ML901
ML901 is a reaction-hijacking PfTyrRS inhibitor that blocks ATP consumption and translation. ML901 inhibits PfYRS by forming a covalent Tyr-ML901 adduct and blocking tRNA tyrosylation. ML901 inhibits Atg7-mediated GABARAP activation/transthioesterification and E1 ubiquitin-like activating enzyme activity. ML901 can be used for research on P. falciparum malaria.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2226228-02-8
- 分子式: C11H14F2N6O7S
- 分子量:412.33
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
|
PfYRS |
Atg7 33 nM (IC50) |
UAE 5.39 μM (IC50) |
NAE 28 μM (IC50) |
GABARAP |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1650 | EC50 |
10.02 μM
Compound: 4
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Antiproliferative activity against human H1650 cells assessed as reduction in cell viability after 72 hrs by cell titer glow assay
Antiproliferative activity against human H1650 cells assessed as reduction in cell viability after 72 hrs by cell titer glow assay
|
[PMID: 32912429] |
体外実験
ML901 (200 nM; 3 h) activates the amino acid starvation/eIF2α phosphorylation pathway in Plasmodium falciparum through an aaRS-related mechanism[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID (engrafted with human RBCs)[2]
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Dosage:50 mg/kg
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Administration:i.p.; single dose
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Result:A single 50 mg/kg i.p. dose reduced parasitemia to baseline.
化学情報
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CAS 番号 2226228-02-8
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分子量 412.33
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分子式 C11H14F2N6O7S
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SMILES
O[C@@H]1[C@H](O)[C@@H](COS(N)(=O)=O)O[C@H]1N2C3=NC=NC(N)=C3C(OC(F)F)=N2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[2]. Xie SC, et al. Reaction hijacking of tyrosine tRNA synthetase as a new whole-of-life-cycle antimalarial strategy. Science (New York, N.Y.). 2022 Jun 03;376(6597):1074-1079. [Content Brief]
[3]. Xie SC, et al. Targeting Aminoacyl tRNA Synthetases for Antimalarial Drug Development. Annu Rev Microbiol. 2023 Sep 15;77:111-129. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)