货号: | IJS1011-0010MG |
保存条件: | -20℃ |
CAS号: | 857064-38-1 |
供应商: | 上海伟进生物科技有限公司 |
数量: | 12 |
英文名: | WP1066(JAK2/STAT3 inhibitor) |
保质期: | 2 years |
规格: | 10MG |
Biological Activity
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WP1066 is a cell-permeable AG490 analogue that acts as an effective JAK2/STAT3 signaling inhibitor. Compared to its parental compound AG490, WP1066 is significantly more potent and active against human malignant gliomas both in vivo and in vitro (IC50=5.6 μM in U87-MG cells and 3.7 μM in U373-MG cells). WP1066 activates Bax, inhibits the expression of c-myc, Bcl-X(L) and Mcl-1, and induces apoptosis [1-2]. Similar to AG490, WP1066 inhibits JAK2 phosphorylation, but unlike AG490, WP1066 also degrades JAK2 protein, thereby blocking its downstream STAT and PI3K pathways [3]. WP1066 functions as a highly potent immune adjuvant by upregulating costimulatory molecules CD80 and CD86 on peripheral macrophages and tumor-infiltrating microglia, stimulating the production of immune- stimulatory cytokines IL-2, IL-4, IL-12, IL-15, and inducing proliferation of effector T cells [4].
Chemical Properties
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Cas No.: 857064-38-1 | M. Wt.: 356.2 |
Formula: C17H14BrN3O | Purity: ≥97% |
Synonym: WP-1066, WP 1066 | |
Chemical Name: 3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide | |
Appearance: Off-white solid | |
Solubility: Soluble in DMSO (10 mg/mL) or Ethanol | |
Storage:Store solid at +4 ºC, protect from light. |
Application Concentration (Just for reference)
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The appropriate working concentration of WP1066 depends on cell types, cell culture properties and specific applications. It is recommended that researchers start with optimal experiments for first use.