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SF3B1 inhibitor

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16399
    Pladienolide B
    5 Publications Verification

    		 Apoptosis SF3B1 Cancer
    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 .
    Pladienolide B
  • HY-16466
    Spliceostatin A

    		SF3B1 Cancer
    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 .
    Spliceostatin A
  • HY-168534
    WX-02-23

    		SF3B1 Apoptosis Cancer
    WX-02-23 is a small-molecule probe that stereoselectively and site-specifically binds to C258 of FOXA1 and C1111 of SF3B1. WX-02-23 remodels FOXA1's chromatin binding and pioneer activity in a DNA-dependent manner, disrupts spliceosome assembly, and enhances the thermal stability of SF3B1. WX-02-23 inhibits tumor cell proliferation and induces apoptosis. WX-02-23 can be used for research on cancers such as prostate cancer .
    WX-02-23
  • HY-141881
    PROTAC-O4I2

    		PROTACs Apoptosis SF3B1 Cancer
    PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells .
    PROTAC-O4I2
  • HY-158783
    SACLAC

    		Ceramidase Bcl-2 Family LPL Receptor Apoptosis Neurological Disease
    SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a Ki of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models .
    SACLAC
  • HY-122637
    Sudemycin K

    		SF3B1 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) .
    Sudemycin K
  • HY-181421
    WX-02-43

    		SF3B1 Cancer
    WX-02-43 is a weak covalent inhibitor of SF3B1, and is the (1S,3R) enantiomer of WX-02-23 (HY-168534). WX-02-43 cannot effectively covalently modify the C258 site in the DNA-binding domain of FOXA1, and its inhibitory activity against SF3B1 is also weaker than that of WX-02-23. WX-02-43 serves as a negative control probe that fails to remodel the chromatin binding pattern and transcriptional activity of FOXA1. WX-02-43 can be used in studies on cancers such as prostate cancer to verify the specific effects of WX-02-23 on FOXA1 and SF3B1 targets .
    WX-02-43
  • HY-15867
    Meayamycin B

    (+)-Meayamycin B

    		 SF3B1 Bcl-2 Family Apoptosis Cancer
    Meayamycin B ((+)-Meayamycin B) is a potent SF3B1 inhibitor. Meayamycin B upregulates the proapoptotic Mcl-1S and downregulates Mcl-1L 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 .
    Meayamycin B

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