A2ti-1
目录号 : GC60546
A2ti-1是选择性的，高亲和力的膜联蛋白A2/S100A10异四聚体(A2t)抑制剂，IC50为24μM。A2ti-1特异性破坏A2和S100A10之间的蛋白质相互作用。A2ti-1可防止人乳头瘤病毒16型(HPV16)感染。
Cas No.:570390-00-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
A2ti-1 is a selective and high-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 24 μM[1]. A2ti-1 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-1 prevents human papillomavirus type 16 (HPV16) infection[2].
A2ti-1 (compound 1 b) is an annexin A2-S100A10 protein-protein interaction blocker[1]. A2ti-1 (100 μM; for 72 hours) reduces HPV16 PsV infection of HeLa cells in a dose-dependent manner[2]. A2ti-1 (10, 25, 50, 75, 100 μM; 24 hours) significantly reduces CFDA-SE-labelled HPV16 PsV entry into HeLa cells in a dose-dependent manner[2]. Cell Viability Assay[2] Cell Line: HeLa cells
[1]. Tummala R K Reddy, et al.Three-dimensional Pharmacophore Design and Biochemical Screening Identifies Substituted 1,2,4-triazoles as Inhibitors of the Annexin A2-S100A10 Protein Interaction. ChemMedChem. 2012 Aug;7(8):1435-46. [2]. Andrew W Woodham, et al. Small Molecule Inhibitors of the Annexin A2 Heterotetramer Prevent Human Papillomavirus Type 16 Infection. J Antimicrob Chemother. 2015;70(6):1686-90.
| Cas No. | 570390-00-0 | SDF | |
| Canonical SMILES | O=C(N)CSC1=NN=C(COC2=CC=CC=C2C)N1C3=CC=CC=C3CC | ||
| 分子式 | C20H22N4O2S | 分子量 | 382.48 |
| 溶解度 | DMSO: 250 mg/mL (653.63 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6145 mL | 13.0726 mL | 26.1452 mL |
| 5 mM | 0.5229 mL | 2.6145 mL | 5.229 mL |
| 10 mM | 0.2615 mL | 1.3073 mL | 2.6145 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Pseudorabies Virus Regulates the Extracellular Translocation of Annexin A2 To Promote Its Proliferation
J Virol 2023 Mar 30;97(3):e0154522.PMID:36786600DOI:PMC10062141
Pseudorabies virus (PRV) infection causes enormous economic losses to the pork industry and severe health consequences in many hosts. Annexin A2 (ANXA2) is a membrane-associated protein with various intracellular functions associated with many viral infections. However, the role of ANXA2 in alphaherpesvirus replication is still not explored. In the present study, we identified the interaction between ANXA2 and PRV US3. The deficiency of ANXA2 significantly restricted PRV proliferation. PRV infection or US3 overexpression led to ANXA2 extracellular translocation. Furthermore, we confirmed that PRV or US3 could lead to the phosphorylation of the Tyr23 ANXA2 and Tyr419 Src kinase, which was associated with the ANXA2 cell surface transposition. US3 can also bind to Src in an ANXA2-independent manner and enhance the interaction between Src and ANXA2. Additionally, inhibitors targeting ANXA2 (A2ti-1) or Src (PP2) could remarkably inhibit PRV propagation in vitro and protect mice from PRV infection in vivo. Collectively, our findings broaden our understanding of the molecular mechanisms of ANXA2 in alphaherpesvirus pathogenicity and suggest that ANXA2 is a potential therapeutic target for treating alphaherpesvirus-induced infectious diseases. IMPORTANCE PRV belongs to the alphaherpesvirus and has recently re-emerged in China, causing severe economic losses. Recent studies also indicate that PRV may pose a potential public health challenge. ANXA2 is a multifunctional calcium- and lipid-binding protein implicated in immune function, multiple human diseases, and viral infection. Herein, we found that ANXA2 was essential to PRV efficient proliferation. PRV infection resulted in the extracellular translocation of ANXA2 through phosphorylation of ANXA2 and Src. ANXA2 and Src formed a complex with PRV US3. Importantly, inhibitors targeting ANXA2 or Src prevented PRV infection in vitro and in vivo. Therefore, our studies reveal a novel strategy by which alphaherpesvirus modifies ANXA2 to promote its replication and highlight ANXA2 as a target in developing novel promising antivirus agents in viral therapy.