| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T421055-1ml |
1ml |
现货  |
|
| 别名 | N-羟基-4-[(1,2,3,4-四氢-2-甲基-5H-吡啶并[4,3-b]吲哚-5-基)甲基]苯甲酰胺 | 图巴他汀A |
|---|---|
| 英文别名 | 1252003-15-8 | 1252003-15-8 (free base) | Calcium oxide, Reagent Grade | Tubastatin A Trifluoroacetate | BRD-K00627859-001-01-5 | DTXSID701318079 | NCGC00263606-15 | potasium hydroxide | Tubastatin A | Benzamide, N-hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl- |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Tubastatin A |
| 生化机理 | Tubastatin A 是一种强效的选择性 HDAC6 抑制剂，在无细胞试验中的 IC50 为 15 nM。它对所有其他同工酶都有选择性（1000 倍），但 HDAC8（57 倍）除外。Tubastatin A 可促进自噬并增加细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 组蛋白去乙酰化酶 1 抑制剂；组蛋白去乙酰化酶 6 抑制剂；组蛋白去乙酰化酶 8 抑制剂 |
| 产品介绍 |
Tubastatin A 是一种有效的，选择性HDAC6抑制剂，无细胞试验中IC50为15 nM，选择性远高于所有其他同工酶(1000倍)除了HDAC8(57倍)。Tubastatin A 可促进自噬并增加凋亡。 Information Tubastatin A is a potent and selectiveHDAC6inhibitor withIC50of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotesautophagyand increasesapoptosis. Targets HDAC6 (Cell-free assay) 15 nM In vitro Tubastatin A is selective at all isozymes except HDAC8 and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. Tubastatin A preferentially induces α-tubulin hyperacetylation at 2.5 μM. Slight induction of histone hyperacetylation is seen for Tubastatin A at 10 μM. Tubastatin A displays dose-dependent protection against homocysteic acid-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM. Tubastatin A (10 μM) induces an increase in acetylated-α-tubulin levels and the restoration of primary cilia expression in the cholangiocarcinoma cell lines (18-fold); and the restoration of primary cilia correlated with downregulated Hedgehog (Hh) and MAPK signaling pathways, as well as decreased cell proliferation rates (in average by 50%) and invasion (by 40%). Tubastatin A shows significant inhibition of TNF-α and IL-6 in LPS stimulated human THP-1 macrophages with an IC50 of 272 nM and 712 nM. Tubastatin A inhibits nitric oxide (NO) secretion in murine Raw 264.7 macrophages dose depenndently with an IC50 of 4.2 μM. In vivo Tubastatin A reduces the growth of cholangiocarcinoma in vivo. Tubastatin A (10 mg/kg) induces a 6-fold lower mean tumor weights in syngeneic rat orthotopic model of cholangiocarcinoma, and reduction of the ratios of tumor weight to liver weight and body weight (5- and 5.6-fold, respectively), as well as a greater frequency of ciliated cholangiocytes compared with controls (29% vs 1.4%). Tubastatin A significantly decreases the amount of PCNA-positive cells in the treated tumors compared with vehicle controls (34% vs 65%). Tubastat A shows significant inhibition of paw volume at 30 mg/kg i.p. in a Freund\'s complete adjuvant (FCA) induced animal model of inflammation. Tubastat A (30 mg/kg i.p.) significant attenuates clinical scores (~ 70%), and IL-6 expression in paw tissues of collagen induced arthritis DBA1 mouse. Cell Research(from reference) Cell lines：Human cholangiocarcinoma cell lines HuCCT-1 Concentrations：~10 μM Incubation Time：21 days Application： Tubastatin A hydrochloride may be used in HDAC6-mediated cell signaling studies. |
| IC50 | HDAC6, IC50: 15 nM |
|---|---|
| ALogP | 3.081 |
| HBD Count | 1 |
| Rotatable Bond | 3 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IUPAC Name | N-hydroxy-4-[(2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl)methyl]benzamide |
| INCHI | InChI=1S/C20H21N3O2/c1-22-11-10-19-17(13-22)16-4-2-3-5-18(16)23(19)12-14-6-8-15(9-7-14)20(24)21-25/h2-9,25H,10-13H2,1H3,(H,21,24) |
| InChi Key | GOVYBPLHWIEHEJ-UHFFFAOYSA-N |
| Canonical SMILES | CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO |
| Isomeric SMILES | CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO |
| 关联CAS | 1252003-15-8 |
| PubChem CID | 49850262 |
| MeSH Entry Terms | tubastatin A |
| 分子量 | 335.4 |
| DMSO(mg / mL) Max Solubility | 67 |
|---|---|
| DMSO(mM) Max Solubility | 199.76 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 335.400 g/mol |
| XLogP3 | 2.300 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 3 |
| 可旋转键计数Rotatable Bond Count | 3 |
| 精确质量Exact Mass | 335.163 Da |
| 单同位素质量Monoisotopic Mass | 335.163 Da |
| 拓扑极表面积Topological Polar Surface Area | 57.500 Ų |
| 重原子数Heavy Atom Count | 25 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 478.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Light-yellow Liquid) | Pass |
| Record the entire process by video | Conform |
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