2. Epigenetics
  3. SF3B1
  4. Spliceostatin A

Spliceostatin A，是 FR901464 (HY-16212) 的甲基化衍生物，是一种有效的抗肿瘤活性分子。Spliceostatin A 通过结合 SF3B1 抑制剪接并促进前体 mRNA 的积累。SF3B1 是剪接体中 U2 小核核糖核蛋白的一个亚复合体。Spliceostatin A 诱导慢性淋巴细胞白血病 (CLL) 细胞凋亡 (Apoptosis)。

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Spliceostatin A Chemical Structure

Spliceostatin A Chemical Structure

CAS No. : 391611-36-2

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Spliceostatin A 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Spliceostatin A, the FR901464 (HY-16212) methylated derivative, is a potent anti-tumor agent. Spliceostatin A inhibits splicing and promotes pre-mRNA accumulation by binding SF3B1. SF3B1 is a subcomplex of U2 small nuclear ribonucleoprotein in the spliceosome. Spliceostatin A induces Apoptosis in chronic lymphocytic leukemia (CLL) cells[1][2][3].

IC50 & Target

IC50: 5.5 nM (wild-type SF3B1), 4.9 nM (SF3B1mutatant)[1]
体外研究
(In Vitro)

Spliceostatin A (2.5-20 nM; 0-24 h) 以剂量和时间依赖的方式诱导 CLL 细胞出现 Caspase 依赖性凋亡[1]。
Spliceostatin A (10 nM, 20 nM; 24 h) 与 ABT-199 或 ABT-263 有协同作用，增加 IL4/CD40L (10 ng/mL, 300 ng/mL;6 h) 处理后 CLL 细胞的凋亡，并降低相关蛋白磷酸化水平[1]。
Spliceostatin A 抑制正常 B (CD19+) 和 T (CD3+) 淋巴细胞的活力，IC50 分别为 12.1 nM 和 61.7 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Spliceostatin A 相关抗体:

Apoptosis Analysis[1]

Cell Line: CLL cells
Concentration: 0, 2.5 nM, 5 nM, 10 nM, and 20 nM
Incubation Time: 0, 6 h, 12 h, and 24 h
Result: Increased cell apoptosis.

Western Blot Analysis[1]

Cell Line: CLL cells
Concentration: 10 nM, and 20 nM
Incubation Time: 24 h; treated after 10 ng/mL IL4 and/or 300 ng/mL CD40L for 6 h
Result: Decreased the level of PARP, phosphorylated STAT6 (pSTAT6), phosphorylated IκBα (pIκBα), Mcl-1L, Bcl-xL , Bcl-2 and Hsc70.
分子量

521.64

Formula

C28H43NO8
CAS 号
性状

固体

颜色

White to off-white

运输条件

Shipping with dry ice.
储存方式

-80°C, protect from light
纯度 & 产品资料
参考文献

Spliceostatin A 相关分类

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  • 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.

Keywords:

Spliceostatin A391611-36-2SF3B1Splicing Factor 3b Subunit 1Inhibitorinhibitorinhibit

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Spliceostatin A
目录号：
HY-16466
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