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Results for "

aberrant activation

" in MedChemExpress (MCE) Product Catalog:

9

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-148324
    PKM2 activator 5

    		Pyruvate Kinase Cancer
    PKM2 activator 5 (compound 8) is a PKM2 activator with an AC50 value of 0.316 µM. PKM2 activator 5 has the potential to alter the aberrant metabolism of cancer cells .
    PKM2 activator 5
  • HY-13649
    Indibulin
    1 Publications Verification

    ZIO 301; D 24851

    		 Microtubule/Tubulin Apoptosis Neurological Disease Cancer
    Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis .
    Indibulin
  • HY-136173
    Batoprotafib
    5 Publications Verification

    TNO155

    		 SHP2 Phosphatase Cancer
    Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors .
    Batoprotafib
  • HY-109001
    Alicapistat
    1 Publications Verification

    ABT-957

    		 Proteasome Neurological Disease
    Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) . Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM .
    Alicapistat
  • HY-109001A
    (1S,2R)-Alicapistat

    (1S,2R)-ABT-957

    		 Proteasome Neurological Disease
    (1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) . (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM .
    (1S,2R)-Alicapistat
  • HY-163705
    BR-cpd7

    		FGFR Cancer
    BR-cpd7 is a PROTAC degrader for fibroblast growth factor receptor FGFR1/2 with DC50 of 10 nM. BR-cpd7 arrests cell cycle, inhibits proliferations of FGFR1/2 aberrant activated tumor cells. (Pink: ligand for target protein FGFR-IN-12 (HY-160013); Black: linker; Blue: ligand for E3 ligase Thalidomide-NH-CH2-COOH (HY-131717))
    BR-cpd7
  • HY-161465
    HDAC8-IN-7

    		HDAC Inflammation/Immunology
    HDAC8-IN-7 (H7E), a HDAC8 inhibitor, exerts retinoprotective effects against glaucomatous injury via ameliorating aberrant Müller glia activation and oxidative stress. HDAC8-IN-7 alleviates functional and structural defects within the inner retina .
    HDAC8-IN-7
  • HY-113081R
    1-Methyladenosine (Standard)

    		Endogenous Metabolite PPAR Hedgehog Cancer
    1-Methyladenosine (Standard) is the analytical standard of 1-Methyladenosine. This product is intended for research and analytical applications. 1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis . In Vitro:Compared to surrounding tumor tissues, 1-methyladenosine methylation in RNA is aberrantly elevated in hepatocellular carcinoma (HCC) cell lines and liver cancer stem cells (CSCs). Methylated 1-methyladenosine can promote cholesterol synthesis and activate the Hedgehog signaling pathway by enhancing the translation of PPARδ in liver CSCs, ultimately driving the self-renewal and tumorigenesis of liver cancer stem cells .
    1-Methyladenosine (Standard)
  • HY-117051
    STA-2842

    		Others Cancer
    STA-2842 is a small molecule agent that inhibits heat shock protein 90 (HSP90) to treat autosomal dominant polycystic kidney disease (ADPKD). The disease is caused by inherited mutations in the PKD1 or PKD2 genes that aberrantly activate multiple signaling proteins and pathways that regulate cell proliferation. Through network construction, we found that many HSP90 client proteins associated with ADPKD are regulated by HSP90. STA-2842 induced degradation of these clients in Pkd1?/? primary kidney cells and in vivo. In experiments using conditional Cre-mediated in vivo knockout of Pkd1 in mice, we found that weekly administration of STA-2842 for 10 weeks significantly reduced initial renal cyst formation and kidney growth in mice and slowed disease progression in mice with pre-existing cysts. These improved disease phenotypes were accompanied by improvements in renal function markers and reductions in the expression and activity of HSP90 clients and their effectors, with the extent of this inhibition correlating with the extent of cyst expansion in individual animals. Pharmacokinetic analysis showed that HSP90 was overexpressed in cystic kidney tissue and HSP90 inhibitors were selectively retained in cystic tissue, which is similar to the situation in solid tumors. These results provide a preliminary basis for evaluating HSP90 inhibitors as therapeutic agents for ADPKD.
    STA-2842

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