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HomeProduct name listWP1066

WP1066

Synonym(s):STAT3 Inhibitor III, WP1066

WP1066 Structural

What is WP1066?

Description

WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells when given at a concentration of 10 μM. It also induces apoptosis in U87-MG (IC50 = 5.6 μM) and U373-MG (IC50 = 3.7 μM) cells. WP1066 is orally bioavailable, crosses the blood-brain barrier, and demonstrates in vivo activity, including immune activation as indicated by the up-regulation of CD80 and CD86 and the induction of proliferation of effector T cells. In addition to inducing apoptosis in cancer cells, WP1066 suppresses vascular smooth muscle cell proliferation after vascular injury in mice and prevents seizures following brain injury in rats.

The Uses of WP1066

WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells.

What are the applications of Application

Stat3 Inhibitor III, WP1066 is a cell permeable inhibitor of Stat3 and JAK2 protein tyrosine kinase

References

1) Kong?et al.?(2005),?Discovery of WP1066, a novel Stat3/c-myc inhibitor with potent antitumor activity against human melanoma in vitro and in vivo;?Cancer Res.?65?1387 2) Iwamaru?et al.?(2007),?A novel inhibitor of the STAT3 pathway induces apoptosis in malignant glioma cells both invitro and in vivo;?Oncogene?26?2435 3) Ferraioli?et al.?(2007),?WP1066 Disrupts Janus Kinase-2 and Induces Caspase-Dependent Apoptosis in acute Myelogenous Leukemia Cells;?Cancer Res.?67?11291 4) Kong,?et al.?(2008),?A novel inhibitor of signal transducers and activators of transcription 3 activation is efficacious against established central nervous system melanoma and inhibits regulatory T cells;?Clin. Cancer Res.?14?5759 5) Kong,?et al.?(2009),?A novel phosphorylated STAT3 inhibitor enhances T cell cytotoxicity against melanoma through inhibition of regulatory T cells;?Cancer Immunol. Immunother.?58?1023 6) Ma,?et al.?(2017),?Stat3 inhibitor abrogates the expression of PD-1 ligands on Lymphoma cell lines;?J. Clin. Exp. Hematop.?57?21

Properties of WP1066

Melting point: 90-93oC
Boiling point: 569.9±50.0 °C(Predicted)
Density  1.425
storage temp.  +2C to +8C
solubility  Soluble in DMSO (up to at least 25 mg/ml)
form  Off-white solid
pka 11.00±0.46(Predicted)
color  White
Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Safety information for WP1066

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for WP1066

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