Spliceostatin A is a potent inhibitor of in vitro and in vivo pre-mRNA splicing. It was shown to inhibit splicing and to interact with an essential component of the spliceosome, SF3b. Spliceostatin A is an inhibitor of RNA synthesis with excellent anticancer activity against a variety of human cancer cell lines. Spliceostatin A inhibits mitotic clone expansion and adipogenesis.
Structure of 391611-36-2
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Size | Price | Stock | Quantity |
---|---|---|---|
5 mg | $2999 | In stock |
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Capabilities & Facilities
Spliceostatin A is a potent natural product derivative and a highly cytotoxic ADC payload employed in antibody-drug conjugates for targeted cancer therapy. Its mechanism involves inhibition of the spliceosome by binding to the SF3b subunit, disrupting pre-mRNA splicing and leading to accumulation of unspliced transcripts. This interference with RNA processing induces cell cycle arrest and apoptosis in proliferating tumor cells. Spliceostatin A’s chemical structure allows covalent attachment to monoclonal antibodies through cleavable or non-cleavable linkers, enabling precise intracellular delivery in ADC applications while maintaining systemic stability.
Within antibody-drug conjugates, Spliceostatin A is conjugated to antibodies using linker chemistries designed for plasma stability and controlled intracellular payload release. The ADC remains inactive during circulation, minimizing off-target cytotoxicity. Following receptor-mediated internalization into antigen-expressing tumor cells, enzymatic or chemical cleavage liberates Spliceostatin A. Once released, it inhibits the SF3b complex, interferes with pre-mRNA splicing, and triggers apoptosis. This targeted delivery ensures cytotoxic activity is confined to tumor cells, enhancing specificity and reproducibility of tumor-targeted therapy.
Applications of Spliceostatin A include incorporation into ADCs targeting both solid tumors and hematologic malignancies with defined antigen expression. Its compatibility with diverse linker systems allows optimization of conjugation efficiency, intracellular release kinetics, and pharmacokinetic profiles. Preclinical studies demonstrate reproducible cytotoxicity in target-expressing tumor cells. Spliceostatin A supports the development of ADCs with defined spliceosome-inhibiting mechanisms, providing mechanistically precise apoptosis induction and tumor cell elimination, facilitating rational design of antibody-drug conjugates for targeted oncology applications.
Catalog | Product Name | CAS | Inquiry |
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BADC-00781 | Spliceostatin B | ||
BADC-00782 | Spliceostatin C |
What is Spliceostatin A?
Spliceostatin A is a potent inhibitor of the spliceosome, acting as a cytotoxic payload in ADCs. It modulates RNA splicing, causing disruption of cell proliferation and induction of apoptosis in target cells.
28/10/2017
Dear BOC Sciences, how is Spliceostatin A used in ADCs?
Spliceostatin A is conjugated to antibodies to selectively deliver its spliceosome-inhibiting effects to tumor cells. This targeted approach enhances therapeutic activity and reduces off-target cytotoxicity.
20/9/2018
Dear BOC Sciences, which linkers are compatible with Spliceostatin A?
Spliceostatin A can be conjugated via cleavable linkers, including peptide and disulfide types, as well as non-cleavable linkers. Linker selection impacts drug release, ADC stability, and pharmacological profile.
3/3/2019
Dear Sir, may I ask if BOC Sciences provides Spliceostatin A ADC development?
BOC Sciences offers custom ADC services for Spliceostatin A, including payload conjugation, linker optimization, and analytical support, enabling precise design of ADC constructs for research purposes.
17/11/2022
Dear BOC Sciences, what precautions are required for handling Spliceostatin A?
Spliceostatin A is highly cytotoxic and must be handled with strict safety protocols, including PPE, controlled laboratory conditions, and adherence to biosafety guidelines to prevent exposure.
2/9/2019
— Dr. Jason Carter, Senior Scientist (USA)
Spliceostatin A from BOC Sciences arrived with high purity, enabling precise and reproducible experiments.
3/3/2019
— Dr. Christopher Reed, Senior Scientist (USA)
Spliceostatin A from BOC Sciences demonstrated excellent stability and high purity for our ADC conjugation experiments.
2/9/2019
— Ms. Lena Fischer, R&D Manager (Germany)
The batch of Spliceostatin A arrived with comprehensive QC documentation, supporting fast integration into our research.
17/11/2022
— Dr. William Hughes, Biotech Researcher (UK)
We achieved reproducible conjugation results using Spliceostatin A, reflecting the high quality of BOC Sciences’ supply.
28/10/2017
— Mr. Antoine Dubois, Medicinal Chemist (France)
Excellent communication and technical support during Spliceostatin A procurement helped maintain our project schedule.
— Dr. Ingrid Svensson, Laboratory Director (Sweden)
High-quality Spliceostatin A with reliable documentation ensured our ADC payload testing was accurate and reproducible.
20/9/2018
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