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Table 2 Small molecules shown to modulate H3S10ph deposition, FDA-approved for clinical trials

From: Rebelled epigenome: histone H3S10 phosphorylation and H3S10 kinases in cancer biology and therapy

Name Target Clinical trial no Phase Disease H3S10ph source
Barasertib (AZD1152-HQPA|AZD281) AURKB/A NCT03366675; NCT03217838 Phase 1/2 Small cell lung cancer, acute myeloid leukemia /high-risk myelodysplastic syndrome, advanced solid tumors [149]
Flavopiridol CDKs, including CDK8 NCT03593915; NCT03441555; NCT03563560 Phase 1/2 Myelodysplastic syndromes; acute myeloid leukemia [150, 151]
BI-847325 AURKA/B/C NCT01324830 Phase 1 Solid tumors [152]
Alisertib AURKA NCT02860000 Phase 2 Breast cancer [91]
SEL120 CDK8 NCT04021368 Phase 1 Acute myeloid leukemia or high-risk myelodysplastic syndrome [153] and unpublished observations
SEL24/MEN1703 PIM kinases NCT03008187 Phase 1/2 Acute myeloid leukemia [154]
PIM447 PIM kinases NCT02370706 Phase 1 Myelofibrosis [62, 63]