NN-390
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).
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- No. CAS: 2490284-25-6
- Fòrmula: C17H16F4N2O4S
- Peso molecular:420.38
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Fibroblast | IC50 |
12.4 μM
Compound: 5a; NN-390
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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
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[PMID: 35119267] |
| Fibroblast | IC50 |
8.8 μM
Compound: 5a; NN-390
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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
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[PMID: 35119267] |
| HUVEC | IC50 |
10.1 μM
Compound: 5a; NN-390
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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
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[PMID: 35119267] |
| MM1.S | IC50 |
1.38 μM
Compound: 5a; NN-390
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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
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[PMID: 35119267] |
| MV4-11 | IC50 |
1.19 μM
Compound: 5a; NN-390
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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
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[PMID: 35119267] |
| NSC | IC50 |
5.76 μM
Compound: 5a; NN-390
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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
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[PMID: 35119267] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells[1]
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Concentration:0, 0.1, 0.25, 1, 2 μM
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Incubation Time:1 h
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Result:Markedly increased acetylation of α-tubulin and minimally changed acetylated histone H3.
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Cell Line:AML (MV4-11) cells[1]
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Concentration:0, 0.1, 0.5, 1, 5 μM
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Incubation Time:6 h
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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.
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Cell Line:Group 3 MB (HD-MB03) cells[1]
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Concentration:0, 0.053, 0.106, 0.158, 0.211 μM
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Incubation Time:6 h
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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.
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Cell Line:MV4-11 cells[1]
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Concentration:0, 0.25, 0.75, 1, 2 μM
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Incubation Time:24 h
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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 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice (male, n=3)[1]
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Dosage:20 mg/kg
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Administration:IP, single dose (Pharmacokinetic Analysis)
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Result:Had a half-life of 115 min in human plasma, a 2.8-fold increase in stability.
Chemical Information
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No. CAS 2490284-25-6
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Peso molecular 420.38
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Fòrmula C17H16F4N2O4S
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SMILES
O=C(NO)C1=CC=C(CN(C(C)C)S(=O)(C2=CC(F)=C(F)C(F)=C2F)=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NN-390 Related Classifications
HY-143877 Related Classifications
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