[CAS NO. 391611-36-2] Spliceostatin A
PRODUCTS SPECIFICATIONS [391611-36-2]
DESCRIPTION [391611-36-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 521.64 |
| Molecular Formula | C28H43NO8 |
| 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 |
Summary
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 IC
50
s of 12.1 nM, and 61.7 nM, respectively
[1]
.
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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [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.
- [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.
- [3] Roybal GA, et al. Spliceostatin A inhibits spliceosome assembly subsequent to prespliceosome formation. Nucleic Acids Res. 2010 Oct;38(19):6664-72.