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^[1][2][3].

IC50: 5.5 nM (wild-type SF3B1), 4.9 nM (SF3B1mutatant)^[1]

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.

521.64

C₂₈H₄₃NO₈

391611-36-2

Solid

White to off-white

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 with dry ice.

-80°C, protect from light

• [1]. Larrayoz M, et al. The SF3B1 inhibitor spliceostatin A (SSA) elicits apoptosis in chronic lymphocytic leukaemia cells through downregulation of Mcl-1. Leukemia. 2016 Feb;30(2):351-60.  [Content Brief]

  [2]. Kaida D, et al. Spliceostatin A targets SF3b and inhibits both splicing and nuclear retention of pre-mRNA. Nat Chem Biol. 2007 Sep;3(9):576-83.  [Content Brief]

  [3]. Roybal GA, et al. Spliceostatin A inhibits spliceosome assembly subsequent to prespliceosome formation. Nucleic Acids Res. 2010 Oct;38(19):6664-72.  [Content Brief]