| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| W409263-1ml |
1ml |
现货  |
|
| 英文别名 | (S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | WP1066 |
| 生化机理 | WP1066 是一种新型的 JAK2 和 STAT3 抑制剂，在 HEL 细胞中的 IC50 值分别为 2.30 μM 和 2.43 μM；对 JAK2、STAT3、STAT5 和 ERK1/2 而非 JAK1 和 JAK3 具有活性。WP1066 可诱导细胞凋亡。第 1 阶段。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | K v1.3通道阻断剂；信号转导和转录激活因子3抑制剂 |
| 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A cell permeable inhibitor of Stat3 and JAK2 protein tyrosine kinase. Information WP1066 is a novel inhibitor ofJAK2andSTAT3withIC50of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1. WP1066 markedly inhibits the growth of HEL cells carrying the JAK2 V617F mutant isoform in a dose-dependent manner with IC20, IC50 and IC80 of 0.8, 2.3 and 3.8 μM. WP1066 at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μM inhibits the phosphorylation of JAK2, STAT3, STAT5, and ERK1/2 without affecting the phosphorylation of JAK1 and JAK3 in erythroid leukemia HEL cells that express the JAK2 V617F isoform. WP1066 at concentrations ranging from 0.5 to 3.0 μM inhibits the proliferation of AML colony-forming cells obtained from patients and that of the AML cell lines OCIM2 and K562 in a dose-dependent manner. WP1066 at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μM dose-dependently decreases JAK2 and pJAK2 protein levels as well as downstream phosphorylation levels of STAT3, STAT5, and AKT in OCIM2 and K562 cells. WP1066 at concentrations of 2 μM inhibits OCIM2 cell multiplication by inducing accumulation of cells at the G0-G1 phase of the cell cycle. WP1066 at concentrations of 1, 2, or 3 μM induces apoptosis in both OCIM2 and K562 cells in a dose-dependent fashion by activating procaspase-3 and cleaving PARP. WP1066 at concentrations of 5 μM prevents the phosphorylation of STAT3, and at concentrations of 2.5μM WP1066 significantly inhibits cell survival and proliferation in Caki-1 and 786-O renal cancer cells. WP1066 at concentrations of 5 μM suppresses HIF1α and HIF2α expression and VEGF production in Caki-1 and 786-O renal cancer cells. In vivo WP1066 orally administrated at dose of 40 mg/kg once daily for 19 days significantly inhibits the tumours growth in Caki-1 xenograft mice, with decreased immunostaining of phosphorylated STAT3 and reduced length of CD34-positive vessels. cell lines： Concentrations：0 - 6 μM Incubation Time：72 hours Powder Purity:≥99% |
| IC50 | JAK2, IC50: 2.3 μM |
|---|
| Canonical SMILES | CC(NC(=O)\C(=C\C1=NC(=CC=C1)Br)C#N)C2=CC=CC=C2 |
|---|---|
| 分子量 | 356.22 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 45 mg/mL (202.05 mM); Water: 45 mg/mL (202.05 mM); Ethanol: 45 mg/mL (202.05 mM); |
|---|
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Colorless Transparent Liquid) | Pass |
| Record the entire process by video | Conform |
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