CID 755673
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.
CAMKIIα及Akt 的IC50值分别为0.182、0.280、0.227、>10、15.3、20.3、40.5及>50 μM。
CID755673,即苯并二氮杂卓环己醇酮,是第一个鉴定的细胞活性小分子PKD拮抗剂。它抑制PKD1活性,IC50值为182 nM,与对AKT、PLK1、CAK、CAMKIIα、PKD2及PKD3相比,对PKD1具有最高选择性。此外,它的酶抑制作用不与ATP竞争[1]。
体外实验:在基于细胞的试验中,CID755673剂量依赖性地抑制LNCaP细胞中内源性佛波酯诱发的PKD1活化。经报道,它也逆转PKD1的生物学效应,包括IIa类组蛋白去乙酰化酶5核排斥、水泡性口炎、病毒糖蛋白从高尔基体到质膜的运输以及ilimaquinone诱导的高尔基体碎片化。此外,CID755673抑制前列腺癌细胞增殖、细胞迁移及侵袭[1]。
体内实验:发展急性胰腺炎的实验模型,以研究CID755673对体内急性胰腺炎的影响。结果表明,该化合物抑制PKD1/2,因此可显著抵消胰腺炎的坏死和严重程度[2]。
临床试验:到目前为止,还未进行临床试验。
参考文献:
[1]Sharlow ER, Giridhar KV, LaValle CR, Chen J, Leimgruber S, Barrett R, Altamirano KB, Wipf P, Lazo JS and Wang QJ. Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone. J Biol Chem. 2008 Nov. 283(48): 3351246.
[2]Yuan JZ, Liu YN, Tan TY, Guha S, Gukovsky I, Gukovskaya A and Pandol SJ. Protein kinase D regulates cell death pathways in experimental pancreatitis. Front Physiol. 2012 Mar. 3: DOI: 10.3389/fphys.2012.00060.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 217.22 |
Cas No. | 521937-07-5 |
Formula | C12H11NO3 |
Solubility | insoluble in H2O; ≥4.94 mg/mL in EtOH with ultrasonic; ≥5.55 mg/mL in DMSO |
Chemical Name | 7-hydroxy-2,3,4,5-tetrahydro-[1]benzofuro[2,3-c]azepin-1-one |
SDF | Download SDF |
Canonical SMILES | C1CC2=C(C(=O)NC1)OC3=C2C=C(C=C3)O |
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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