应用 |
A cell permeable inhibitor of Stat3 and JAK2 protein tyrosine kinase. |
产品介绍 |
WP1066是一种新型JAK2和STAT3抑制剂,在HEL细胞中IC50分别为2.30 μM和2.43 μM;对JAK2,STAT3,STAT5和ERK1/2具有抑制活性,而对JAK1和JAK3没有作 |
备注 |
WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. |
生化机理 |
WP1066 (WP10666) is a cell permeable AG 490 tyrphostin analog that effectively inhibits the STAT3 pathway. The inhibitor is a potent antitumor agent as displayed in the growth inhibition of malignant glioma cell and acute myelogenous leukemia cells. Stat3 Inhibitor III, WP1066 has shown more potency as an antitumor agent than AG 490 when inhibiting malignant glioma growth in vitro. WP1066 also acts as an immune adjuvant by inducing proliferation of effector T cells and upregulating CD86 and CD80. In addition WP1066 has displayed inhibition of JAK2 protein tyrosine kinase as well as suggested activation of Bax. |
别名 |
WP-1066;WP 1066;(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基乙基]-2-丙烯酰胺;(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide;(S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide;WP-1066;WP 1066 |