LY2409881 trihydrochloride

SKU: orb1306525

Description

LY2409881 trihydrochloride is a potent and selective IKK2 inhibitor with an IC50 of 30 nM, exhibiting over 10-fold selectivity against IKK1 and other common kinases. This compound is a valuable research tool for studying NF-κB signaling in inflammatory and autoimmune disease models, both in cellular assays and in vivo.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 946518-60-1
• MW: 594.43
• Purity: 98.00% (May vary between batches)
• Formula: C₂₄H₃₂Cl₄N₆OS
• SMILES: Cl.Cl.Cl.CN1CCN(CCCNc2ncc(Cl)c(n2)-c2cc3c(cccc3s2)C(=O)NC2CC2)CC1
• Target: Apoptosis,IκB/IKK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.68 mM);DMSO:16 mg/mL (26.92 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  IKKβ:30 nM
• In Vivo:
  LY240988 was moderately toxic to ovarian cancer SKOV3 cell line. In diffuse large B-cell lymphoma cells, LY2409881 inhibited activated NF- B, concentration- and time-dependently inhibiting cell growth and causing apoptosis. In SUDHL2 cells, LY2409881 inhibited cell growth synergistically with cyclophosphamide and adriamycin, but had no synergistic effect on LY1 cells. In SUDHL22 and LY1 cells, histone deacetylase inhibitor romidepsin synergized with LY2409881 to inhibit cell growth.
• In Vitro:
  LY240988 was moderately toxic to ovarian cancer SKOV3 cell line. In diffuse large B-cell lymphoma cells, LY2409881 inhibited activated NF- B, concentration- and time-dependently inhibiting cell growth and causing apoptosis. In SUDHL2 cells, LY2409881 inhibited cell growth synergistically with cyclophosphamide and adriamycin, but had no synergistic effect on LY1 cells. In SUDHL22 and LY1 cells, histone deacetylase inhibitor romidepsin synergized with LY2409881 to inhibit cell growth.
• Cell Research:
  Cytotoxicity is evaluated using the CellTiter-Glo Reagent according to the manufacturer's manual. Experiments are carried out in 96-well plates, with each treatment in triplicate. Samples are taken at typically 24, 48, and 72 hours after treatment. Cytotoxicity is expressed by the decreasing percentage of live cells in each treatment relative to the untreated control from the same experiment. IC50 for each cell line is calculated using the CalcuSyn Version 2.0 software.(Only for Reference)

Storage & Handling

• Storage: Pure form: -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

IKK2, IKK, IkB/IKK, IkB, LY 2409881, LY 2409881 Trihydrochloride, LY-2409881, IκB, Apoptosis

Compound Identifiers

PubChem CID

68856073