WCY-8-67
WCY-8-67 is an orally active and selective USP5 inhibitor, with an IC50 value of 1.33 μM. WCY-8-67 induces apoptosis and suppresses JAK/STAT3 and PI3K/AKT signaling pathways in vitro. WCY-8-67 inhibits proliferation of AE-positive AML cells, induces G1 phase arrest and differentiation of AML cells. WCY-8-67 demonstrates potent anti-leukemic efficacy in mice. WCY-8-67 can be used for the study of acute myeloid leukemia.
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- CAS No.: 3052618-54-6
- Formule: C25H32FN7
- Masse moléculaire:449.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
USP5 1.33 μM (IC50) |
In Vitro
WCY-8-67 (0.5-2 μM, 24 h) dose-dependently reduces AML1-ETO (AE) protein abundance in Kasumi-1 and Skno-1 cells[1].
WCY-8-67 (0.5-2 μM, 24 h) inhibits proliferation of AE-positive AML cells (Kasumi-1: IC50 = 1.75 μM; Skno-1: IC50 = 0.99 μM; U937-AE: IC50 = 1.20 μM), but shows negligible effect on AE-negative AML cells (MV-4-11, MOLM-13, HL-60)[1].
WCY-8-67 (0.5-7.5 μM, 24-48 h) induces apoptosis and G1 phase cell cycle arrest in Kasumi-1 and Skno-1 cells[1].
WCY-8-67 (0.5-2 μM, 7 days) reduces colony formation of Kasumi-1 and Skno-1 cells in agarose colony assays, decreasing the number of malignant clones[1].
WCY-8-67 (0.5-2 μM, 24 h) decreases CD34+CD38- leukemia stem cell (LSC) population and increases CD11b+ differentiated cell population in Kasumi-1 and Skno-1 cells[1].
WCY-8-67 (0-2.5 μM, 24 h) suppresses JAK/STAT3 and PI3K/AKT signaling pathways in Kasumi-1 and Skno-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Kasumi-1 and Skno-1 cells
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Concentration:0, 1.25, 5, 7.5 μM
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Incubation Time:48 h
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Result:Downregulated MDM2 and upregulated p53.
Promoted cleavage of PARP1 and activation of caspase-3.
Reduced anti-apoptotic proteins Bcl-2 and Mcl-1.
In Vivo
WCY-8-67 (40 mg/kg, p.o., once daily, 42 days) reduces tumor burden and extends survival in Kasumi-1-luciferase-GFP orthotopic xenograft model[1].
WCY-8-67 (20 mg/kg, i.p., once daily, 14 days) prolongs survival and reduces spleen weight in t(8;21) AML xenograft (PDX) model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Skno-1 cells (1 × 107) were subcutaneously implanted into the flanks of 6-week-old female NU/NU mice[1]
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Dosage:20, 40 mg/kg
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Administration:p.o., once daily, 12 days
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Result:Reduced tumor weight and volume.
Showed no significant changes in body weight.
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Animal Model:Kasumi-1 cells expressing luciferase-GFP (2 × 106) were intravenously injected into the tail veins of the 6-week-old NOG mice[1]
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Dosage:40 mg/kg
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Administration:p.o., once daily, 42 days
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Result:Decreasedspleen weight and hCD45+ leukemic cell percentage in bone marrow, spleen, and peripheral blood.
Reduced tumor burden and extends survival.
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Animal Model:Primary t(8;21) AML cells were intravenously injected into the tail veins of the 6-week-old NOG mice[1]
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Dosage:20 mg/kg
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Administration:i.p., once daily, 14 days
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Result:Decreased hCD45+ cell infiltration in bone marrow, spleen, and peripheral blood.
Prolonged survival and reduces spleen weight.
Chemical Information
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CAS No. 3052618-54-6
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Masse moléculaire 449.57
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Formule C25H32FN7
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SMILES
CN(C)CCN(C1=C2C(CN(C3=C4C=CC=CC4=C(F)C=C3)C2)=NC(N5CCNCC5)=N1)C
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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)
WCY-8-67 Related Classifications
HY-178500 Related Classifications
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