Skip to main content

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[153] and unpublished observations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]