Chemical Structure : TAK-418
CAS No.:
1818252-53-7
TAK-418
(TAK418)
Catalog No.: PC-20519Not For Human Use, Lab Use Only.
TAK-418 (TAK418) is a potent, specific inhibitor of LSD1 (KDM1A) enzyme activity with IC50 of 2.9 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TAK-418 (TAK418) is a potent, specific inhibitor of LSD1 (KDM1A) enzyme activity with IC50 of 2.9 nM.
does not inhibit recombinant human MAO-A and MAO-B with IC50 of >100 uM.
TAK-418 (0.1-10 uM) increases H3K4me1/2/3 and H3K9me2 levels at the Ucp2 gene and induces Ucp2 mRNA expression in primary cultured rat neurons, also increases H3K4me1/2/3 at the Bdnf gene.
TAK-418 has minimal impact on the interaction between LSD1 and its cofactor, GFI1B.
Single administration of TAK-418 at 1 or 3 mg/kg increases H3K4me2 levels at Ucp2 gene in the mouse brain.
TAK-418 normalizes mRNA expression dysregulated in neurodevelopmental disorder model rodents.
TAK-418 produces inverse correlation against the histone modification and DNA methylation levels altered in VPA rats and poly I:C mice.
TAK-418 ameliorates some ASD-like behaviors in neurodevelopmental disorder model rodents.
Physicochemical Properties
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M.Wt
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356.91
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Formula
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C17H25ClN2O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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O=C(C1=CSC([C@H]2[C@H](NCC3CC3)C2)=C1)NC4CCOCC4.[H]Cl
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References
1. Baba R, et al. ci Adv. 2021 Mar 12;7(11):eaba1187.
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