PS-1145

SKU: orb1304547

Description

PS-1145 is a potent and selective inhibitor of IκB kinase (IKK), exhibiting an IC50 of 88 nM. This small molecule is widely used in biochemical and cellular research to investigate NF-κB signaling pathways in both in vitro and in vivo models of inflammation and cancer.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 431898-65-6
• MW: 322.75
• Purity: >99.99% (May vary between batches)
• Formula: C₁₇H₁₁ClN₄O
• SMILES: Clc1cc(NC(=O)c2cccnc2)c2[nH]c3cnccc3c2c1
• Target: IκB/IKK,Apoptosis
• Solubility: DMSO:50 mg/mL (154.92 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+90% Corn Oil:2.5 mg/mL (7.75 mM);Ethanol:2 mg/mL (6.2 mM)

Bioactivity

• Target IC50:
  IKKϵ:88 nM
• In Vivo:
  PS-1145 inhibits the proliferation of primary human CD4(+) T cells and impedes the activation of NF-κB and AP-1 transcription factors through the cooperative engagement of CD3 and CD28 co-receptors. Additionally, PS-1145 blocks TNFalpha-induced NF-kappaB activation by inhibiting the phosphorylation of IkappaBalpha and disrupting the protective effect of IL-6 on Dex-induced apoptosis.
• In Vitro:
  Administering 50 mg/kg of PS-1145 intravenously in male Wistar rats with DMBA-induced skin tumors resulted in the upregulation of p53 and activation of caspases, coupled with the downregulation of NF-κB and VEGF factors, thereby enhancing apoptosis in tumor cells.
• Cell Research:
  The inhibitory effect of PS-1145 on MM growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-h cultures are pulsed with 10 μL of 5 mg/ml MTT to each well for the last 4 h of 48-h cultures, followed by 100 μl of isopropanol containing 0.04N HCl. Absorbance is measured at 570 nm using a spectrophotometer. (Only for Reference)

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

Apoptosis, IκB kinase, IκB, inhibit, IKK, IKK Inhibitor X, IkB/IKK, IkB, I kappa B kinase, Inhibitor, PS 1145, PS1145, PS-1145

Compound Identifiers

PubChem CID

9949093