WP1066

10mg

Cat. No.: 76-J32

$115.00

WP1066 is a Janus kinase (Jak) 2 inhibitor. It works by degrading the Jak2 protein, thus blocking its downstream signal transducer and activator of transcription (STAT) and phosphoinositide-3-kinase pathways to result in the activation of the caspase pathway. The Jak/STAT pathway is one of a handful of pleiotropic cascades used to transduce a multitude of signals for development and homeostasis in animals. In mammals, it is the principal signaling mechanism for a wide array of cytokines and growth factors. WP1066 also acts as an immune adjuvant by inducing proliferation of effector T cells and upregulating CD86 and CD80.

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Details

TECHNICAL INFORMATION

Other Names: (S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamine

Chemical Formula: C17H14BrN3O

CAS Number: 857064-38-1

Molecular Weight: 356.22

Purity: >99%

IC50= JAK2= 2.3µm, Stat3= 2.43µm

Appearance: Off-White Solid

Solubility: DMSO

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C. 

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO. Soluble at 71mg/ml

References

Hatiboglu | M.A. | et al (2012). The tumor microenvironment expression of the p-Stat3 influences the efficacy of cyclophosphamide with WP1066 in murine melanoma models. Int. J. Cancer. 131:8-17.

Horiquchi | A. | et al (2010). Stat3 inhibitor WP1066 as a novel therapeutic agent for renal cell carcinoma. Br. J. Cancer. 102-1592-9.

Verstovsek | S. | et al (2008). WP1066 | a novel JAK2 inhibitor | suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin. Cancer Res. 14:788-96.

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