2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. 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。

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NN-390 Chemical Structure

NN-390 Chemical Structure

CAS No. : 2490284-25-6

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NN-390 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

IC50 & TargetHDAC

HDAC2

>5 μM (IC50)

HDAC1

>5 μM (IC50)

HDAC6

9.8 nM (IC50)

HDAC3

>1 μM (IC50)

HDAC8

>1 μM (IC50)

HDAC11

>1 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Fibroblast IC50
12.4 μM
Compound: 5a; NN-390
Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
Fibroblast IC50
8.8 μM
Compound: 5a; NN-390
Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
HUVEC IC50
10.1 μM
Compound: 5a; NN-390
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
MM1.S IC50
1.38 μM
Compound: 5a; NN-390
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
MV4-11 IC50
1.19 μM
Compound: 5a; NN-390
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
NSC IC50
5.76 μM
Compound: 5a; NN-390
Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NN-390 相关抗体:

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.
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

MCE 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.
分子量

420.38

Formula

C17H16F4N2O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NN-390 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NN-3902490284-25-6NN390NN 390HDACHistone deacetylasesGroup 3 MBAMLMV4-11 cellsHD-MB03 cellsPediatric brain tumorReversibilityPlasma StabilityPermeabilitySelectivityInhibitorinhibitorinhibit

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