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

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.

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WP-1034

WP-1034 Chemical Structure

CAS No. : 857064-42-7

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WP-1034 Related Antibodies

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JAK1 JAK2 JAK3 Tyk2 JAK

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STAT3 STAT5 STAT6 STAT1

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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

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

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].

In Vitro

WP-1034 (1-6 μM, 7 days) suppresses the colony-forming growth of OCIM2 and K562 cells in a dose-dependent manner, and inhibits leukemia colony-forming cell proliferation of fresh AML cells[1].
WP-1034 (1-10 μM, 0-4 h) inhibits Stat 3 and Stat 5 phosphorylation in a time- and dose-dependent manner in OCIM2 cells, indicating that it effectively inhibits Jak-Stat signaling in AML cells[1].
WP-1034 (5 μM, 0-16 h) induces Sub-G0 phase cell cycle arrest in OCIM2 cells[1].
WP-1034 (3-6 μM) induces apoptosis in OCIM2 cells in a dose-dependent manner with caspase 3 and PARP cleavage, and this effect is blocked by the caspase inhibitor Ac-DEVD-CHO (HY-P1001)[1].

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

WP-1034 Related Antibodies

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.
Molecular Weight

321.33

Formula

C18H15N3O3
CAS No.
SMILES

O=C(N[C@@H](C1=CC=CC=C1)C)/C(C#N)=C/C2=CC=C([N+]([O-])=O)C=C2
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WP-1034 Related Classifications

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    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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