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aberrant activation

" in MedChemExpress (MCE) Product Catalog:

13

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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

    		 Apoptosis Microtubule/Tubulin Checkpoint Kinase (Chk) 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-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-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-163705
    BR-cpd7

    		PROTACs 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-13649R
    Indibulin (Standard)

    		Microtubule/Tubulin Apoptosis Neurological Disease Cancer
    Indibulin (Standard) is the analytical standard of Indibulin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-171579
    RS47

    		NF-κB Cancer
    RS47 (Compound 1a) is a selective inhibitor of the non-canonical NF-κB signaling pathway targeting RelB with a Kd of 1.1 μM. RS47 competitively blocks RelB binding to target DNA, inhibiting downstream gene (e.g., BCL3, PIM2) expression, thereby suppressing tumor cell proliferation. RS47 is promising for research of cancers with aberrant activation of the non-canonical NF-κB pathway, such as colorectal cancer and B lymphoma .
    RS47
  • HY-113081R
    1-Methyladenosine (Standard)

    		Reference Standards 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-172747
    TNKS-2-IN-3

    		PARP Cancer
    TNKS-2-IN-3 (Compound 5) is a selective competitive tankyrase 2 (TNKS2) inhibitor with an IC50 value of 0.3 nM, showing over 20-fold selectivity over TNKS1 and more than 100-fold selectivity over PARP1/2. TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway by inhibiting TNKS2-mediated ADP-ribosylation, exhibiting antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 is proming for rasearch of solid tumors with aberrant Wnt pathway activation, such as colorectal cancer .
    TNKS-2-IN-3
  • HY-19916A
    Lisavanbulin dihydrochloride

    BAL-101553 dihydrochloride

    		 Microtubule/Tubulin TNF Receptor CTLA-4 PD-1/PD-L1 Checkpoint Kinase (Chk) Cancer
    Lisavanbulin (BAL-101553) dihydrochloride is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin dihydrochloride exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin dihydrochloride has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin dihydrochloride is also a spindle assembly checkpoint activator, agonistic anti-CD40 antibody, and double immune checkpoint blockade (anti-PD-1 and anti-CTLA-4). Lisavanbulin dihydrochloride induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin dihydrochloride can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma .
    Lisavanbulin dihydrochloride
  • HY-19916
    Lisavanbulin

    BAL-101553

    		 Microtubule/Tubulin Checkpoint Kinase (Chk) TNF Receptor PD-1/PD-L1 CTLA-4 Cancer
    Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin is a BBB-penetrant and orally active antitumor agent, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin is also a spindle assembly checkpoint activator, agonistic anti-CD40 antibody, and double immune checkpoint blockade (anti-PD-1 and anti-CTLA-4). Lisavanbulin induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma .
    Lisavanbulin

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