WP1066(JAK2/STAT3 inhibitor)

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单价: 1929.00
品牌: Gene Operation
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更新: 2020-10-30
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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

StorageStore 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.

温馨提示:不可用于临床治疗。