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

AP232 dihydrochloride is a selective U2AF1-UHM Inhibitor with an IC50 of 7.96 μM. AP232 dihydrochloride exhibits 2.8-24-fold selectivity against other UHM-containing proteins. AP232 dihydrochloride exerts anti-leukemia activity and shows higher activities in cell lines carrying splicing factor mutations. AP232 dihydrochloride can induce leukemia cells G2/M and G1 arrest, impair lysosome acidification, and inhibit autophagy. AP232 dihydrochloride can be used for the research of cancer, such as Leukemia.

For research use only. We do not sell to patients.

AP232 dihydrochloride

AP232 dihydrochloride Chemical Structure

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Description

AP232 dihydrochloride is a selective U2AF1-UHM Inhibitor with an IC50 of 7.96 μM. AP232 dihydrochloride exhibits 2.8-24-fold selectivity against other UHM-containing proteins. AP232 dihydrochloride exerts anti-leukemia activity and shows higher activities in cell lines carrying splicing factor mutations. AP232 dihydrochloride can induce leukemia cells G2/M and G1 arrest, impair lysosome acidification, and inhibit autophagy. AP232 dihydrochloride can be used for the research of cancer, such as Leukemia[1].

In Vitro

AP232 dihydrochloride 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) dihydrochloride stabilizes endogenous full-length U2AF1 and reduces its sensitivity to Pronase in K562 cell[1].
AP232 (72 h) dihydrochloride 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) dihydrochloride disrupts the cell cycle of leukemia cells[1].
AP232 (20 μM, 2 h) dihydrochloride reduces the proportion of functional lysosomes in NKM-1, K562, and MV4-11 cells[1].
AP232 (10-30 μM, 48 h) dihydrochloride 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

402.40

Formula

C20H33Cl2N3O

Appearance

Solid

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 dihydrochloride
Cat. No.:
HY-178155A
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