ML309
ML309 is a highly selective and potent inhibitor of the R132H mutant isocitrate dehydrogenase 1 (IDH1 R132H), with an IC50 of 96 nM. ML309 is a competitive inhibitor of α-KG, with a Ki value of 156 nM, and its inhibitory activity against the wild-type IDH1 is greater than 35 μM. ML309 effectively reduces the production of the tumor metabolite 2-HG in U87MG cells. ML309 can be used as a chemical probe to study the role of the mutant IDH1 in cancer.
For research use only. We do not sell to patients.
- CAS No.: 1355446-05-7
- Formula: C29H29FN4O2
- Molecular Weight:484.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
R132H IDH1 96 nM (IC50) |
Chemical Information
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CAS No. 1355446-05-7
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Molecular Weight 484.56
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Formula C29H29FN4O2
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SMILES
O=C(N(C(C1=CC=CC=C1C)C(NC2CCCC2)=O)C3=CC=CC(F)=C3)CN4C5=CC=CC=C5N=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[1]. Davis M, et al. ML309: A potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells. 2012 Apr 16 [updated 2013 May 8]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ML309 Related Classifications
HY-121916 Related Classifications
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