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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- CAS No.: 857064-42-7
- Formule: C18H15N3O3
- Masse moléculaire:321.33
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Activité biologique
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.
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Cell Line:OCIM2, K562, AML and marrow cells
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Concentration:1, 2, 2.5, 3, 4, 5, 6, 7.5 and 10 μM
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Incubation Time:7 days
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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.
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Cell Line:OCIM2 cells
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Concentration:1, 2.5, 5, 7.5 and 10 μM
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Incubation Time:20 and 40 min, 1, 2, 3, and 4 h
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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.
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Cell Line:OCIM2 cells
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Concentration:5 μM
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Incubation Time:0, 2, 4, 6, and 16 h
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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.
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Cell Line:OCIM2 cells
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Concentration:4 μM
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Incubation Time:2 h
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Result:Induced apoptotic cell death in OCIM2 cells, and this effect was blocked by the caspase inhibitor Ac-DEVD-CHO.
Chemical Information
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CAS No. 857064-42-7
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Masse moléculaire 321.33
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Formule C18H15N3O3
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WP-1034 Related Classifications
HY-111275 Related Classifications
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