AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML) In Vitro AC-4-130 (0.1-100 μM; 72 hours) leads to a significant increase in apoptosis in a dose-dependent and time-dependent manner in MV4-11 or MOLM-13 cells. ? AC-4-130 (2, 5 μM; 72 hours) induces cell cycle arrest with an increase in G0/G1 arrested cells and a concomitant reduction in cells in S or G2/M. ? AC-4-130 (0.5-2; 24 hours) reveals reduced pY-STAT5 levels both in the cytoplasm and nucleus. ? AC-4-130-mediated STAT5 inhibition efficiently blocks the proliferation and clonogenic growth of primary human AML cells, while healthy CD34+ cells are less sensitive. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:STAT5
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AC-4-130
CAS number：1834571-82-2(DMSO) molecular formula：C37H36ClF5N2O5S
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1834571-82-2(DMSO) | molecular formula | C37H36ClF5N2O5S |
| molecular weight | 751.20 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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