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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
291 Results for "
Mediator complex
" in MedChemExpress (MCE) Product Catalog:
Products (291)
291 Results for "Mediator complex" in MCE Product Catalog:
Cat. No.: HY-W998347
CAS No.: 2922884-90-8
Research Areas:
ABS-752 hydrochloride is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation. ABS-752 hydrochloride preferentially degrades GSPT1 and induces cytotoxicity through this degradation, while it also degrades NEK7, SALL4 and CK1α, with weaker degradation potency against CK1α. As a prodrug, ABS-752 hydrochloride requires metabolic activation to ABT-002 to form the active complex; VAP-1 mediates its conversion to an aldehyde intermediate. ABS-752 hydrochloride induces cell death, reduces cell viability, and exhibits antitumor activity, leading to regression and inhibition of tumor growth. ABS-752 hydrochloride shows no cytotoxicity in primary human hepatocytes. ABS-752 hydrochloride can be used in the research of hepatocellular carcinoma .
Cat. No.: HY-P86959
Synonyms: Activator recruited cofactor 240 kDa component antibody; Activator-recruited cofactor 240 kDa component antibody; ARC240 antibody; CAG repeat protein 45 antibody; CAGH45 antibody; HOPA antibody; KIAA0192 antibody; MED12 antibody; MED12_HUMAN antibody; Mediator complex subunit 12 antibody; Activator recruited cofactor 240 kDa component antibody; Activator-recruited cofactor 240 kDa component antibody; ARC240 antibody; CAG repeat protein 45 antibody; CAGH45 antibody; HOPA antibody; KIAA0192 antibody
Cat. No.: HY-174379
NTLiverTac PDE6D degrader-1 is a PDE6D NTLiverTac degrader with a DC50 of 4.09 μM. NTLiverTac PDE6D degrader-1 is formed by conjugating a PDE6D PROTAC degrader with the NTCP ligand Cholic acid (HY-N0324). NTLiverTac PDE6D degrader-1 triggers the ubiquitin-proteasome system-mediated degradation process by forming a complex with PDE6D and MDM2, inducing proteasome-dependent and NTCP-dependent degradation. NTLiverTac PDE6D degrader-1 inhibits PDE6D-dependent KRAS trafficking and suppresses KRAS-related oncogenic signaling cascades. NTLiverTac PDE6D degrader-1 inhibits the activation of the PI3K/AKT/mTOR signaling pathway and induces cellular Apoptosis. NTLiverTac PDE6D degrader-1 enters cancer cells via NTCP-mediated endocytosis. NTLiverTac PDE6D degrader-1 can be used in the research of hepatoblastoma (MDM2 ligand: (4R,5S)-Nutlin carboxylic acid (HY-128836); NTCP ligand: Cholic acid (HY-N0324); PDE6D ligand: Sorafenib (HY-10201)) .
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2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) is a metal chelator precursor containing a DOTA macrocyclic structure. DOTA can form highly stable complexes with metal ions (such as 68Ga, 177Lu) through four nitrogen atoms and four carboxylic acid groups to mediate targeted delivery of radionuclides. The tert-butyl ester group (tBu ester) of 2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) also protects the carboxylic acid group during synthesis, and forms a free carboxyl group after deprotection reaction for coupling with targeting molecules (such as antibodies, peptides). 2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) may be combined with tumor pre-targeting systems through bioorthogonal reactions (such as reverse electron demand Diels-Alder reaction) to study radioactive imaging or therapy of tumor tissues, and is mainly used in tumor pre-targeting research in the field of nuclear medicine .
Cat. No.: HY-153321A
CAS No.: 2649400-33-7
Synonyms: (R,R)-NX-5948; (R,R)-BTK-IN-24
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(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
Cat. No.: HY-178122
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THNAN69 is a PROTAC degrader targeting LIMK2, which efficiently degrades ectopically expressed EGFP-LIMK2 in live HuCCT1 cells with a DC50 of 1 nM. THNAN69 induces isoform-specific ubiquitin-mediated degradation of LIMK2 by recruiting the CRBN E3 ligase, forming a stable ternary complex with LIMK2 and CRBN; this degradation process depends on the activity of cullin-RING ligase. THNAN69 does not reduce phosphorylated cofilin levels, as LIMK1 can compensate for the loss of LIMK2; it also stimulates compensatory activation of the Rho signaling pathway including PAK1/2 and ROCK1/2. THNAN69 serves as a selective chemical probe for dissecting the LIMK2 isoform-dependent biological mechanisms. THNAN69 can be used in the research of cholangiocellular carcinoma and acute lymphoblastic leukemia .
Cat. No.: HY-184915
CAS No.: 3065495-08-8
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APH003 is an orally active IRAK4 PROTAC degrader with a DC50 of 0.74 nM in human peripheral blood mononuclear cells (hPBMCs). APH003 recruits IRAK4 to CRBN to form a ternary complex, mediates the ubiquitination and degradation of IRAK4 via the ubiquitin-proteasome pathway, and inhibits the kinase activity of IRAK4. APH003 inhibits LPS- or IL-1β/LPS-induced phosphorylation of ERK, JNK and NF-κB. APH003 inhibits the secretion of TNF-α, IL-6, IL-8 and IL-13 by stimulated hPBMCs. APH003 exhibits anti-inflammatory activity in rat TNBS-induced intestinal inflammation models and mouse IL-33-induced skin inflammation models. APH003 can be used in research related to inflammatory bowel disease and skin inflammation .
Cat. No.: HY-W010514R
CAS No.: 1460-57-7
Category:
Cat. No.: HY-W015954
CAS No.: 24347-58-8
Cat. No.: HY-W1113135A
CAS No.: 2828447-14-7
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Carboxymethyl-β-cyclodextrin sodium salt, for capillary electrophoresis is a negatively charged β-cyclodextrin derivative, as well as a metal ion chelator and solubilizing reagent. Carboxymethyl-β-cyclodextrin sodium salt, for capillary electrophoresis forms stable aqueous complexes with Ba 2+, Ca 2+, Cd 2+, Ni 2+, Pb 2+, Sr 2+, and Zn 2+ ions. Carboxymethyl-β-cyclodextrin sodium salt derived hydrogel carriers support oral insulin delivery via paracellular permeation across Caco-2 monolayers and produce sustained hypoglycemic effects in diabetic mice. Carboxymethyl-β-cyclodextrin sodium salt can be conjugated onto folate-modified BSA nanoparticles to boost folate receptor-mediated endocytosis, elevate intracellular anticancer drug uptake and trigger cell apoptosis. Carboxymethyl-β-cyclodextrin sodium salt can be utilized for chiral separation in capillary electrophoresis, development of nanoscale drug carriers and nucleic acid transfection research .
Cat. No.: HY-W322225
CAS No.: 59752-57-7
Synonyms: DLPE; 1,2-Dilauroyl-sn-glycero-3-PE
1,2-Dilauroyl-sn-glycero-3-phosphoethanolamine (DLPE; 1,2-Dilauroyl-sn-glycero-3-PE) is an anionic phospholipid. 1,2-Dilauroyl-sn-glycero-3-phosphoethanolamine promotes the endocytosis of liposome-DNA complexes into target cells, and subsequently mediates membrane fusion between liposome carriers and endosomes to deliver DNA into the nucleus. 1,2-Dilauroyl-sn-glycero-3-phosphoethanolamine is a component of anionic artificial viral envelope liposomes, which deliver plasmid DNA to hepatoma cells without serum inhibition. 1,2-Dilauroyl-sn-glycero-3-phosphoethanolamine enables the construction of biocompatible non-viral gene delivery vector systems. 1,2-Dilauroyl-sn-glycero-3-phosphoethanolamine is applicable for liposome synthesis .
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DpC is a selective, orally active iron chelator with anticancer activity. DpC acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer .
Cat. No.: HY-114243A
CAS No.: 1382469-40-0
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Research Areas:
Neurological Disease Inflammation/Immunology Endocrinology Cancer
DpC hydrochloride is a selective, orally active iron chelator with anticancer activity. DpC hydrochloride acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC hydrochloride induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC hydrochloride inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC hydrochloride is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer .
Cat. No.: HY-175870A
CAS No.: 3024878-21-2
(7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRAS G12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer .
Cat. No.: HY-P4087
CAS No.: 1417221-06-7
Cat. No.: HY-P4087B
Synonyms: (1S,9R)-DX8951f
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(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is a non-prodrug camptothecin derivative and a topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1S,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1S,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1S,9R)-Exatecan mesylate is widely used in preclinical studies of various cancers such as pancreatic cancer, lung cancer, breast cancer, and leukemia .
The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
Cat. No.: HY-188120
Research Areas:
AZD5335 is an ADC targeting FRα, with an IC50 of 10.6 nM against human FRα. AZD5335 specifically binds to FRα, mediates internalization and trafficking to lysosomal compartments, while delivering a topoisomerase I inhibitor payload that traps TOP1-DNA cleavage complexes. AZD5335 induces DNA damage response via the ATR, ATM, Chk1 and Chk2 signaling pathways, and increases the levels of phosphorylated KAP1, phosphorylated RPA, phosphorylated γH2AX, as well as PARP cleavage. AZD5335 exhibits bystander cytotoxicity against FRα-negative cells co-cultured with FRα-expressing cells. AZD5335 induces potent and durable responses and complete regression in ovarian cancer models, including models with low FRα expression and models resistant to Elahere, with enhanced efficacy when combined with Carboplatin, Bevacizumab or poly (ADP-ribose) polymerase inhibitors. AZD5335 can be used for ovarian cancer research .
Cat. No.: HY-N10508
CAS No.: 71204-89-2
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Cat. No.: HY-L128
187 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation.
Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).
MCE carefully prepared a unique collection of 187 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.
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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
