WP1066
JAK/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
Biochemicals & reagents
857064-38-1
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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TARGET: Kinase; Transcription factor -- PATHWAY: AKT; Apoptosis inducer; Myc; JAK/STAT; Transcription -- RESEARCH AREA: Cell death; Immunology -- DISEASE AREA: Cancer