TAK-418 | LSD1 (KDM1A) inhibitor | Probechem Biochemicals

Chemical Structure : TAK-418

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TAK-418 (TAK418)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	356.91
分子式	C17H25ClN2O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	O=C(C1=CSC([C@H]2[C@H](NCC3CC3)C2)=C1)NC4CCOCC4.[H]Cl

参考文献

1. Baba R, et al. ci Adv. 2021 Mar 12;7(11):eaba1187.

TAK-418 (TAK418)

生物&药学活性

物理化学性质&存储条件

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TAK-418 (TAK418)

生物&药学活性

物理化学性质&存储条件

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