LY2409881 trihydrochloride

• CAT Number: I005636
• CAS Number: 946518-60-1
• Molecular Formula: C24H29ClN6OS • 3HCl
• Molecular Weight: 594.4
• Purity: ≥95%
• Synonyms: LY-2409881; LY 2409881
• Target: Apoptosis
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 30 nM
• IUPAC Name: 2-[5-chloro-2-[3-(4-methylpiperazin-1-yl)propylamino]pyrimidin-4-yl]-N-cyclopropyl-1-benzothiophene-4-carboxamide;trihydrochloride
• InChI: InChI=1S/C24H29ClN6OS.3ClH/c1-30-10-12-31(13-11-30)9-3-8-26-24-27-15-19(25)22(29-24)21-14-18-17(4-2-5-20(18)33-21)23(32)28-16-6-7-16;;;/h2,4-5,14-16H,3,6-13H2,1H3,(H,28,32)(H,26,27,29);3*1H
• InChIKey: IEXCRLAGBWKVPW-UHFFFAOYSA-N
• SMILES: CN1CCN(CC1)CCCNC2=NC=C(C(=N2)C3=CC4=C(C=CC=C4S3)C(=O)NC5CC5)Cl.Cl.Cl.Cl

LY2409881（Cat No.:I005636） is a highly potent and selective inhibitor of IKK2 (IκB kinase 2), with an IC50 value of 30 nM. It demonstrates more than a 10-fold selectivity over IKK1 and other commonly targeted kinases. By selectively inhibiting IKK2, LY2409881 effectively interferes with the NF-κB signaling pathway, which plays a crucial role in inflammation and cancer. This compound shows promise as a potential therapeutic agent for conditions associated with aberrant NF-κB signaling, including autoimmune diseases and certain types of cancer.

Reference

[1]. Deng C, et al. The novel IKK2 inhibitor LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-κB. Clin Cancer Res. 2015 Jan 1;21(1):134-45.