NN-390 是一种有效的选择性HDAC6抑制剂，其IC50为 9.8 nM。NN-390 可穿透血脑屏障。NN-390 在转移性第 3 组成神经管细胞瘤中显示出研究潜力。

NN-390 is a potent and selective HDAC6 inhibitor, with an IC 50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) [1].

NN-390 exhibits cellular potency with IC 50 values of 1.19 μM in MV4-11 cells and 1.38 μM in MM.1S cells while having minimal effects on noncancerous counterparts ( IC 50 >50 μM in MRC-9) [1]. NN-390 (72 h) strongly decreases proliferation in HD-MB03 cells, with an IC 50 of 0.13 μM, and significantly impairs self-renewal of BTIC-enriched HD-MB03s [1]. NN-390 (0-2 μM, 1 h) markedly increases acetylation of α-tubulin and minimally changes acetylated histone H3 [1]. NN-390 (6 h) results in acetylation of α-tubulin from concentrations as low as 0.1 μM (0-0.2 μM), and dose-dependent increases in acetylation of α-tubulin (0-0.2 μM) [1]. NN-390 (0-2 μM, 24 h) promotes cancer cells apoptosis in MV4-11 cells [1]. Immunofluorescence Cell Line: HeLa cells [1] Concentration: 0, 0.1, 0.25, 1, 2 μM Incubation Time: 1 h Result: Markedly increased acetylation of α-tubulin and minimally changed acetylated histone H3. Western Blot Analysis Cell Line: AML (MV4-11) cells [1] Concentration: 0, 0.1, 0.5, 1, 5 μM Incubation Time: 6 h Result: Resulted in acetylation of α-tubulin from concentrations as low as 0.1 μM and with limited acetylation of histone H3 at only the highest concentration of 5 μM. Western Blot Analysis Cell Line: Group 3 MB (HD-MB03) cells [1] Concentration: 0, 0.053, 0.106, 0.158, 0.211 μM Incubation Time: 6 h Result: Dose-dependent increased in acetylation of α-tubulin from the lowest concentration of 53 nM, with no observable change in acetylation of off-target histone H3 up to 211 nM. Apoptosis Analysis Cell Line: MV4-11 cells [1] Concentration: 0, 0.25, 0.75, 1, 2 μM Incubation Time: 24 h Result: Promoted cancer cells apoptosis, 39% of cancer cells were undergoing late-stage apoptosis after 18 h at 2 μM, and 11% of cells were in the late apoptosis stage at 0.25 μM.

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 t 1/2 (h) 1.05 1.90 C max (ng/mL) 493 750 AUC last (h*ng/mL) 1576 2523 AUC lnf (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.

2490284-25-6

C17H16F4N2O4S

420.38

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years