Spliceostatin A
CAS No. : 391611-36-2
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|---|---|---|
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| 1mg | $1500 | In-stock |
| 5mg | $3350 | In-stock |
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| Cat. No. : | HY-16466 |
| M.Wt: | 521.64 |
| Formula: | C28H43NO8 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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].
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