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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| B421846-1ml |
1ml |
现货 ![]() |
|
| 英文别名 | Benzamide,4-(acetylamino)-N-(2-amino-4-fluorophenyl)- |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | BRD3308 |
| 生化机理 | BRD3308 是一种强效、高选择性的 HDAC3 抑制剂,对 HDAC3、HDAC1 和 HDAC2 的 IC50 分别为 54 nM、1.26 μM 和 1.34 μM。BRD3308 可激活 HIV-1 的转录。BRD3308 可抑制炎性细胞因子(糖脂毒性应激)诱导的胰腺 β 细胞凋亡,并增加功能性胰岛素的释放。 |
| 储存温度 | 避光,-80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
Information BRD3308 is a potant and highly selective inhibitor ofHDAC3with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release. Targets HDAC3 (Cell-free assay); HDAC1 (Cell-free assay); HDAC2 (Cell-free assay) 54 nM; 1.26 μM; 1.34 μM In vitro BRD3308 is a derivative of the ortho-aminoanilide HDAC inhibitor CI-994 and is developed to be highly selective for inhibition of HDAC3 with an IC50 value that is 23-fold lower for HDAC3 than for HDAC1 or 22. HDAC3 selective inhibition induces expression of HIV and exposure to BRD3308 allows the recovery of latent HIV-1 from patient cells. In vivo Selective inhibition of HDAC3 by BRD3308 prevents diabetes onset in female NOD mice. HDAC3 treatment in vivo prevents pancreatic islet infiltration and protects β-cells from apoptosis. β-cell proliferation is increased in animals treated with BRD3308. HDAC3 treatment in vivo prevents white adipose tissue infiltration in NOD mice. Cell Research(from reference) Cell lines:2D10 cells, J89 cells, THP89 cells, J-Lat 6.3 cells Concentrations:5 μM, 10 μM, 15 μM, 30 μM Incubation Time:6 h, 12 h, 18 h, 24 h |
| 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 | 4-acetamido-N-(2-amino-4-fluorophenyl)benzamide |
| INCHI | InChI=1S/C15H14FN3O2/c1-9(20)18-12-5-2-10(3-6-12)15(21)19-14-7-4-11(16)8-13(14)17/h2-8H,17H2,1H3,(H,18,20)(H,19,21) |
| InChi Key | RRJDFENBXIEAPD-UHFFFAOYSA-N |
| Canonical SMILES | CC(=O)NC1=CC=C(C=C1)C(=O)NC2=C(C=C(C=C2)F)N |
| Isomeric SMILES | CC(=O)NC1=CC=C(C=C1)C(=O)NC2=C(C=C(C=C2)F)N |
| PubChem CID | 72734382 |
| 分子量 | 287.29 |
| 敏感性 | 对光线敏感 |
|---|---|
| 分子量 | 287.290 g/mol |
| XLogP3 | 1.400 |
| 氢键供体数Hydrogen Bond Donor Count | 3 |
| 氢键受体数Hydrogen Bond Acceptor Count | 4 |
| 可旋转键计数Rotatable Bond Count | 3 |
| 精确质量Exact Mass | 287.107 Da |
| 单同位素质量Monoisotopic Mass | 287.107 Da |
| 拓扑极表面积Topological Polar Surface Area | 84.200 Ų |
| 重原子数Heavy Atom Count | 21 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 383.000 |
| 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 |
| RIDADR | NONHforallmodesoftransport |
|---|
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Light yellow liquid) | pass |
| Record the entire process by video | Conform |