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).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 97.85%
- CAS No.: 3066894-28-5
- 화학식: C42H34ClF3N8O7
- 분자량:855.22
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보관:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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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.
Chemical Information
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CAS No. 3066894-28-5
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Appearance Solid
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분자량 855.22
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
용액&용해도
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
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 |
FC-14369 Related Classifications
HY-171860 Related Classifications
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