Droxinostat
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.
Droxinostat是一种选择性的HDAC3、HDAC6和HDAC8抑制剂,IC50值分别为16.9 ± 5.0 μM、2.47 ± 1.09 μM和1.46 ± 0.11 μM[1]。
组蛋白去乙酰化酶(HDACs)是一种酶,负责核心组蛋白上赖氨酸残基的去乙酰化,在控制染色质重组和转录激活中具有举足轻重的作用。据报道,HDACs控制多个非组蛋白的乙酰化和激活状态,包括热休克蛋白90(Hsp90),它是真菌毒力和抗真菌抗性一个重要的分子伴侣。多个HDACs已被鉴定到,HDAC1到HDAC10均在恶性细胞中表达,提醒HDAC的抑制剂是癌症治疗的靶标[2] [3]。
Droxinostat是一种选择性的HDAC抑制剂,不同于抑制的pan-HDACi TSA,其抑制所有检测的HDAC。在PPC-1前列腺癌细胞系中,droxinostat在50 μM/L浓度时选择性地抑制HDAC3、HDAC6和HDAC8的活性,使细胞对死亡配体更敏感[1]。在雄激素依赖性CaP细胞中,droxinostat选择性地抑制HDACs,下调c-FLP的表达,从而导致细胞凋亡[4]。
参考文献:
[1]. Wood, T.E., et al., Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands. Mol Cancer Ther, 2010. 9(1): p. 246-56.
[2]. Lamoth, F., P.R. Juvvadi, and W.J. Steinbach, Histone deacetylase inhibition as an alternative strategy against invasive aspergillosis. Front Microbiol, 2015. 6: p. 96.
[3]. Mackmull, M.T., et al., Histone deacetylase inhibitors cause the selective depletion of bromodomain containing proteins. Mol Cell Proteomics, 2015.
[4]. McCourt, C., et al., Elevation of c-FLIP in castrate-resistant prostate cancer antagonizes therapeutic response to androgen receptor-targeted therapy. Clin Cancer Res, 2012. 18(14): p. 3822-33.
- 1.Huang Y, Yang W, et al. "Droxinostat sensitizes human colon cancer cells to apoptotic cell death via induction of oxidative stress." Cell Mol Biol Lett. 2018 Jul 28;23:34. PMID:30065760
- 2.Bagnall NH, Hines BM, et al. "Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. PMID:28110187
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 243.69 |
Cas No. | 99873-43-5 |
Formula | C11H14ClNO3 |
Solubility | insoluble in H2O; ≥102.8 mg/mL in EtOH; ≥11.35 mg/mL in DMSO |
Chemical Name | 4-(4-chloro-2-methylphenoxy)-N-hydroxybutanamide |
SDF | Download SDF |
Canonical SMILES | CC1=C(C=CC(=C1)Cl)OCCCC(=O)NO |
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。 |
描述 | Droxinostat是一种选择性的HDAC抑制剂,作用于HDACs 6和8,IC50值分别为2.47 μM和1.46 μM。 | |||||
靶点 | HDAC8 | HDAC6 | HDAC3 | HDAC1 | HDAC2 | |
IC50 | 1.46 μM | 2.47 μM | 16.9 μM | >20 μM | >20 μM |