SF3B1 Inhibitor

Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis.

H3B-8800 is a potent and orally active SF3B splicing modulator. H3B-8800 direct interaction with the SF3b complex and shows anti-cancer activity. H3B-8800 has the potential for the research of acute myeloid leukemia (AML) with SF3B1 mutant.

Meayamycin B ((+)-Meayamycin B) is a potent SF3B1 inhibitor. Meayamycin B upregulates the proapoptotic Mcl-1_S and downregulates Mcl-1_L at the pre-mRNA splicing level. Meayamycin B does not regulate the alternative splicing of Bcl-x. Meayamycin B and ABT-737 (HY-50907) synergistically causes Apoptosis. Meayamycin B exhibits anticancer activity against non-small cell lung cancer.

Sudemycin K is a selective splicing inhibitor targeting SF3B1. Sudemycin K blocks U2 snRNP recognition of branch point sequences in pre-mRNA, inducing tumor-specific splicing deregulation and apoptosis. Sudemycin K is promising for research of SF3B1-mutated malignancies such as chronic lymphocytic leukemia (CLL) and myelodysplastic syndromes (MDS).

18-Deoxyherboxidiene (RQN-18690A) is a potent angiogenesis inhibitor. 18-Deoxyherboxidiene targets SF3b, a spliceosome component that is a subcomplex of the U2 small nuclear ribonucleoprotein (snRNP) in the spliceosome. 18-Deoxyherboxidiene inhibits the migration and tube formation of human umbilical vein endothelial cells (HUVECs) without significant cell toxicity. 18-Deoxyherboxidiene has the potential for cancer research.