A cell-permeable flavone derivative that arrests the proliferation of acute myeloid leukemia cells (NB4, U937, HL-60, OCI AML3), in a dose and time-dependent manner (optimum at ~20uM and 96h) and blocks the colony formation in samples from acute myeloid leukemia patients, without affecting normal blood cells. Shown to reduce mitochondrial membrane potential and Bad phosphorylation (at Ser136), induce Bax and caspase 3, 8, and 9 activation in U937 cells. Does not affect the phosphorylation of Akt1, but significantly reduces the expression and phosphorylation of p70S6 kinase in U937 cells. Reported to inhibit the chymotrypsin-like activity of proteasome (IC50 = 2.0uM) and this effect is synergistic with bortezomib.
Primary Target IC50:2u
Solubility:DMSO
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
