Biochem/physiol Actions
Potent and selective IκB kinase β (IKK2, IKKβ, IKKbeta) inhibitor with in vitro and in vivo anticancer efficacy.
LY2409881 is a potent IκΒ kinase β (IKK2, IKKβ, IKKbeta) inhibitor (IC50 = 30 nM) that effectively inhibits 10 ng/mL TNFα-induced IκB phosphorylation in LY10 DLBCL cells (by >95%; 10 μM) and exhibits good selectivity by kinase profiling among more than 300 kinases (>10-fold selectivity). LY2409881 enhances TNFα cytotoxicity in SKOV3 ovarian cancer cultures (~20% survival with 316 nM LY2409881 & 10 ng/mL TNFα in 72 hrs; 100% survival with LY2409881 or TNFα alone) by blocking NF-κB antiapoptotic signal activation without affecting TRADD & FADD proapoptotic pathway induction. When administered in vivo, LY2409881 is shown to suppress LY10 xenograft-derived tumor growth in mice (50-200 mg/kg, twice weekly ip.).
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | H2O: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | [s]1c2c(c(ccc2)C(=O)NC5CC5)cc1c3nc(ncc3Cl)NCCCN4CCN(CC4)C |
| InChI key | BNFAYJPQCPZQND-UHFFFAOYSA-N |

