| Chemical Properties | Back Directory | [density ]
1.393±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
8.68±0.20(Predicted) | [color ]
White to off-white | [optical activity]
[α]/D -175.0 to -135.0°, c =1.0 in chloroform-d |
| Hazard Information | Back Directory | [Biological Activity]
OSMI-2 is a cell-permeable precursor of an active site-targeting (Kd = 140 nM) O-GlcNAc transferase (OGT) inhibitor. Upon cell entryOSMI-2 is activated by cellular esterase to the active inhibitor th at effectively downregulates cellular protein O-GlcNAc level (20-40 μM for 4 h/HCT11650 μM for 24 h/HEK293T) and renders LNCaP prostate cancer cells dependent on CDK9 for growth (confluency post 96-hr treatment = 73% with 40 μM OSMI-256% with 0.5 μM AT751919% with co-treatment; control cells at 20% and 81% at 0 and 96 hrrespectively). |
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