORγt inverse agonist 37 inhibits the secretion of IL-17 in cells and in LPS-induced systemic inflammation mouse models. RORγt inverse agonist 37 improves disease-related symptoms in mouse models of psoriasiform dermatitis. RORγt inverse agonist 37 can be used in research related to psoriasiform dermatitis and systemic inflammation .
Cat. No.: HY-182098
DSPE-PEG1000-GALA is a PEG compound which composed of DSPE and a lung endothelium-targeting peptide GALA (HY-P5423). GALA is a pH-responsive amphipathic peptide consisting of 30 amino acids, which acts as a lung endothelium-targeting ligand. GALA undergoes a conformational transition from random coil to α-helix in an acidic environment at pH 5.0, thereby inducing endosomal membrane destabilization and fusion. GALA-modified liposomes traverse lung endothelial cells via clathrin-dependent endocytosis and transcytosis, and specifically accumulate in the lungs after intravenous injection. DSPE-PEG1000-GALA can be used for drug delivery .
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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
