sf3b1

H3B-8800 is an SF3B1 modulator that can be used to study transfusion-dependent anemia.

Pladienolide B is a potent spliceosome inhibitor, a macrolide isolated from Streptomyces obtusususus Mer-12, which targets the SF3B1 subunit of the spliceosome.Pladienolide B exerts its antitumor effects by inhibiting pre-mRNA splicing and inducing necrosis.Pladienolide B possesses antitumor activity and can be used to study leukemia and lymphoid tumors. Pladienolide B has antitumor activity and can be used to study leukemia and lymphoid tumors.

Spliceostatin A is an anticancer agent and splicing inhibitor that inhibits the splicing mechanism of the spliceosome and inhibits mitotic clonal expansion and adipogenesis.Spliceostatin A induces cell cycle arrest in the G1 and G2 M phases, and induces apoptosis.

Dyrk1A-IN-5 (compound 5j) is a highly potent and selective DYRK1A inhibitor with an IC50 of 6 nM, reducing the phosphorylation of Thr434 in SF3B1 dose-dependently (IC50 = 0.5 μM) and inhibiting tau phosphorylation at Thr212 (IC50 = 2.1 μM), making it valuable for Down syndrome research [1].

PROTAC-O4I2, a PROTAC ligand targeting splicing factor 3B1 (SF3B1), induced FLAG-SF3B1 degradation in K562 cells with an IC50 value of 0.244 μM. PROTAC-O4I2 induced apoptosis in K562 WT cells.

3’-Me Meayamycin D is a splice modulator that targets SF3B1 and PHF5A, affecting the pre-mRNA splicing process and downregulating MCL-1 expression. It inhibits the proliferation of cancer cell lines HCT116, SW48, A549, DMS53, and DMS114, with a GI50 range of 4.6-7.2 nM. In mice, it demonstrates good plasma stability with a half-life of 16 hours.