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Stafib-2 是一种有效和选择性的转录因子 STAT5b 抑制剂,抑制 STAT5b 和 STAT5a 的 IC50 值分别为 82 nM 和 1.7 μM。Stafib-2 的细胞通透性较差。
Stafib-2 is a potent and selctive inhibitor of the transcription factor STAT5b, with an IC50 of 82 nM and 1.7 μM for STAT5b and STAT5a, respectively. Stafib-2 exhibits poor cell permeability[1].
Stafib-2 has an extremely high affinity for STAT5b (Ki=8.8 nM)[1].Stafib-2 (3-10 μM; 4-48 h) does not show significant activity in K562 and MDA-MB-231 cells[1].
[1]. Elumalai N, et, al. Rational development of Stafib-2: a selective, nanomolar inhibitor of the transcription factor STAT5b. Sci Rep. 2017 Apr 11;7(1):819.
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