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.
For research use only. We do not sell to patients.
- Formula: C20H31N3O
- Molecular Weight:329.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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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Molecular Weight 329.48
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Formula C20H31N3O
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SMILES
NC1(C)CCN(C(CCC2=CNC3=C2C(OCC)=CC=C3)C)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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