BRD3308

HDAC3 选择性抑制剂
  • 10mM in DMSO
有货

库存信息

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B421846-1ml
1ml 现货 Stock Image
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Compound libraries (12326)

基本描述

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 

关联靶点(人)

HDAC1 Tclin 组蛋白去乙酰化酶1(Histone deacetylase 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC2 Tclin 组蛋白去乙酰化酶2(Histone deacetylase 2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC3 Tclin 组蛋白去乙酰化酶3(Histone deacetylase 3) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC8 Tclin Histone deacetylase 8 (4516 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC2 Tclin Histone deacetylase 2 (3971 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC3 Tclin Histone deacetylase 3 (3654 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC4 Tclin Histone deacetylase 4 (2328 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC9 Tclin Histone deacetylase 9 (708 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC7 Tclin Histone deacetylase 7 (1047 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点(其它种属)

Hdac1 Histone deacetylase 1 (93 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac5 Histone deacetylase 5 (5 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

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

化学和物理性质

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

安全和危险性(GHS)

RIDADR NONHforallmodesoftransport

质量标准

Concentration(Compounding value) 9.0-11.0(mmol/L)
Appearance(Light yellow liquid) pass
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

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