PM-43I

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PM-43I 是 STAT5/6 Src Homology 2 (SH2) 结构域的选择性抑制剂。

PM-43I is a selective inhibitor of STAT5/6 Src Homology 2 (SH2) domain, binds recombinant STAT6 and STAT5B (IC50=1.8 and 3.8 uM) with much lower affinity for STAT3 (IC50=29.9 uM); potently inhibits both STAT5- and STAT6-dependent allergic airway disease in mice; PM-43I reverses preexisting allergic airway disease in mice with a minimum ED50 of 0.25 μg/kg.

Western Blot Analysis Cell Line:Beas-2B immortalized human airway cells Concentration:0.05, 0.1, 0.5, 1, 2.5, 5 μM Incubation Time:2 h Result:Inhibited STAT6 phosphorylation level to 18%, 21% at 2.5 and 5 μM, respectively.

PM-43I (intranasal administration; 5 μg per mouse; every other day; 18 d) activity is restricted to the lung by intranasal administration. Animal Model:Mice injected with Ovalhumin/Alum Dosage:5 μg per mouse Administration:Intranasal administration; 5 μg per mouse; every other day; 18 days Result:Showed no effect on the sensisization of peripheral spleenocytes to ovalbumin.

PM-43-I

JAK/STAT Signaling

STAT

STAT

——

——

1637532-77-4

559.559

C30H30N3O6P

>98% (HPLC)

In Vitro:?DMSO : 35 mg/mL (45.00 mM)

O=P(OCOC(C(C)(C)C)=O)(OCOC(C(C)(C)C)=O)C(F)(F)C1=CC=C(/C(C)=C/C(N[C@@H]2C(N(CC(N(C)C3=CC=CC=C3)=O)CCCC2)=O)=O)C=C1

(4-((E)-4-(((3S,6S)-6-(methyl(phenyl)carbamoyl)-4-oxo-1,2,3,4,6,7-hexahydroazepino[3,2,1-hi]indol-3-yl)amino)-4-oxobut-2-en-2-yl)phenyl)phosphonic acid

(-20℃)

With Ice Pack

≥ 2 years