Biological Activity
OTS193320 is a SUV39H2 methyltransferase inhibitor for histone methylation, DNA-damage-response and cancer-cell research. OTS193320 IC50 was 22.2 nM.
In Vitro
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| SUV39H2 inhibition | Biochemical assay. [1] | OTS193320 IC50 was 22.2 nM. |
| Cancer-cell growth | A549 lung-cancer and breast-cancer cell models. [1] | Growth IC50 was 0.38 µM in A549 and 0.41–0.56 µM in the tested breast-cancer cells. |
| Mechanistic markers | H3K9 methylation and doxorubicin-response assays. [1] | Lower H3K9me3 and altered γH2AX responses accompanied increased cytotoxic effects with doxorubicin. |
In Vivo
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| In-vivo limitation | Reported preclinical development comparison. [1] | The authors did not obtain tumor-growth inhibition with OTS193320 without toxicity. OTS186935 xenograft results should not be assigned to OTS193320. |
Interpretation
OTS186935 xenograft efficacy must not be attributed to OTS193320.
