MS436
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.
MS436是BRD4的一个有效的、选择性小分子抑制剂,Ki值<0.085 μM。对BRD1和BRD2抑制的Ki值为0.34 μM。BRD4在基因转录过程中发挥作用,是一种针对癌症和炎症的药物靶标。它有两个溴化识别结构域。MS436是一个diazobenzene化合物,是从SAR研究中被设计出来的,且具有较高的选择性。体外荧光各向异性分析显示MS436对BRD1的亲和力大约有BRD2的10倍高。MS436通过一组水介导相互作用的方式结合BRD4,这也是亲和力的分子基础。MS436对CBP-BRD也有结合活性。在RAW264.7细胞中,MS436可阻止NF-κB介导的NO的产生,也可阻止LPS诱导的促炎细胞因子白介素IL6的表达[1]。
参考文献:
[1] Zhang G, Plotnikov AN, Rusinova E, Shen T, Morohashi K, Joshua J, Zeng L, Mujtaba S, Ohlmeyer M, Zhou MM. Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J Med Chem. 2013 Nov 27;56(22):9251-64.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 383.42 |
Cas No. | 1395084-25-9 |
Formula | C18H17N5O3S |
Solubility | insoluble in H2O; insoluble in EtOH; ≥19.15 mg/mL in DMSO |
Chemical Name | 4-[(2Z)-2-(2-amino-5-methyl-4-oxocyclohexa-2,5-dien-1-ylidene)hydrazinyl]-N-pyridin-2-ylbenzenesulfonamide |
SDF | Download SDF |
Canonical SMILES | CC1=CC(=NNC2=CC=C(C=C2)S(=O)(=O)NC3=CC=CC=N3)C(=CC1=O)N |
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 | MS436是BRD4的一个有效的、选择性小分子抑制剂,Ki值<0.085 μM。对BRD1和BRD2抑制的Ki值为0.34 μM。 | |||||
靶点 | BrD1 | BrD2 | ||||
IC50 | <0.085 μM | 0.34 μM |
质量控制和MSDS
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