Preferred Label : Splicing Inhibitor H3B-8800;
NCIt synonyms : Splicing Modulator H3B-8800; Splicing Factor Inhibitor H3B-8800;
NCIt related terms : H3B-8800;
NCIt definition : An orally bioavailable inhibitor of the splicing factor 3B subunit 1 (SF3B1), with
potential antineoplastic activity. Upon administration, H3B-8800 binds to and blocks
the activity of SF3B1, a core spliceosome protein that is mutated in various cancer
cells. This modulates RNA splicing by preventing aberrant mRNA splicing by the spliceosome,
blocks RNA mis-splicing, enhances proper RNA splicing and prevents the expression
of certain tumor-associated genes. This leads to an induction of apoptosis and prevents
tumor cell proliferation. In many cancer cells, core spliceosome proteins, including
SF3B1, U2 small nuclear ribonucleoprotein auxiliary factor 1 (U2AF1), serine/arginine-rich
splicing factor 2 (SRSF2) and U2 small nuclear ribonucleoprotein auxiliary factor
subunit-related protein 2 (ZRSR2), are mutated and aberrantly activated leading to
a dysregulation of mRNA splicing.;
UNII : 90YLS47BRX;
CAS number : 1825302-42-8;
Molecule name : H3B 8800; H3B-8800;
NCI Metathesaurus CUI : CL512654;
Origin ID : C129546;
UMLS CUI : C4331307;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
