BG45
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:289 nM
组蛋白去乙酰化酶(HDACs)是治疗各种癌症的一个新型分子靶点,包括多发性骨髓瘤(MM).临床前研究表明,多种HDAC抑制剂具有显着的抗肿瘤活性.然而,HDAC抑制剂具有广谱的HDAC抑制效应,引起相关毒性,使其临床应用受限.BG45是一种新型的以及选择性的HDAC3小分子抑制剂.
体外:据报道,BG45属于I型HDAC抑制剂,相对于HDAC1和HDAC2,选择性地作用于HDAC3.与HDAC3敲减数据一致,BG45呈剂量依赖性地显著抑制MM细胞生长.此外,BG45有效地抑制源于患者的MM细胞生长,而不会影响源于健康人的PBMCs[1].
体内:BG45呈剂量依赖性地显著抑制MM肿瘤生长.例如,在对照组与BG45 15 mg/kg组\对照组与BG45 50 mg/kg组以及BG45 15 mg/kg组与BG45 50 mg/kg组中,于第22天,可以观察到显著差异.此外,50 mg/kg BG45与Bortezomib联合用药可进一步增加单一用药的疗效.上述结果表明,BG45在体内具有抗MM活性[1].
临床试验:到目前为止,BG45还处于临床前开发阶段.
参考文献:
[1] Minami J, Suzuki R, Mazitschek R, Gorgun G, Ghosh B, Cirstea D, Hu Y, Mimura N, Ohguchi H, Cottini F, Jakubikova J, Munshi NC, Haggarty SJ, Richardson PG, Hideshima T, Anderson KC. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. Leukemia. 2014 Mar;28(3):680-9.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 214.22 |
Cas No. | 926259-99-6 |
Formula | C11H10N4O |
Solubility | Soluble in DMSO |
Chemical Name | (Z)-N-(2-aminophenyl)pyrazine-2-carbimidic acid |
SDF | Download SDF |
Canonical SMILES | NC1=CC=CC=C1/N=C(O)/C2=CN=CC=N2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |