BC 11-38
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.
BC 11-38是PDE11的选择性抑制剂,IC50值为0.28 μM[1]。
PDE11是一个PDE家族。在人类中,PDE11A基因编码4个亚型,水解cAMP和cGMP。PDE11A在骨骼肌、脑、前列腺、睾丸、肾、胰腺、肝脏、淋巴样细胞、垂体和肾上腺中表达[2]。
在H295R人腺癌细胞中,在腺苷酸环化酶激活剂forskolin存在和不存在的情况下,BC11-38显著增加皮质醇的生成和cAMP水平。在H295R细胞中,BC11-38以作用于PDE11的方式提高ATF-1的磷酸化。在包括MDA-MB-231和HeLa细胞在内的几个细胞系中,PDE11A的mRNA含量极低。在MDA-MB-231细胞中,BC11-38不能提高cAMP水平及CREB磷酸化。在HeLa细胞中,BC11-38不影响cAMP水平或CREB磷酸化[2]。在p54nrb/NONOKD细胞中,BC11-38和ACTH联合治疗部分恢复响应于cAMP刺激产生脱氢表雄酮及皮质醇的能力,以及响应于促肾上腺皮质激素刺激产生cAMP的能力[3]。
有一项发明,是关于使用化合物如BC11-38提升肾上腺抑制受试者中的皮质醇水平,如正在进行皮质类固醇给药或长期进行皮质类固醇治疗的受试者[4]。
参考文献:
[1]. Cichero E, D'Ursi P, Moscatelli M, et al. Homology modeling, docking studies and molecular dynamic simulations using graphical processing unit architecture to probe the type-11 phosphodiesterase catalytic site: a computational approach for the rational design of selective inhibitors. Chemical biology & drug design, 2013, 82(6): 718-731.
[2]. Ceyhan O, Birsoy K, Hoffman CS. Identification of biologically active PDE11-selective inhibitors using a yeast-based high-throughput screen. Chemistry & biology, 2012, 19(1): 155-163.
[3]. Lu JY, Sewer MB. p54nrb/NONO Regulates Cyclic AMP-Dependent Glucocorticoid Production by Modulating Phosphodiesterase mRNA Splicing and Degradation. Molecular and cellular biology, 2015, 35(7): 1223-1237.
[4]. Hoffman CS, Ceyhan O. Inhibitors of phosphodiesterase 11 (PDE11): U.S. Patent 9,173,884[P]. 2015-11-3.
Physical Appearance | White solid |
Storage | Store at -20°C |
M.Wt | 304.43 |
Cas No. | 686770-80-9 |
Formula | C15H16N2OS2 |
Solubility | Soluble in DMSO |
Chemical Name | 3-phenyl-2-(propylthio)-6,7-dihydrothieno[3,2-d]pyrimidin-4(3H)-one |
SDF | Download SDF |
Canonical SMILES | O=C1N(C2=CC=CC=C2)C(SCCC)=NC3=C1SCC3 |
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。 |