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

AP232 是一种选择性的 U2AF1-UHM 抑制剂,其 IC50 值为 7.96 μM。AP232 对其他含 UHM 的蛋白质表现出 2.8-24 倍的选择性。AP232 具有抗白血病活性,并且在携带剪接因子突变的细胞系中显示出更高的活性。AP232 可以诱导白血病细胞 G2/M 期和 G1 期停滞,损害溶酶体酸化,并抑制自噬 (autophagy)。AP232 可用于癌症研究,如白血病。

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AP232

AP232 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

AP232 抑制 U2AF1 的 U2 辅助因子同源基序 (U2AF1-UHM),其 IC50 值为 7.96 μM,并且对其他含 UHM 的蛋白质 (RBM39-UHM, SPF45-UHM, PUF60-UHM, U2AF2-UHM) 表现出 2.8-24 倍的选择性[1]
AP232 (40 μM) 可稳定内源性全长 U2AF1,并降低其在 K562 细胞中对链霉蛋白酶的敏感性[1]
AP232 (1-1000 μM, 72 h) 可抑制 6 种白血病细胞系 (MV4-11, NKM-1, K562, MOLM13, HNT-34, MONO-MAC1) 的细胞生长[1]
AP232 (5-30 μM, 24-48 h) 可破坏白血病细胞的细胞周期[1]
AP232 (20 μM, 2 h) 可降低 NKM-1、K562 和 MV4-11 细胞中功能性溶酶体的比例[1]
AP232 (10-30 μM, 48 h) 可抑制 NKM-1 和 K562 细胞中的自噬[1]

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.
分子量

329.48

Formula

C20H31N3O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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产品名称:
AP232
目录号:
HY-178155
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