1. Epigenetics
  2. SF3B1
  3. Spliceostatin A

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.

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Spliceostatin A Chemical Structure

Spliceostatin A Chemical Structure

CAS No. : 391611-36-2

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Based on 1 publication(s) in Google Scholar

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Description

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]

In Vitro

Spliceostatin A (2.5-20 nM; 0-24 h) induces caspase-dependent apoptosis of CLL cells in a dose- and time-dependent manner[1].
Spliceostatin A (10 nM, 20 nM; 24 h) in combination with ABT-199 or ABT-263 synergises, augments apoptosis in CLL cells following IL4/CD40L (10 ng/mL, 300 ng/mL; 6 h) treatment, and reduce phosphorylation levels of related proteins[1].
Spliceostatin A inhibits the viability of normal B (CD19+) and T (CD3+) lymphocytes with IC50s of 12.1 nM, and 61.7 nM, respectively[1].

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

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.
Molecular Weight

521.64

Formula

C28H43NO8

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H]1C[C@@H](NC(/C=C\[C@@H](OC(C)=O)C)=O)[C@@H](C)O[C@H]1C/C=C(C)/C=C/[C@@H]2[C@@H](O)[C@]3(CO3)C[C@@](C)(OC)O2

Shipping

Shipping with dry ice.

Storage

-80°C, protect from light

Purity & Documentation
References
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    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:
Spliceostatin A
Cat. No.:
HY-16466
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