TAK-418
Based on 2 publication(s) in Google Scholar
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.
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- 純度: 99.81%
- CAS 番号: 1818252-53-7
- 分子式: C17H25ClN2O2S
- 分子量:356.91
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保管条件:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 TAK-418
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生物活性
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KDM1/LSD1 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1818252-53-7
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性状 Solid-Liquid Mixture
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分子量 356.91
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分子式 C17H25ClN2O2S
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Color White to yellow
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SMILES
O=C(C1=CSC([C@H]2[C@H](NCC3CC3)C2)=C1)NC4CCOCC4.[H]Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Nature
Perturbing LSD1 and WNT rewires transcription to synergistically induce AML differentiation. [Abstract]2025 Jun;642(8067):508-518. PMID: 40240608 -
Proc Natl Acad Sci U S A
2025 May 20;122(20):e2425812122. PMID: 40366693
溶剤 & 溶解度
DMSO : 55 mg/mL (154.10 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 16.67 mg/mL (46.71 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5.5 mg/mL (15.41 mM); Clear solution
This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5.5 mg/mL (15.41 mM); Clear solution
This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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. Published 2021 Mar 12. [Content Brief]
[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. Published 2021 Feb 18 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.8018 mL | 14.0091 mL | 28.0183 mL | 70.0457 mL |
| 5 mM | 0.5604 mL | 2.8018 mL | 5.6037 mL | 14.0091 mL | |
| 10 mM | 0.2802 mL | 1.4009 mL | 2.8018 mL | 7.0046 mL | |
| 15 mM | 0.1868 mL | 0.9339 mL | 1.8679 mL | 4.6697 mL | |
| 20 mM | 0.1401 mL | 0.7005 mL | 1.4009 mL | 3.5023 mL | |
| 25 mM | 0.1121 mL | 0.5604 mL | 1.1207 mL | 2.8018 mL | |
| 30 mM | 0.0934 mL | 0.4670 mL | 0.9339 mL | 2.3349 mL | |
| 40 mM | 0.0700 mL | 0.3502 mL | 0.7005 mL | 1.7511 mL | |
| DMSO | 50 mM | 0.0560 mL | 0.2802 mL | 0.5604 mL | 1.4009 mL |
| 60 mM | 0.0467 mL | 0.2335 mL | 0.4670 mL | 1.1674 mL | |
| 80 mM | 0.0350 mL | 0.1751 mL | 0.3502 mL | 0.8756 mL | |
| 100 mM | 0.0280 mL | 0.1401 mL | 0.2802 mL | 0.7005 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
TAK-418 関連分類
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