STAT3-IN-17

Names

[ CAS No. ]:
1245814-52-1

[ Name ]:
STAT3-IN-17

Biological Activity

[Description]:

STAT3-IN-17 is a moderate STAT3 inhibitor (IC50=0.7 μM; HEK-Blue IL-6), with antiproliferative activity in HeLa cells. STAT3-IN-17 has good pharmacokinetic characteristics. STAT3-IN-17 also inhibits pyruvate-ferredoxin oxidoreductase (PFOR), and inhibits Helicobacter pylori[1][2].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> STAT
Research Areas >> Cancer
Research Areas >> Infection
Signaling Pathways >> JAK/STAT Signaling >> STAT

[Target]

STAT3


[In Vitro]

STAT3-IN-17 (化合物 15) (10 μM; 20 h, 48 h) 抑制 STAT3 通路，抑制率为 76.5%，同时抑制 HEK-Blue IL-6 细胞活力至 15%[1]。 STAT3-IN-17 (2.5-40 μM; 24 h) 抑制 STAT3 的磷酸化 (Y705)[1]。 STAT3-IN-17 (10 μM, 50 μM; 48 h) 抑制 HEK 293T 细胞生长，抑制 HeLa 细胞生长，IC50 值为 2.7 μM[1]。 (D)-PPA 1 (化合物 24) 抑制微生物幽门螺杆菌和空肠弯曲杆菌，MIC 值分别为 1.6 μM 和 4.7 μM[2]。

[In Vivo]

STAT3-IN-17 (化合物 15) (5 mg/kg 灌胃给药, 或 25 mg/kg 静脉注射; 单剂量) 在大鼠体内表现出优于 Nitazoxanide (HY-B0217) 的药代动力学特性，具有明显较长的消除半衰期 (t1/2β) (11.1 vs 0.8 h)，更高的绝对生物利用度 (F) (87.4% vs 5.7%)，以及更高的最大血浆浓度 (Cmax) (20.7 vs 1.0 mg/L)[1]。

[References]

[1]. Lü Z, et al. Structure-Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors. ACS Med Chem Lett. 2021 Apr 1;12(5):696-703.  

Chemical & Physical Properties

[ Molecular Formula ]:
C11H6F3N3O3S

[ Molecular Weight ]:
317.24

Related Compounds