产品介绍
Product Description
Biochem/physiol Actions
Cell-permeable precursor of an active-site O-GlcNAc transferase (OGT) inhibitor that effectively downregulates cellular protein O-GlcNAc level.
OSMI-2 is a cell-permeable precursor of an active site-targeting (Kd = 140 nM) O-GlcNAc transferase (OGT) inhibitor. Upon cell entry, OSMI-2 is activated by cellular esterase to the active inhibitor that effectively downregulates cellular protein O-GlcNAc level (20-40 μM for 4 h/HCT116, 50 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-2, 56% with 0.5 μM AT7519, 19% with co-treatment; control cells at 20% and 81% at 0 and 96 hr, respectively).
技术参数
Specifications
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| optical activity | [α]/D -175.0 to -135.0°, c = 1.0 in chloroform-d |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | O=C(N1)C=CC2=C1C=CC(S(N[C@@H](C(N(CC3=CC=CS3)CC(OC)=O)=O)C4=C(C=CC=C4)OC)(=O)=O)=C2 |
