| Bioactivity | PS-1145 is an IκB kinase (IKK) inhibitor with an IC50 of 88 nM. | ||||||||||||
| Invitro | PS-1145 blocks TNFα-induced NF-κB activation in a dose- and time-dependent fashion in MM cells through inhibition of IκBα phosphorylation. Dexamethasone (Dex), which up-regulates IκBα protein, enhances blockade of NF-κB activation by PS-1145. PS-1145 blocks the protective effect of IL-6 against Dex-induced apotosis. TNFα-induced intracellular adhesion molecule (ICAM)-1 expression on both RPMI8226 and MM.1S cells is also inhibited by PS-1145. Moreover, PS-1145 inhibits both IL-6 secretion from bone marrow stromal cells (BMSCs) triggered by MM cell adhesion and proliferation of MM cells adherent to BMSCs[1]. | ||||||||||||
| Name | PS-1145 | ||||||||||||
| CAS | 431898-65-6 | ||||||||||||
| Formula | C17H11ClN4O | ||||||||||||
| Molar Mass | 322.75 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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