SML4109
PDK4-IN-1
≥98% (HPLC)
Synonym(s):
1-(1-(Piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9,10-dione hydrochloride, 1-[1-(4-Piperidinyl)-1H-pyrazol-4-yl]-9,10-anthracenedione hydrochloride
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About This Item
Quality Level
Assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
SMILES string
Cl.[n]2(ncc(c2)c3c4c(ccc3)C(=O)c5c(cccc5)C4=O)C1CCNCC1
InChI key
ZIMLKZKPNALXKK-UHFFFAOYSA-N
Biochem/physiol Actions
PDK4-IN-1 (PDK4i-8c) is a cell-penetrating anthraquinone derivative that has been identified as an allosteric inhibitor of pyruvate dehydrogenase kinase 4 (PDK4), whis is binding to its lipoamide binding site with a high affinity (IC50 = 84 nM). PDK4-IN-1 is orally available, demonstrates excellent metabolic stability, and exhibits a promising pharmacokinetic profile in rat studies. Moreover, PDK4-IN-1 substantially enhances glucose tolerance in mice with diet-induced obesity and mitigates allergic reactions in a passive cutaneous anaphylaxis mouse model. The in vivo data support its effectiveness as a potential treatment for diabetes. Additionally, PDK4-IN shows notable anticancer properties by regulating cell proliferation, transformation, and apoptosis.
Disclaimer
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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