PM-43I( PM-43-I )

Catalog No. M12467 CAS No. 1637532-77-4

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PM-43I
Note

Research use only, not for human use.
Brief Description

PM-43I is a selective inhibitor of STAT5/6 Src Homology 2 (SH2) domain.
Description

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.
In Vitro

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.
In Vivo

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.
Synonyms

PM-43-I
Pathway

JAK/STAT Signaling
Target

STAT
Recptor

STAT
Research Area

——
Indication

——

CAS Number

1637532-77-4
Formula Weight

559.559
Molecular Formula

C30H30N3O6P
Purity

>98% (HPLC)
Solubility

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

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
Chemical Name

(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

1. Knight JM, et al. J Biol Chem. 2018 May 8. pii: jbc.RA117.000567.

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