| Identification | Back Directory | [Name]
Benzamide, N-hydroxy-4-[[(1-methylethyl)[(2,3,4,5-tetrafluorophenyl)sulfonyl]amino]methyl]- | [CAS]
2490284-25-6 | [Synonyms]
NN-390
Benzamide, N-hydroxy-4-[[(1-methylethyl)[(2,3,4,5-tetrafluorophenyl)sulfonyl]amino]methyl]- | [Molecular Formula]
C17H16F4N2O4S | [MOL File]
2490284-25-6.mol | [Molecular Weight]
420.38 |
| Chemical Properties | Back Directory | [density ]
1.463±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A crystalline solid | [pka]
8.83±0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma)[1]. | [in vivo]
NN-390 (male CD-1 mice, 20 mg/kg, IP, single dose) increases plasma stability[1].
NN-390 can improve PAMPA (parallel artificial membrane permeability assay)-BBB (blood-brain barrier) score[1].
Pharmacokinetic Parameters of NN-390 in male male CD-1 mice[1].
| Compound | KT-531 | 5a; NN-390 | | t1/2 (h) | 1.05 | 1.90 | | Cmax (ng/mL) | 493 | 750 | | AUClast (h*ng/mL) | 1576 | 2523 | | AUClnf (h*ng/mL) | 1519 | 2548 | | AUC/D (h*ng/mL) | 79 | 126 |
| Animal Model: | CD-1 mice (male, n=3)[1] | | Dosage: | 20 mg/kg | | Administration: | IP, single dose (Pharmacokinetic Analysis) | | Result: | Had a half-life of 115 min in human plasma, a 2.8-fold increase in stability. |
| [IC 50]
HDAC6: 9.8 nM (IC50); HDAC3: >1 μM (IC50); HDAC8: >1 μM (IC50); HDAC11: >1 μM (IC50); HDAC1: >5 μM (IC50); HDAC2: >5 μM (IC50) | [References]
[1] Nawar N, Bukhari S, Adile AA, et al. Discovery of HDAC6-Selective Inhibitor NN-390 with in Vitro Efficacy in Group 3 Medulloblastoma. J Med Chem. 2022;65(4):3193-3217. DOI:10.1021/acs.jmedchem.1c01585 |
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