IMB-301
目录号 : GC61820
IMB-301 是一种 HIV-1 辅助蛋白 Vif 降解 hA3G 的拮抗剂。IMB-301 通过抑制 hA3G-Vif 相互作用，来抑制 Vif 降解 hA3G。IMB-301 具有抗 HIV-1 活性。
Cas No.:64009-84-3
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
IMB-301 is a HIV-1 auxilins Vif degradation hA3G antagonist. IMB-301 inhibits hA3G-Vif interactions to inhibit Vif degradations hA3G. IMB-301 has anti-HIV-1 activity[1].
IMB-301 can effectively inhibit the combination of Vif and hA3G[1].IMB 301 can be by inhibiting Vif to inhibit Vif degradations hA3G with hA3G binding specificities[1].
References:
[1]. Zhou, Jinming, et al. Applications of the IMB-301 in antiviral drugs is prepared. CN108261413A.
| Cas No. | 64009-84-3 | SDF | |
| Canonical SMILES | FC1=CC=C(OCCC(C2=CC=C(Cl)C=C2Cl)CN3C=CN=C3)C=C1 | ||
| 分子式 | C19H17Cl2FN2O | 分子量 | 379.26 |
| 溶解度 | DMSO : 100 mg/mL (263.67 mM; Need ultrasonic) | 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 | 2.6367 mL | 13.1836 mL | 26.3671 mL |
| 5 mM | 0.5273 mL | 2.6367 mL | 5.2734 mL |
| 10 mM | 0.2637 mL | 1.3184 mL | 2.6367 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。
Identification of small molecule compounds targeting the interaction of HIV-1 Vif and human APOBEC3G by virtual screening and biological evaluation
Sci Rep 2018 May 23;8(1):8067.PMID:29795228DOI:PMC5966509
Human APOBEC3G (hA3G) is a restriction factor that inhibits human immunodeficiency 1 virus (HIV-1) replication. The virally encoded protein Vif binds to hA3G and induces its degradation, thereby counteracting the antiviral activity of hA3G. Vif-mediated hA3G degradation clearly represents a potential target for anti-HIV drug development. Herein, we have performed virtual screening to discover small molecule inhibitors that target the binding interface of the Vif/hA3G complex. Subsequent biochemical studies have led to the identification of a small molecule inhibitor, IMB-301 that binds to hA3G, interrupts the hA3G-Vif interaction and inhibits Vif-mediated degradation of hA3G. As a result, IMB-301 strongly inhibits HIV-1 replication in a hA3G-dependent manner. Our study further demonstrates the feasibility of inhibiting HIV replication by abrogating the Vif-hA3G interaction with small molecules.