AP232
AP232 is a selective U2AF1-UHM Inhibitor with an IC50 of 7.96 μM. AP232 exhibits 2.8-24-fold selectivity against other UHM-containing proteins. AP232 exerts anti-leukemia activity and shows higher activities in cell lines carrying splicing factor mutations. AP232 can induce leukemia cells G2/M and G1 arrest, impair lysosome acidification, and inhibit autophagy. AP232 can be used for the research of cancer, such as Leukemia.
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- Formule: C20H31N3O
- Masse moléculaire:329.48
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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
AP232 inhibits the U2 auxiliary factor homology motif of U2AF1 (U2AF1-UHM) with an IC50 of 7.96 μM and exhibits 2.8-24-fold selectivity against other UHM-containing proteins (RBM39-UHM, SPF45-UHM, PUF60-UHM, U2AF2-UHM) [1].
AP232 (40 μM) stabilizes endogenous full-length U2AF1 and reduces its sensitivity to Pronase in K562 cell [1].
AP232 (72 h) inhibits cell growth in 6 leukemia cell lines (MV4-11, NKM-1, K562, MOLM13, HNT-34, MONO-MAC1) [1].
AP232 (5-30 μM, 24-48 h) disrupts the cell cycle of leukemia cells [1].
AP232 (20 μM, 2 h) reduces the proportion of functional lysosomes in NKM-1, K562, and MV4-11 cells [1].
AP232 (10-30 μM, 48 h) inhibits autophagy in NKM-1 and K562 cells [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NKM-1 cells and K562 cells
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Concentration:5, 10, 20 and 30 μM
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Incubation Time:24 and 48 h
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Result:Increased the G2/M phase ratio at 48 h in NKM-1 cells.
Reduced the S phase and increased the sub-G1 phase at 24 h in K562 cells.
Increased the G1 phase while reduced the S and G2/M phases at 48 h in K562 cells.
Chemical Information
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Masse moléculaire 329.48
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Formule C20H31N3O
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SMILES
NC1(C)CCN(C(CCC2=CNC3=C2C(OCC)=CC=C3)C)CC1
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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)
AP232 Related Classifications
HY-178155 Related Classifications
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