1. Cell Cycle/DNA Damage Autophagy
  2. DNA/RNA Synthesis Autophagy
  3. 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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AP232

AP232 Chemical Structure

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Description

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[1].

In Vitro

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.

Cell Cycle Analysis[1]

Cell Line: NKM-1 cells and K562 cells
Concentration: 5, 10, 20 and 30 μM
Incubation Time: 24 and 48 h
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.
Molecular Weight

329.48

Formula

C20H31N3O

SMILES

NC1(C)CCN(C(CCC2=CNC3=C2C(OCC)=CC=C3)C)CC1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

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Product Name:
AP232
Cat. No.:
HY-178155
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