WP1066 | JAK2/STAT3 inhibitor

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:
C17H14BrN3O
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
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.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
10 mg$79.00
50 mg$295.00

WP1066 (857064-38-1) is an inhibitor of the JAK2/STAT3 pathway as well as STAT5 and AKT.1-3 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 See propyl analog WP1130.

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

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:
C17H14BrN3O
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
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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