PDK4-IN-1 hydrochloride

SKU: orb1309267

Description

PDK4-IN-1 hydrochloride is an orally bioavailable anthraquinone-based compound that potently inhibits pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 of 84 nM. This inhibitor is a valuable research tool for studying metabolic disorders, such as diabetes and cancer, in both cellular and animal models.

Research Area

Cell Biology, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 2310262-11-2
• MW: 393.87
• Purity: 99.67%
• Formula: C₂₂H₂₀ClN₃O₂
• SMILES: Cl.O=C1c2ccccc2C(=O)c2c(cccc12)-c1cnn(c1)C1CCNCC1
• Target: Apoptosis,Dehydrogenase,PDK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.16 mM);DMSO:125 mg/mL (317.36 mM)

Bioactivity

• Target IC50:
  PDK4:84 nM
• In Vivo:
  PDK4-IN-1 (C57BL/6J mice) treatment significantly improves glucose tolerance. Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs,
• In Vitro:
  PDK4-IN-1 hydrochloride 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 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, p-Akt, PARP1, p53, metabolites, Inhibitor, caspase-3, Apoptosis, anticancer, anti-allergic, antidiabetic, BAX, BCL-xL, Pyruvate dehydrogenase kinase, PDK-4-IN-1 hydrochloride, PDK4-IN-1 Hydrochloride, PDK4, PDK4 IN 1 hydrochloride, PDK4IN1 hydrochloride, PDHK, PDHE1α, PDH kinase

Compound Identifiers

PubChem CID

146026197