NN-390,2490284-25-6

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NN-390

CAS No. : 2490284-25-6

MCE 国际站：NN-390

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：HDAC

In Vitro: NN-390 exhibits cellular potency with IC₅₀ values of 1.19 μM in MV4-11 cells and 1.38 μM in MM.1S cells while having minimal effects on noncancerous counterparts (IC₅₀ > 50 μM in MRC-9).
NN-390 (72 h) strongly decreases proliferation in HD-MB03 cells, with an IC₅₀ of 0.13 μM, and significantly impairs self-renewal of BTIC-enriched HD-MB03s.
NN-390 (0-2 μM, 1 h) markedly increases acetylation of α-tubulin and minimally changes acetylated histone H3.
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).
NN-390 (0-2 μM, 24 h) promotes cancer cells apoptosis in MV4-11 cells.

In Vivo: NN-390 (male CD-1 mice, 20 mg/kg, IP, single dose) increases plasma stability.
NN-390 can improve PAMPA (parallel artificial membrane permeability assay)-BBB (blood-brain barrier) score.
Pharmacokinetic Parameters of NN-390 in male male CD-1 mice.

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

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