2. Epigenetics
  3. SF3B1
  4. 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

Spliceostatin A Related Antibodies

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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]
Cellular Effect
Cell Line Type Value Description References
CWR22R IC50
0.6 nM
Compound: 1
Suppression of AR-V7 expression in human CWR22Rv1 cells expressing GFP measured after 3 days by FACS assay
Suppression of AR-V7 expression in human CWR22Rv1 cells expressing GFP measured after 3 days by FACS assay
[PMID: 32551017]
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.

Spliceostatin A Related Antibodies

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
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (95.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9170 mL 9.5852 mL 19.1703 mL
5 mM 0.3834 mL 1.9170 mL 3.8341 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (protect from light). When stored at -80°C, please use it within 6 months.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (protect from light). When stored at -80°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9170 mL 9.5852 mL 19.1703 mL 47.9258 mL
5 mM 0.3834 mL 1.9170 mL 3.8341 mL 9.5852 mL
10 mM 0.1917 mL 0.9585 mL 1.9170 mL 4.7926 mL
15 mM 0.1278 mL 0.6390 mL 1.2780 mL 3.1951 mL
20 mM 0.0959 mL 0.4793 mL 0.9585 mL 2.3963 mL
25 mM 0.0767 mL 0.3834 mL 0.7668 mL 1.9170 mL
30 mM 0.0639 mL 0.3195 mL 0.6390 mL 1.5975 mL
40 mM 0.0479 mL 0.2396 mL 0.4793 mL 1.1981 mL
50 mM 0.0383 mL 0.1917 mL 0.3834 mL 0.9585 mL
60 mM 0.0320 mL 0.1598 mL 0.3195 mL 0.7988 mL
80 mM 0.0240 mL 0.1198 mL 0.2396 mL 0.5991 mL
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Spliceostatin A Related Classifications

Help & FAQs
  • 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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