2. Cell Cycle/DNA Damage Apoptosis Stem Cell/Wnt JAK/STAT Signaling Protein Tyrosine Kinase/RTK Epigenetics PI3K/Akt/mTOR
  3. Deubiquitinase Apoptosis STAT JAK Akt PI3K
  4. 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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WCY-8-67

WCY-8-67 Chemical Structure

CAS No. : 3052618-54-6

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WCY-8-67 Related Antibodies

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Description

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[1].

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.

WCY-8-67 Related Antibodies

Apoptosis Analysis[1]

Cell Line: Kasumi-1 and Skno-1 cells
Concentration: 0, 1.25, 5, 7.5 μM
Incubation Time: 48 h
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 (20-40 mg/kg, p.o., once daily, 12 days) exhibits potent anti-tumor activity in Skno-1 subcutaneous xenograft model[1].
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.

Animal Model: Skno-1 cells (1 × 107) were subcutaneously implanted into the flanks of 6-week-old female NU/NU mice[1]
Dosage: 20, 40 mg/kg
Administration: p.o., once daily, 12 days
Result: Reduced tumor weight and volume.
Showed no significant changes in body weight.
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]
Dosage: 40 mg/kg
Administration: p.o., once daily, 42 days
Result: Decreasedspleen weight and hCD45+ leukemic cell percentage in bone marrow, spleen, and peripheral blood.
Reduced tumor burden and extends survival.
Animal Model: Primary t(8;21) AML cells were intravenously injected into the tail veins of the 6-week-old NOG mice[1]
Dosage: 20 mg/kg
Administration: i.p., once daily, 14 days
Result: Decreased hCD45+ cell infiltration in bone marrow, spleen, and peripheral blood.
Prolonged survival and reduces spleen weight.
Molecular Weight

449.57

Formula

C25H32FN7
CAS No.
SMILES

CN(C)CCN(C1=C2C(CN(C3=C4C=CC=CC4=C(F)C=C3)C2)=NC(N5CCNCC5)=N1)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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WCY-8-67 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:

WCY-8-673052618-54-6DeubiquitinaseApoptosisSTATJAKAktPI3KDUBsJanus kinasePKBProtein kinase BPhosphoinositide 3-kinaseJAK/STAT3PI3K/AKTAML cellsacute myeloid leukemiaInhibitorinhibitorinhibit

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