上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
NN-390
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 Chemical Structure
CAS No. : 2490284-25-6
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
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].
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| IC50 & TargetHDAC |
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HDAC2
>5 μM (IC50)
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HDAC1
>5 μM (IC50)
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HDAC6
9.8 nM (IC50)
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HDAC3
>1 μM (IC50)
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HDAC8
>1 μM (IC50)
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HDAC11
>1 μM (IC50)
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体外研究
(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)[1].
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[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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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体内研究
(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 |
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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.
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