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PDK4-IN-1
CAS No. 2310262-10-1
PDK4-IN-1 ( —— )
Catalog No. M21874 CAS No. 2310262-10-1
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
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Biological Information
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Product NamePDK4-IN-1
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NoteResearch use only, not for human use.
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Brief DescriptionPDK4-IN-1 is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM).
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DescriptionPDK4-IN-1 treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO. The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1. PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis. PDK4-IN-1 (compound 8c)-induced phosphorylation of p53 on serine 15 is a dose-dependent response in both HCT116 and RKO cells. PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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Recptor——
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Research AreaPyruvate dehydrogenase kinase 4 (PDK4),84 nM
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Indication——
Chemical Information
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CAS Number2310262-10-1
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Formula Weight357.41
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Molecular FormulaC22H19N3O2
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Purity>98% (HPLC)
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Solubility——
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SMILES——
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Lee D, et al. Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases. J Med Chem. 2019 Jan 24;62(2):575-588.
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