FC-14369
Based on 1 Customer Validation
FC-14369 is a PROTAC degrader targeting the HIV-1 Nef protein, with a DC50 value of 160 nM. Through its bifunctional structure, FC-14369 binds to Nef and the Cereblon E3 ubiquitin ligase, induces Nef ubiquitination and proteasomal degradation, restores the expression of cell-surface CD4 and MHC-I, and inhibits HIV-1 replication. FC-14369 can be used in research on HIV infection and AIDS. FC-14369 is applicable to studies related to HIV-1 infection.
(Pink: HIV-1 Nef ligand (HY-171862); Blue: Cereblon ligand (HY-14658); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 97.85%
- CAS 番号: 3066894-28-5
- 分子式: C42H34ClF3N8O7
- 分子量:855.22
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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生物活性
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HIV-1 |
FC-14369 binds directly to recombinant HIV-1 Nef (NL4-3 variant) with high affinity (Kd = 6.5 nM) and to the CRBN thalidomide-binding domain with nanomolar affinity, forming stable interactions with both proteins in vitro[1].
FC-14369 (3 μM; 24 h/48 h) induces robust degradation of Nef-eGFP in CEM/Nef-eGFP T cells, restoring cell surface CD4 and MHC-I expression by ~70% after 24 h, and reducing Nef protein levels to <5% of control after 48 h[1].
FC-14369 (48 h) induces Nef degradation in CEM/Nef-eGFP T cells with a DC50 of 160 nM after 48 h, and targeted degradation occurs without cytotoxicity at active concentrations (CC50 = 3.0 μM)[1].
FC-14369 (48 h) inhibits HIV-1 infectivity in TZM-bl reporter cells with an IC50 of 250 nM after 48 h, without inducing cytotoxicity[1].
FC-14369 (1 μM; 4 days) potently inhibits Nef-dependent enhancement of HIV-1 replication in activated human PBMCs after 4 days, with minimal cytotoxicity (viability ≥90% relative to control)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Doxycycline-inducible CEM/Nef-eGFP human T cells
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Concentration:Multi-point concentrations
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Incubation Time:48 h
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Result:Induced Nef degradation with a DC50 (concentration producing 50% degradation of Nef) value of 160 nM.
Showed a CC50 (concentration producing 50% cytotoxicity) value of approximately 3.0 μM in parallel cell viability assays.
化学情報
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CAS 番号 3066894-28-5
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性状 Solid
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分子量 855.22
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分子式 C42H34ClF3N8O7
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Color Light yellow to green yellow
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SMILES
O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCCNC(COC4=CC=C(CCC5=C(O)N(C6=NC7=C(N6)C=CC(Cl)=C7)N=C5C8=CC=C(C(F)(F)F)C=C8)C=C4)=O)=CC=C3)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶剤 & 溶解度
DMSO : 100 mg/mL (116.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1693 mL | 5.8464 mL | 11.6929 mL | 29.2322 mL |
| 5 mM | 0.2339 mL | 1.1693 mL | 2.3386 mL | 5.8464 mL | |
| 10 mM | 0.1169 mL | 0.5846 mL | 1.1693 mL | 2.9232 mL | |
| 15 mM | 0.0780 mL | 0.3898 mL | 0.7795 mL | 1.9488 mL | |
| 20 mM | 0.0585 mL | 0.2923 mL | 0.5846 mL | 1.4616 mL | |
| 25 mM | 0.0468 mL | 0.2339 mL | 0.4677 mL | 1.1693 mL | |
| 30 mM | 0.0390 mL | 0.1949 mL | 0.3898 mL | 0.9744 mL | |
| 40 mM | 0.0292 mL | 0.1462 mL | 0.2923 mL | 0.7308 mL | |
| 50 mM | 0.0234 mL | 0.1169 mL | 0.2339 mL | 0.5846 mL | |
| 60 mM | 0.0195 mL | 0.0974 mL | 0.1949 mL | 0.4872 mL | |
| 80 mM | 0.0146 mL | 0.0731 mL | 0.1462 mL | 0.3654 mL | |
| 100 mM | 0.0117 mL | 0.0585 mL | 0.1169 mL | 0.2923 mL |