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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:
3
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3
3 Cited Publications
Cat. No.: HY-P2141A
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2
Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC50 values of 4.5 nM and 31 nM against wild-type BTK and BTK C481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies .
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2 Cited Publications
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Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization by stabilization of the closed, autoinhibited conformation, thereby preventing Arp2/3 complex activation. Wiskostatin is also a dynamin inhibitor with an IC50 value of 20.7 μM and a potent inhibitor of clathrin-mediated endocytosis with an IC50 value of 6.9 μM. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels. Wiskostatin also induces disassembly of podosomes in a murine monocyte cell line .
2
2 Cited Publications
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM .
2
2 Cited Publications
Cat. No.: HY-N2197
CAS No.: 35467-43-7
Category:
Uncaria rhynchophylla (Miq.) Miq. ex Havil. Alkaloids Neurological Disease Rubiaceae Plants Disease Research Fields Indole Alkaloids
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2
2 Cited Publications
ARV-393 is a BCL6 PROTAC degrader. ARV-393 forms a complex with BCL6 and Cereblon, induces BCL6 ubiquitination, and mediates BCL6 degradation via the ubiquitin-proteasome system. ARV-393 enhances CD20 expression, interferon pathway activity and antigen presentation. ARV-393 induces tumor growth inhibition and regression. ARV-393 can be used in research related to non-Hodgkin's lymphoma, high-grade B-cell lymphoma, diffuse large B-cell lymphoma, Burkitt's lymphoma and follicular lymphoma .
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2 Cited Publications
Synonyms: NSC55712; TPU-260 Dihydrochloride
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Cardiovascular Disease Neurological Disease Inflammation/Immunology
TPT-260 Dihydrochloride (NSC55712), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (Kd = ~5 µM). TPT-260 Dihydrochloride increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 Dihydrochloride inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 Dihydrochloride improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 Dihydrochloride exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 Dihydrochloride can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease .
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2 Cited Publications
Cat. No.: HY-162080
CAS No.: 374705-10-9
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METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 μM). METTL1-WDR4-IN-1 inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
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2 Cited Publications
Cat. No.: HY-162080A
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METTL1-WDR4-IN-1 (Compound 1) TFA is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50=144 μM). METTL1-WDR4-IN-1 TFA inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking the m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 TFA can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 TFA can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
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2 Cited Publications
Cat. No.: HY-P2259
CAS No.: 1404188-93-7
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1
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1
1 Cited Publications
Cat. No.: HY-N0492S
CAS No.: 1189471-66-6
Synonyms: Thioctic acid-d5; (±)-α-Lipoic acid-d5; DL-α-Lipoic acid-d5
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1 Cited Publications
Cat. No.: HY-P701373
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: CDK8; Cell Division Protein Kinase 8; Cyclin Dependent Kinase 8; Mediator complex Subunit CDK8; Cyclin-Dependent Kinase 8; Protein Kinase K35; K35; CDK8 Protein Kinase; Mediator Of RNA Polymerase II Transcription Subunit CDK8; IDDHBA; CCNC; SRB11 Homolog
Species:
Human
Source:
Sf9 insect cells
1
1 Cited Publications
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XL01126 is a blood-brain barrier-permeable, selective LRRK2 PROTAC degrader (DC50: 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2)). XL01126 forms a positively cooperative ternary complex with VHL E3 ubiquitin ligase and LRRK2, mediating the polyubiquitination and proteasomal degradation of LRRK2. XL01126 induces Mitophagy. XL01126 is applicable to research related to Parkinson's disease .
1
1 Cited Publications
Cat. No.: HY-N2345
CAS No.: 23567-23-9
1
1 Cited Publications
Cat. No.: HY-W110883
CAS No.: 3618-43-7
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1 Cited Publications
YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization .
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1 Cited Publications
1
1 Cited Publications
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Complement C5-IN-1 is a Complement C5 inhibitor with an IC50 of less than 0.005 μM in serum inhibition assays. Complement C5-IN-1 stabilizes the α-helical conformation, thereby burying the cleavage site and preventing cleavage of C5 by C5 convertase. Complement C5-IN-1 inhibits membrane attack complex deposition in human serum and whole blood complement activation assays. Complement C5-IN-1 can be used in research related to complement-mediated diseases, such as paroxysmal nocturnal hemoglobinuria .
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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
