PYZD-4409
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.
PYZD-4409是一种新型的泛素激活酶E1小分子抑制剂，其IC50值为20 μM[1]。
泛素激活酶E1参与蛋白质降解的第一步，利用ATP使泛素分子腺苷酸化，并将其传送到酶E2。实验表明，泛素化途径在原代白血病细胞中较活跃。因此，抑制E1可以成为恶性血液病治疗的一个靶标。基于吡唑烷药效基团，从化合物库中筛选出PTSD-4409。其IC50值（20 μM）由无细胞酶试验评估。在培养的K562白血病细胞中，PYZD-4409也可以抑制E1。PYZD-4409引起白血病、骨髓瘤和实体瘤细胞系死亡。在克隆的生长试验中，相对于正常造血细胞，PYZD-4409抑制AML细胞生长。E1在蛋白质降解中起着重要作用，抑制E1可以增加细胞周期蛋白D3和p53的表达[1]。
参考文献：
[1] G. Wei Xu, Mohsin Ali, Tabitha E. Wood et al. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. Blood. 2010, 115(11): 2251-2259.
| Physical Appearance | Brown solid |
| Storage | Store at -20°C |
| M.Wt | 351.67 |
| Cas No. | 423148-78-1 |
| Formula | C14H7ClFN3O5 |
| Solubility | Soluble in DMSO |
| Chemical Name | (4E)-1-(3-chloro-4-fluorophenyl)-4-[(5-nitrofuran-2-yl)methylidene]pyrazolidine-3,5-dione |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=C(C=C1N2C(=O)C(=CC3=CC=C(O3)[N+](=O)[O-])C(=O)N2)Cl)F |
| 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 | PYZD-4409是泛素激活酶（E1）的小分子抑制剂，其IC50值为20 μM。 | |||||
| 靶点 | E1 | |||||
| IC50 | 20 μM | |||||
化学结构
