Biochem/physiol Actions
Active site-targeting, potent and selective histone deacetylase 6 inhibitor that augments the cytotoxicity ofbortezomib, epirubicin, and daunorubicin.
NR-160 is an active site-targeting, potent and selective histone deacetylase 6 inhibitor (HDAC6 IC50 = 30 nM; IC50 >2 μM against HDAC1/2/3/4/8) that upregulates HL60 cellular acetylation of HDAC6 substrate α-tubulin (2.5 μM), but not that of class I HDACs substrate histone H3. NR-160 augments the apoptosis induction by the proteasome inhibitor bortezomib (0.6/1.2 nM BTZ with 2.5/5.0 μM NR-160; HL60) and significantly enhances the cytotoxicity of DNA-intercalating anti-cancer drugs epirubicin and daunorubicin (2.5 or 5.0 μM NR-160 in combination with 10 nM of either compound to T-ALL line HSB-2).
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | FC(F)(C1=CC=CC=C1C(N(CC2=CC=C(C=C2)C(NO)=O)CC3=NN=NN3CC4=CC=CC=C4)=O)F |
| InChI | 1S/C25H21F3N6O3/c26-25(27,28)21-9-5-4-8-20(21)24(36)33(14-18-10-12-19(13-11-18)23(35)30-37)16-22-29-31-32-34(22)15-17-6-2-1-3-7-17/h1-13,37H,14-16H2,(H,30,35) |
| InChI key | MEWDNULKAXEKII-UHFFFAOYSA-N |
