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.
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- No. CAS: 2226228-02-8
- Fòrmula: C11H14F2N6O7S
- Peso molecular:412.33
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
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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 |
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| 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
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[PMID: 32912429] |
In Vitro
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.
In Vivo
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.
Chemical Information
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No. CAS 2226228-02-8
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Peso molecular 412.33
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ML901 Related Classifications
HY-171215 Related Classifications
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