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WP1066 | JAK2/STAT3 inhibitor

WP1066 (857064-38-1) is an inhibitor of the JAK2/STAT3 pathway as well as STAT5 and AKT.1,2,3 It downregulated Bcl-XL, Mcl-1, and c-myc while activating Bax and inducing apoptosis.1 Active against human malignant glioma U87-MG (IC50 = 5.6µM) and U373-MG (IC50 = 3.7µM) cells. Enhances T-cell cytotoxicity via inhibition of regulatory T-cells.4,5  WP1066 abrogated PD-L1 expression in lymphoma cell lines.6

References/Citations

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

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Catalog#  10-4831-0010

$79.00
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CAS:
857064-38-1
Catalog Number:
10-4831
Activity:
JAK2/STAT3 inhibitor
Chemical Name:
(E)-3-(6-Pyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide
Molecular Weight:
356.22
Molecular Formula:
C18H14BrN3O
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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