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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
4 Results for "
LSD1-GFI1B interaction
" in MedChemExpress (MCE) Product Catalog:
Products (4)
4 Results for "LSD1-GFI1B interaction" in MCE Product Catalog:
2
2 Cited Publications
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Research Areas:
TAK-418 is an orally active, blood-brain barrier-penetrant LSD1 inhibitor with a human IC50 of 2.9 nM. TAK-418 irreversibly inhibits LSD1 by forming a compact flavin-FAD adduct with the catalytic domain FAD, blocking the demethylation of H3K4me1/2 and H3K9me1/2 without disrupting the LSD1-GFI1B interaction. TAK-418 restores normally dysregulated brain gene expression and DNA methylation, increases H3K4me1/2/3 and H3K9me2 at the Ucp2 locus, and induces Ucp2 mRNA expression. TAK-418 rescues defective H3K4 histone modifications, normalizes adult neurogenesis, and improves recognition memory, social behavior, and cognition in rodent models. TAK-418 can be used in research related to neurodevelopmental disorders, Alzheimer's disease, and autism spectrum disorders .
Cat. No.: HY-183202
CAS No.: 1456907-39-3
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NCD38 is a Lysine-specific demethylase 1 (LSD1) inhibitor with a target IC50 of 0.59 μM. NCD38 selectively disrupts LSD1-GFI1B interactions, dissociates LSD1 and CoREST from the ERG super-enhancer. NCD38 increases apoptosis-related protein levels, induces apoptosis and reduces SOX2 and Oct4 levels. NCD38 can be used for the research of acute myeloid leukemia .
Cat. No.: HY-138830B
CAS No.: 1818252-52-6
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TAK-418 free base is an orally active, blood-brain barrier-penetrant LSD1 inhibitor with a human IC50 of 2.9 nM. TAK-418 free base irreversibly inhibits LSD1 by forming a compact flavin-FAD adduct with the catalytic domain FAD, blocking the demethylation of H3K4me1/2 and H3K9me1/2 without disrupting the LSD1-GFI1B interaction. TAK-418 free base restores normally dysregulated brain gene expression and DNA methylation, increases H3K4me1/2/3 and H3K9me2 at the Ucp2 locus, and induces Ucp2 mRNA expression. TAK-418 free base rescues defective H3K4 histone modifications, normalizes adult neurogenesis, and improves recognition memory, social behavior, and cognition in rodent models. TAK-418 free base can be used in research related to neurodevelopmental disorders, Alzheimer's disease, and autism spectrum disorders .
Cat. No.: HY-183105
CAS No.: 2133291-32-2
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DC551040 is an orally active and selective lysine demethylase 1 (LSD1) inhibitor with a human IC50 of 2.14 nM. DC551040 binds to LSD1 via π-π stacking with Trp552, polar interactions with Phe538, and covalent adduct formation with FAD, and disrupts the LSD1-GFI1B-CoREST complex. DC551040 induces H3K4me2 accumulation, apoptosis, and cell differentiation, activates STAT5, NF-κB, AKT, and IL6-STAT3 pathways, and upregulates IL6 expression. DC551040 can be used for the research of acute myeloid leukemia .
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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
