2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Apoptosis Cell Cycle/DNA Damage
  3. JAK STAT Apoptosis Caspase PARP
  4. WP-1034

WP-1034 是一种 JAK-STAT 抑制剂，在急性髓系白血病 (AML) 中具有促凋亡和抗白血病活性。WP-1034 可阻断 Stat 3 和 Stat 5 的激活。WP-1034 可诱导细胞周期阻滞并触发细胞凋亡 (apoptosis)。WP-1034 可用于 AML 研究。

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WP-1034

WP-1034 Chemical Structure

CAS No. : 857064-42-7

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WP-1034 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

查看所有亚型
JAK1 JAK2 JAK3 Tyk2 JAK

查看 STAT 亚型特异性产品:

查看所有亚型
STAT3 STAT5 STAT6 STAT1

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WP-1034 is a JAK-STAT inhibitor with proapoptotic and antileukemic activity in acute myeloid leukemia (AML). WP-1034 blocks activation of Stat 3 and 5. WP-1034 induces cell cycle arrest and triggers apoptosis. WP-1034 can be used for AML research[1].

体外研究
(In Vitro)

WP-1034 (1-6 μM，7 天) 以剂量依赖的方式抑制 OCIM2 和 K562 细胞的集落形成生长，并抑制新鲜 AML 细胞的白血病集落形成与细胞增殖[1]。
WP-1034 (1-10 μM，0-4 小时) 以时间和剂量依赖的方式抑制 OCIM2 细胞中 Stat3 和 Stat5 的磷酸化，表明其能有效抑制 AML 细胞中的 Jak-Stat 信号通路[1]。
WP-1034 (5 μM，0-16 小时) 诱导 OCIM2 细胞发生亚 G0 期细胞周期阻滞[1]。
WP-1034 (3-6 μM) 以剂量依赖的方式诱导 OCIM2 细胞凋亡，并伴有 caspase 3 和 PARP 裂解，而这种作用可被 caspase 抑制剂 Ac-DEVD-CHO (HY-P1001) 阻断[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

WP-1034 相关抗体:

Cell Proliferation Assay[1]

Cell Line: OCIM2, K562, AML and marrow cells
Concentration: 1, 2, 2.5, 3, 4, 5, 6, 7.5 and 10 μM
Incubation Time: 7 days
Result: Suppressed the colony-forming growth of OCIM2 cells in a dose-dependent manner at concentrations ranging from 1 to 5 μM.
Almost completely abolished cell proliferation at concentrations of ≥4 μM.
Inhibited the proliferation of K562 cells by >80% at concentrations of ≥5 μM.
A concentration of at least 10 μM was necessary to inhibit OCIM2 cell proliferation by >80%.
Inhibited the proliferation of AML colony-forming blasts in a dose-dependent manner at concentrations ranging from 1 to 6 μM.
Suppressed AML colony-forming blast proliferation at more than 50% at 5 μM.
Almost completely inhibited AML proliferation at 6 μM.
Showed a dose-dependent inhibition of the growth of healthy marrow between 4 to 6 μM.
The inhibition of normal marrow cells was less than the inhibition of AML blast cells at the same concentrations.

Western Blot Analysis[1]

Cell Line: OCIM2 cells
Concentration: 1, 2.5, 5, 7.5 and 10 μM
Incubation Time: 20 and 40 min, 1, 2, 3, and 4 h
Result: Reduced phospho-Stat 3 and phospho-Stat 5 levels to undetectable levels after incubation times of ≥1 hour.
Significantly down-regulated Stat 3 and Stat 5 phosphorylation at concentrations of 1, 2.5, 5, 7.5 and 10 μM for 2 hours.
Showed no effect on levels of phospho-Stat 1.
Induced dose-dependent caspase 3 cleavage.
Resulted in a dose-dependent increase in cleaved PARP protein levels.

Cell Cycle Analysis[1]

Cell Line: OCIM2 cells
Concentration: 5 μM
Incubation Time: 0, 2, 4, 6, and 16 h
Result: Induced cell cycle arrest at Sub-G0 phase at 6 hours of incubation, with around 23% of the cells accumulating at sub-G0 phase at 16 hours of incubation.

Apoptosis Analysis[1]

Cell Line: OCIM2 cells
Concentration: 4 μM
Incubation Time: 2 h
Result: Induced apoptotic cell death in OCIM2 cells, and this effect was blocked by the caspase inhibitor Ac-DEVD-CHO.
分子量

321.33

Formula

C18H15N3O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

WP-1034 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WP-1034857064-42-7WP1034WP 1034JAKSTATApoptosisCaspasePARPJanus kinasepoly ADP ribose polymeraseOCIM2JAK-STATAMLStat 3Stat 5K562Inhibitorinhibitorinhibit

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