Spliceostatin A
Based on 1 Customer Validation
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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- Reinheit: 96.64%
- CAS. Nr.: 391611-36-2
- Formel: C28H43NO8
- Molecular Weight:521.64
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Speicherung:
-80°C, protect from light
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
IC50: 5.5 nM (wild-type SF3B1), 4.9 nM (SF3B1mutatant)[1]
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Cell Line
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Type | Value | Description | References |
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| CWR22R | IC50 |
0.6 nM
Compound: 1
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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
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[PMID: 32551017] |
| CWR22R | IC50 |
0.6 nM
Compound: 1; SSA
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Inhibition of AR-V7 expression in human 22Rv1 cells
Inhibition of AR-V7 expression in human 22Rv1 cells
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[PMID: 37207846] |
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.
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Cell Line:CLL cells
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Concentration:0, 2.5 nM, 5 nM, 10 nM, and 20 nM
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Incubation Time:0, 6 h, 12 h, and 24 h
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Result:Increased cell apoptosis.
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Cell Line:CLL cells
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Concentration:10 nM, and 20 nM
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Incubation Time:24 h; treated after 10 ng/mL IL4 and/or 300 ng/mL CD40L for 6 h
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Result:Decreased the level of PARP, phosphorylated STAT6 (pSTAT6), phosphorylated IκBα (pIκBα), Mcl-1L, Bcl-xL , Bcl-2 and Hsc70.
Chemical Information
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CAS. Nr. 391611-36-2
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Appearance Solid
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Molecular Weight 521.64
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Formel C28H43NO8
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Color White to off-white
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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
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Versand
Shipping with dry ice.
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Speicherung
-80°C, protect from light
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
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 |
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| 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 |
Spliceostatin A Related Classifications
HY-16466 Related Classifications
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