1. Epigenetics
  2. Histone Demethylase
  3. TAK-418

TAK-418 

Cat. No.: HY-138830
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TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models.

For research use only. We do not sell to patients.

TAK-418 Chemical Structure

TAK-418 Chemical Structure

CAS No. : 1818252-53-7

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Description

TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models[1][2].

In Vivo

TAK-418 (1 mg/kg; p.o.; once daily for 14 days) ameliorates some autism spectrum disorder (ASD) -like behaviors in neurodevelopmental disorder model rodents[1].
TAK-418 increases H3K4me1/2/3 and H3K9me2 levels at the Ucp2 gene and induced Ucp2 mRNA expression in primary cultured rat neurons. TAK-418 also increases H3K4me1/2/3 at the Bdnf gene. TAK-418 avoids the steric interference with GFI1B in the binding pocket through the generation of a compact formylated adduct form of coenzyme flavin adenine dinucleotide (FAD). TAK-418 shows a good pharmacokinetic profile in rodents and inhibits LSD1 enzyme activity in the brain without causing hematological toxicity in rodents[1].
Single administration of TAK-418 at 1 or 3 mg/kg increases H3K4me2 levels at Ucp2 gene in the mouse brain[1].
TAK-418 can ameliorate neurological problems at the cellular, molecular, gene expression, and functional levels in a mouse model of KS (Kmt2d+/βGeo mice)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

356.91

Formula

C₁₇H₂₅ClN₂O₂S

CAS No.
SMILES

O=C(C1=CSC([[email protected]]2[[email protected]](NCC3CC3)C2)=C1)NC4CCOCC4.[H]Cl

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

TAK-418TAK418TAK 418Histone DemethylaseneurodevelopmentaldisorderUcp2behaviorsInhibitorinhibitorinhibit

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TAK-418
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