Cat. No. Name Size Price Add Cart
KI1071WP106610 mg$176
WP106625 mg$432

Chemical Characteristic

Product NameWP1066
CAS No.857064-38-1
Molecular Weight 356.22
FormulaC17H14BrN3O
Chemical Name(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide
SmilesC(=O)(/C(=C/c1cccc(n1)Br)/C#N)NC(C)c1ccccc1
Chemical Structure

Biological activities

WP1066 is a novel JAK2 inhibitor. WP1066 markedly and dose-dependently inhibits the growth of HEL cells with an IC50 of 2.3 µM. The IC80 and IC20 of WP1066 are 3.8 and 0.8 µM, respectively. WP1066 prevents the proliferation of BFU-E colony-forming cell. WP1066 causes apoptosis of HEL cells in time- and dose-dependent manners. WP1066 prevents the phosphorylation of JAK2, STAT3, STAT5, and ERK1/2. WP1066 affects the phosphorylation of JAK1 and JAK3.[1] WP1066 inhibits OCIM2 cell multiplication by inducing accumulation of cells at the G0-G1 phase of the cell cycle. WP1066 not only inhibits the phosphorylation of JAK2 but also degrades JAK2 protein. WP1066 activates caspase-3. WP1066 induces cleavage of poly(ADP-ribose) polymerase. WP1066 causes caspase-dependent apoptotic cell death in OCIM2 and K562 cells. [2] In Caki-1 and 786-O renal cancer cells, 5 µM WP1066 prevents the phosphorylation of STAT3. WP1066 at the dose of 2.5 µM significantly inhibits cell survival and proliferation. WP1066 inhibits tumor growth in the murine xenograft model of Caki-1 cells. [3]

Protocols

In vitro WP1066 is dissolved in 1% DMSO, diluted with a 5% dextrose solution, and stored at -20°C until use.[1]

References

[1] Verstovsek S, et al. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation.Clin Cancer Res. 2008, 14(3): 788-796.
[2] Ferrajoli A, et al. WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells. Cancer Res. 2007, 67(23): 11291-1129.
[3] Horiguchi A, et al. STAT3 inhibitor WP1066 as a novel therapeutic agent for renal cell carcinoma. Br J Cancer. 2010, 102(11): 1592-1529.

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