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TAK-418

Catalog No. T39252 CAS 1818252-53-7

TAK-418 is a selective and orally active inhibitor of LSD1/KDM1A enzyme with an IC50 of 2.9 nM. TAK-418 unlocks abnormal epigenetic mechanisms and improves autism symptoms in models of neurodevelopmental disorders.

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TAK-418, CAS 1818252-53-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 233.00
5 mg	In stock	$ 578.00
10 mg	In stock	$ 913.00
25 mg	In stock	$ 1,870.00
50 mg	In stock	$ 2,520.00
100 mg	In stock	$ 3,380.00
1 mL * 10 mM (in DMSO)	In stock	$ 678.00

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Purity: 98.87%

ee: 98%

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Description	TAK-418 is a selective and orally active inhibitor of LSD1/KDM1A enzyme with an IC50 of 2.9 nM. TAK-418 unlocks abnormal epigenetic mechanisms and improves autism symptoms in models of neurodevelopmental disorders.
Targets&IC50	LSD1/KDM1A:2.9 nM
In vivo	TAK-418 (1 mg/kg; oral; once daily for 14 days) improves certain autism spectrum disorder (ASD)-like behaviors in rodents that model neurodevelopmental disorders.[1] TAK-418 increases H3K4me1/2/3 and H3K9me2 levels of the Ucp2 gene and induces Ucp2 mRNA expression in primary cultured rat neurons. TAK-418 also increases H3K4me1/2/3 of the Bdnf gene. TAK-418 avoids steric interference of GFI1B in the binding pocket by generating a tightly formylated adduct form of coenzyme flavin adenine dinucleotide (FAD). TAK-418 exhibits favorable pharmacokinetic profiles in rodents and inhibits LSD1 enzymatic activity in the brain without causing hematological toxicity in rodents.[1] A single administration of 1 or 3 mg/kg of TAK-418 increases H3K4me2 levels of the Ucp2 gene in the mouse brain.[1] TAK-418 can improve neurological problems at cellular, molecular, gene expression, functional, and functional levels in the KS mouse model (Kmt2d+/βGeo mice).[2]

Molecular Weight	356.91
Formula	C17H25ClN2O2S
CAS No.	1818252-53-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 49.5 mg/mL (138.7 mM), Sonication and heating to 60℃ are recommended.

H2O: 15.0 mg/mL (42.0 mM)

References and Literature

1. Baba R, et al. LSD1 enzyme inhibitor TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models. Sci Adv. 2021;7(11):eaba1187. 2. Zhang L, et al. Inhibition of KDM1A activity restores adult neurogenesis and improves hippocampal memory in a mouse model of Kabuki syndrome. Mol Ther Methods Clin Dev. 2021;20:779-791.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Clinical Compound Library Bioactive Compound Library Bioactive Compounds Library Max Covalent Inhibitor Library Histone Modification Compound Library

Related Products

Related compounds with same targets

Seclidemstat GSK-LSD1 YUKA1 LSD1-IN-25 GSK2879552 L-2-Hydroxyglutaric acid disodium KDM5-C70 GSK-LSD1 dihydrochloride

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TAK-418 1818252-53-7 Chromatin/Epigenetic Histone Demethylase TAK 418 TAK418 inhibitor inhibit

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