DASA-58
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.
DASA-58是丙酮酸激酶M2（PKM2）的选择性活化剂，AC90值为680 nM，AC50值为38 nM [1]。
在癌症中，PKM2的调节性能可以改变糖代谢。PKM2和含磷酸酪氨酸蛋白的相互作用抑制了酶的活性，因此加强了糖酵解的代谢[1]。
Flag-PKM1和Flag-PKM2均在A549-PKM1/KD和A549-PKM2/KD细胞中表达。内源性PKM2表达被降低。经过DMSO的处理，导致A549-PKM2/kd和A549-PKM1/kd细胞裂解物中丙酮酸激酶的活性增加233 ± 27％。DASA-58没有增加A549-PKM1/kd细胞中的丙酮酸激酶的活性，但它导致了A549-PKM2/kd细胞裂解液中丙酮酸激酶活性增加248 ± 21％。在细胞中，0-100 μM 的DASA-58会剂量依赖性地活化PKM2，EC50值为19.6 μM[1]。
TEPP-46是另一个PKM2活化剂。在A549移植瘤中，急性口服剂量150 mg/kg 的TEPP-46能最大程度激活PKM2。在H1299异种移植瘤中，50 mg/kg 剂量的TEPP-46，连续5天，每天两次，使肿瘤完全含有四聚体PKM2。在载体处理的小鼠异种移植物中，发现少量的PKM2四聚体[1]。
参考文献：
[1]. Anastasiou D, Yu Y, Israelsen WJ, et al. Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nature chemical biology, 2012, 8(10): 839-847.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 453.53 |
| Cas No. | 1203494-49-8 |
| Formula | C19H23N3O6S2 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥127.2 mg/mL in DMSO |
| Chemical Name | 3-((4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)sulfonyl)-1,4-diazepan-1-yl)sulfonyl)aniline |
| SDF | Download SDF |
| Canonical SMILES | O=S(N1CCN(S(C2=CC(OCCO3)=C3C=C2)(=O)=O)CCC1)(C4=CC=CC(N)=C4)=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
- 批次:
化学结构
