N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide
Tubastatin-A
CAS: 1252003-15-8
Molecular Formula: C20H21N3O2
N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide - Names and Identifiers
N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide - Physico-chemical Properties
| Molecular Formula | C20H21N3O2 |
| Molar Mass | 335.4 |
| Density | 1.28±0.1 g/cm3(Predicted) |
| Solubility | DMSO: ≥ 45 mg/mL |
| pKa | 8.95±0.10(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| In vitro study | Tubastatin A selectively acts on all isozymes except HDAC8 and does not contain HDAC8 for ALL subtypes, maintaining over 1000-fold selectivity and approximately 57-fold selectivity for hdac8. 2.5 μm Tubastatin A preferentially induced hyperacetylation of α-tubulin. 10 μm Tubastatin A slightly induced histone acetylation. Tubastatin A 5 μm began to have A protective effect on homocysteine-induced neuronal cell death in A dose-dependent manner, with complete protection at 10 μm. Tubastatin A (10 μm) acts on cholangiocarcinoma cell lines, inducing an increase in acetylated α-tubulin levels, and restoration of primary cilia expression, restoration of primary cilia expression and down-regulation of Hedgehog (Hh) and MAPK signaling pathways, and reduced cell proliferation rate (mean 50%) and infiltration (40%) were associated. Tubastatin A significantly inhibited TNF-α and THP-1 in LPS-stimulated human IL-6 macrophages with IC50 of 272 nM and 712 nM, respectively. Tubastatin A inhibited nitric oxide (NO) secretion in mouse Raw 264.7 macrophages in A dose-dependent manner with an IC50 of 4.2 μm. Tubastatin A selectively acts on all isozymes except HDAC8 and does not contain HDAC8 for all isoforms, maintaining over 1000-fold selectivity and approximately 57-fold selectivity for hdac8. 2.5 μm Tubastatin A preferentially induced hyperacetylation of α-tubulin. 10 μm Tubastatin A slightly induced histone acetylation. Tubastatin A 5 μm began to have A protective effect on homocysteine-induced neuronal cell death in A dose-dependent manner, with complete protection at 10 μm. Tubastatin A (10 μm) acts on cholangiocarcinoma cell lines, inducing an increase in acetylated α-tubulin levels, and restoration of primary cilia expression, restoration of primary cilia expression and down-regulation of Hedgehog (Hh) and MAPK signaling pathways, and reduced cell proliferation rate (mean 50%) and infiltration (40%) were associated. Tubastatin A significantly inhibited TNF-α and THP-1 in LPS-stimulated human IL-6 macrophages with IC50 of 272 nM and 712 nM, respectively. Tubastatin A inhibited nitric oxide (NO) secretion in mouse Raw 264.7 macrophages in A dose-dependent manner with an IC50 of 4.2 μm. |
| In vivo study | Tubastatin A reduces the growth of cholangiocarcinoma in vivo. Tubastatin A(10 mg/kg) treatment of syngeneic rat orthotopic cholangiocarcinoma model induced 6 times lower than the average tumor weight, reduced tumor weight and liver weight and body weight (5 and 5.6 times respectively) the ratio. Tubastatin A treatment significantly reduced the number of PCNA positive cells compared to the control group (34% vs 65%). Tubastat A dose of 30 mg/kg intraperitoneal administration of Freund's complete adjuvant (FCA) induced animal inflammation model, significantly inhibited the mouse paw volume. Tubastat A(30 mg/kg I. P.) treatment of paw tissue of collagen-induced arthritic DBA1 mice significantly reduced clinical score (-70%), and IL-6 expression. Tubastatin A reduces the growth of cholangiocarcinoma in vivo. Tubastatin A(10 mg/kg) treatment of syngeneic rat orthotopic cholangiocarcinoma model induced 6 times lower than the average tumor weight, reduced tumor weight and liver weight and body weight (5 and 5.6 times respectively) the ratio. Tubastatin A treatment significantly reduced the number of PCNA positive cells compared to the control group (34% vs 65%). Tubastat A dose of 30 mg/kg intraperitoneal administration of Freund's complete adjuvant (FCA) induced animal inflammation model, significantly inhibited the mouse paw volume. Tubastat A(30 mg/kg I. P.) treatment of paw tissue of collagen-induced arthritic DBA1 mice significantly reduced clinical score (-70%), and IL-6 expression. |
N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.982 ml | 14.908 ml | 29.815 ml |
| 5 mM | 0.596 ml | 2.982 ml | 5.963 ml |
| 10 mM | 0.298 ml | 1.491 ml | 2.982 ml |
| 5 mM | 0.06 ml | 0.298 ml | 0.596 ml |
Last Update：2024-01-02 23:10:35
N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide - Reference Information
| biological activity | Tubastatin A is an effective, selective HDAC6 inhibitor with an IC50 of 15 nM, which selectively acts on all other isozymes (1000 times) except HDAC8(57 times). Tubastatin A is an effective, selective HDAC6 inhibitor. IC50 in cell-free test is 15 nM, and the selectivity is much higher than all other isozymes (1000 times) except HDAC8(57 times). Tubastatin A can promote autophagy and increase apoptosis. |
| in vitro study | Tubastatin a selectively acts on all isoenzymes except HDAC8, does not contain HDAC8 for all subtypes, maintains a selectivity of more than 1000 times, and has a selectivity of about 57 times for HDAC8. 2.5 μM Tubastatin A preferentially induces high acetylation of α-tubulin. 10 μM Tubastatin A slightly induced histone acetylation. Tubastatin A 5 μM begins to have a protective effect on homocysteine-induced neuronal cell death. This effect is dose-dependent. At 10 μM, complete protection is achieved. Tubastatin A (10 μM) acts on cholangiocarcinoma cell lines to induce an increase in acetylated α-tubulin levels and a recovery of primary cilia expression. The recovery of primary cilia expression is associated with down-regulation of Hedgehog (Hh) and MAPK signaling pathways, as well as a reduction in cell proliferation rate (mean 50%) and infiltration (40%). Tubastatin A significantly inhibited TNF-α and IL-6 on LPS-stimulated human THP-1 macrophages with IC50 of 272 nM and 712 nM respectively. Tubastatin A acts on mouse Raw 264.7 macrophages and inhibits nitric oxide (NO) secretion. This effect is dose-dependent with an IC50 of 4.2 μM. Tubastatin a selectively acts on all isozymes except HDAC8, does not contain HDAC8 for all subtypes, maintaining a selectivity of more than 1000 times and a selectivity of about 57 times for HDAC8. 2.5 μM Tubastatin A preferentially induces high acetylation of α-tubulin. 10 μM Tubastatin A slightly induced histone acetylation. Tubastatin A 5 μM begins to have a protective effect on homocysteine-induced neuronal cell death. This effect is dose-dependent. At 10 μM, complete protection is achieved. Tubastatin A (10 μM) acts on cholangiocarcinoma cell lines to induce an increase in acetylated α-tubulin levels and a recovery of primary cilia expression. The recovery of primary cilia expression is associated with down-regulation of Hedgehog (Hh) and MAPK signaling pathways, as well as a reduction in cell proliferation rate (mean 50%) and infiltration (40%). Tubastatin A significantly inhibited TNF-α and IL-6 on LPS-stimulated human THP-1 macrophages with IC50 of 272 nM and 712 nM respectively. Tubastatin A acts on mouse Raw 264.7 macrophages and inhibits nitric oxide (NO) secretion. This effect is dose-dependent with an IC50 of 4.2 μM. |
| in vivo research | Tubastatin A reduces the growth of cholangiocarcinoma in vivo. Tubastatin A(10 mg/kg) was used to treat the orthotopic cholangiocarcinoma model of syngeneic rats, which induced 6 times lower than the average tumor weight and reduced the ratio of tumor weight to liver weight and body weight (5 and 5.6 times respectively). Compared with the control group, Tubastatin A significantly reduced the amount of PCNA positive cells (34% vs 65%). Tubastat A was injected intraperitoneally at a dose of 30 mg/kg to give Freund's complete adjuvant (FCA) to induce inflammation in animal model, which significantly inhibited the volume of mouse claws. Tubastat A(30 mg/kg intraperitoneal injection) treated claw tissue of collagen-induced arthritis DBA1 mice, significantly reducing clinical score (70%) and IL-6 expression. Tubastatin a reduces the growth of cholangiocarcinoma in vivo. Tubastatin A(10 mg/kg) was used to treat the orthotopic cholangiocarcinoma model of syngeneic rats, which induced 6 times lower than the average tumor weight and reduced the ratio of tumor weight to liver weight and body weight (5 and 5.6 times respectively). Compared with the control group, Tubastatin A significantly reduced the amount of PCNA positive cells (34% vs 65%). Tubastat A was injected intraperitoneally at a dose of 30 mg/kg to give Freund's complete adjuvant (FCA) to induce inflammation in animal model, which significantly inhibited the volume of mouse claws. Tubastat A(30 mg/kg intraperitoneal injection) treated claw tissue of collagen-induced arthritis DBA1 mice, significantly reducing clinical score (70%) and IL-6 expression. |
| target | TargetValue HDAC6 (Cell-free say) 15 nM |
| Target | Value |
| HDAC6 (Cell-free assay) | 15 nM |
Last Update：2024-04-09 20:52:54
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Product Name: Tubastatin-A Visit Supplier Webpage Request for quotationCAS: 1252003-15-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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