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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-182098A
DSPE-PEG2000-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-PEG2000-GALA can be used for drug delivery .
Cat. No.: HY-182098B
DSPE-PEG3400-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-PEG3400-GALA can be used for drug delivery .
Cat. No.: HY-182098C
DSPE-PEG5000-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-PEG5000-GALA can be used for drug delivery .
Cat. No.: HY-P11614
Cat. No.: HY-183073
Research Areas:
TZ1104 is a PROTAC-based CDK7 degrader, with a DC50 of 0.88 nM. TZ1104 forms a ternary complex with VHL E3 ligase and CDK7 to trigger proteasome-dependent CDK7 degradation, destabilizing the CDK7-cyclin H-MAT1 complex. TZ1104 suppresses phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. TZ1104 activates the p53-p21 axis and suppresses oncogenic Myc signaling. TZ1104 induces cell cycle arrest, apoptosis, and differentiation of acute leukemia cells. TZ1104 can be used for the research of acute leukemia .
Cat. No.: HY-N13009
CAS No.: 2744300-63-6
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Cat. No.: HY-P4119
CAS No.: 863608-35-9
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Cat. No.: HY-17663
CAS No.: 2992741-10-1
KMR-206 is a PARP7 inhibitor with an IC50 of 13.7 nM. KMR-206 relieves AHR-mediated transcriptional repression and enhances CYP1A1 expression in the presence of TCDD. KMR-206 induces the STING-dependent IFN-β signaling pathway and increases the levels of STAT1, pSTAT1 and nuclear PARP7 in cancer cells. KMR-206 reduces the viability of lung adenocarcinoma cells, enhances radiation-induced immunogenic signals, and induces the production of immunogenic signals in glioblastoma cancer stem cells. KMR-206 destabilizes FRA1 to increase IRF1 levels and promotes the IRF3-CBP/p300 interaction. KMR-206 can be used in studies related to lung adenocarcinoma and glioblastoma .
Cat. No.: HY-179558
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MS1-96 is an orally active PD-L1 (programmed death-ligand 1) molecular glue degrader. MS1-96 effectively reduced PD-L1 protein levels across multiple colorectal cancer (CRC) cell lines. MS1-96 directly binds to PD-L1 (KD = 2.58 μM) and enhances the interaction between HIP1R and PD-L1, thereby altering the intracellular trafficking of PD-L1 within clathrin-coated vesicles. MS1-96 induces abnormal N-glycosylation of PD-L1, destabilizing the protein and hastening its lysosome-mediated degradation. MS1-96 can be used for the study of colorectal cancer .
Cat. No.: HY-180576
CAS No.: 2231746-53-3
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Nurr1/RXR dual agonist 1 is a dual activator of Nurr1 (EC50 = 2.6 µM) and RXR with K s of 0.6 and 1.1 µM, respectively. Nurr1/RXR dual agonist 1 exclusively activates the heterodimer response element DR5 by selectively destabilizing the Nurr1 homodimer and stabilizing the Nurr1:RXR heterodimer. Nurr1/RXR dual agonist 1 enhances expression of a specific subset of neuroprotective Nurr1 target genes while avoiding induction of genes associated with potential off-target effects in neuronal cells. Nurr1/RXR dual agonist 1 can be used for neurodegenerative diseases research .
Cat. No.: HY-P5423
CAS No.: 107658-43-5
Cat. No.: HY-W001974
CAS No.: 6960-42-5
Cat. No.: HY-186321
CAS No.: 501124-40-9
Synonyms: KF25706
Radicicol 6-oxime (KF25706) is an Hsp90 inhibitor with an EC50 of 5.5 nM against human Hsp90. Radicicol 6-oxime binds to Hsp90 and disrupts its chaperone function, leading to destabilization and depletion of Hsp90-associated signaling molecules. Radicicol 6-oxime depletes Hsp90-associated signaling proteins such as Raf-1, v-src, p185erbB2, Cdk4, and mutant p53, thereby inhibiting K-ras and v-src signaling pathways. Radicicol 6-oxime exhibits antiproliferative activity against various tumor cells. Radicicol 6-oxime inhibits tumor growth in mouse tumor xenograft models. Radicicol 6-oxime can be used for research on breast cancer, colon cancer, and vulvar epidermoid carcinoma .
Cat. No.: HY-112005G
CAS No.: 4004-05-1
Synonyms: Dioleoylphosphatidylethanolamine (GMP); 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine (GMP)
Cat. No.: HY-138794A
CAS No.: 2417089-73-5
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(Rac)-XL177A is the racemic isomer of XL177A (HY-138794). XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections .
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].
Cat. No.: HY-138794G
CAS No.: 2417089-74-6
Cat. No.: HY-P11353
CAS No.: 117138-19-9
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U7D-1 is a USP7 PROTAC degrader that induces selective proteasomal degradation of USP7. U7D-1 destabilizes and downregulates the expression of variant PRC1 complex subunits PCGF1, RING1A and PCGF6, and also slightly reduces the protein level of KDM2B. U7D-1 decreases cell viability, arrests neuroblastoma cells at the G0/G1 cell cycle phase, and downregulates the expression of target genes of PAX3::FOXO1 in FP-RMS cells. U7D-1 increases the level of cleaved PARP in FP-RMS cells, induces cell apoptosis, and upregulates the expression of muscle differentiation markers MYH1 and MYF5. U7D-1 inhibits the growth and proliferation of p53 wild-type and mutant cancer cells, and regulates the apoptosis pathway and E2F pathway. U7D-1 is applicable to studies on neuroblastoma, fusion-positive rhabdomyosarcoma, p53-mutant cancers and cancer-related research .
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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
