Molecular Formula | C24H30Cl2N6OS |
Molar Mass | 521.51 |
Solubility | 10 mM in DMSO |
Storage Condition | -20℃ |
In vitro study | LY2409881 inhibits constitutively activated NF-ƘB, and causes concentration- and time-dependent growth inhibition and apoptosis in diffuse large B-cell lymphoma (DLBCL) cells. In the ovarian cancer cell line SKOV3, LY2409881 demonstrates moderate cytotoxicity. LY2409881 is synergistic with doxorubicin and cyclophosphamide in SUDHL2 cell in inhibiting the cell growth, but not in LY1 cell. In both SUDHL2 and LY1 cells, LY2409881 is synergistic with the histone deacetylase (HDAC) inhibitor romidepsin in inhibiting the cell growth. |
In vivo study | In SCID-beige xenograft mouse model, LY2409881 (50, 100, and 200 mg/kg, i.p.) significantly inhibits the tumor growth. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.682 ml | 8.411 ml | 16.823 ml |
5 mM | 0.336 ml | 1.682 ml | 3.365 ml |
10 mM | 0.168 ml | 0.841 ml | 1.682 ml |
5 mM | 0.034 ml | 0.168 ml | 0.336 ml |
biological activity | LY2409881 is an effective selective IKK2 inhibitor with IC50 of 30 nM, which is more than 10 times higher than IKK1 and other common kinases. |
in vitro study | LY2409881 inhibits constitutively activated NF-ƘB, and causes concentration- and time-dependent growth inhibition and apoptosis in diffuse large B- cell lymphoma (DLBCL) cells. in the ovarian cancer cell line SKOV3, LY2409881 demonstrates moderate cytotoxicity. LY2409881 is synergistic with doxorubicin and cyclophosphamide in SUDHL2 cell in inhibiting the cell growth, but not in LY1 cell. In both SUDHL2 and LY1 cells, LY2409881 is synergistic with the histone deacetylase (HDAC) inhibitor romidepsin in inhibiting the cell growth. |
in vivo study | in SCID-beige xenograft mouse model, LY2409881 (50, 100, and 200 mg/kg, I. p.) significantly inhibits the tumor growth. |