SML2989

OSMI-2

≥98% (HPLC)

• Sinónimos: (R)-Methyl 2-(2-(2-methoxyphenyl)-2-(2-oxo-1,2-dihydroquinoline-6-sulfonamido)-N-(thiophen-2-ylmethyl)acetamido)acetate, OSMI 2, OSMI2
• Fórmula empírica (notación de Hill): C₂₆H₂₅N₃O₇S₂
• Número de CAS: 2260542-60-5
• Peso molecular: 555.62
• UNSPSC Code: 12352200
• NACRES: NA.77

Propiedades

• Quality Level: 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

Descripción

Biochem/physiol Actions

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).

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable