LMK 235
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:细胞毒性IC50(对A2780细胞为490 nM、对 A2780 CisR细胞为320 nM);HDAC抑制活性(对A2780细胞为650 nM、对A2780CisR细胞为320 nM);
组蛋白去乙酰化酶(EC 3.5.1.98,HDAC)是一种从组蛋白的ε-N-乙酰赖氨酸上脱去乙酰基(O=C-CH3)的酶,以使组蛋白将DNA包裹得更紧。组蛋白去乙酰化酶抑制剂(HDIS)作为一种情绪稳定剂和抗癫痫剂,在精神病学和神经病学具有较长的使用历史,例如戊酸。近年来,HDIS主要作为缓解或治疗神经退行性疾病的药物来研究。
体外试验:在pan-HDAC实验中,LMK235显示出和伏立诺他(vorinostat)相似的HDACs抑制效果,但LMK235提高了对人肿瘤细胞系A2780、Cal27、Kyse510和MDA-MB231的细胞毒活性。LMK235对HDAC4和HDAC5的抑制活性在纳摩尔级别,而伏立诺他(vorinostat)和TSA对HDAC4和HDAC5的抑制活性在更高的微摩尔级别。和伏立诺他(vorinostat)相比,LMK235具有新的HDAC异构体选择特性,对HDAC4和HDAC5 具有优先选择性[1]。
体内试验:在老鼠体内试验中,通过细胞增殖和平板克隆形成试验证明LMK235和Cytarabine起协同抑制作用。这些结果表明体内RNAi筛选活性是可行的。HDAC4可能是增强抗白血病药物疗效的重要靶点[2]。
临床试验:目前LMK235的临床前研究正在进行中,还没有进行临床试验。
参考文献:
[1] Marek L, Hamacher A, Hansen FK, Kuna K, Gohlke H, Kassack MU, Kurz T. Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. J Med Chem. 2013;56(2):427-36.
[2] Stephanie Lettermann, Konstantin Agelopoulos, Christian Rohde, Beate Lindtner, Linda Marek, Georg Hempel, Matthias Stelljes, Wolfgang E. Berdel, Thomas Kurz and Carsten Müller-Tidow. In Vivo RNAi Screening Identifies HDAC4 As a Mediator Of Chemoresistance In Acute Myeloid Leukemia. 55th ASH Annual Meeting and Exposition (2013) (https://ash.confex.com/ash/2013/webprogram/Paper60036.html)
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 294.35 |
Cas No. | 1418033-25-6 |
Formula | C15H22N2O4 |
Solubility | insoluble in H2O; ≥53.8 mg/mL in EtOH with ultrasonic; ≥9.95 mg/mL in DMSO |
Chemical Name | N-((6-(hydroxyamino)-6-oxohexyl)oxy)-3,5-dimethylbenzamide |
SDF | Download SDF |
Canonical SMILES | CC1=CC(C)=CC(C(NOCCCCCC(NO)=O)=O)=C1 |
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。 |
质量控制和MSDS
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