RJS308
Based on 1 Customer Validation
RJS308 is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 induces ubiquitin-dependent CypA degradation by recruiting the VHL E3 ligase complex, and forms a ternary complex with CypA and VHL/elongin C/elongin B. RJS308 exhibits anti-HIV-1 and anti-HCV activities. RJS308 can be used in studies related to viral infections.
(Pink: Cyclophilin A ligand (HY-173012); Blue: VHL ligand (HY-112078); Black: linker (HY-W123015)).
For research use only. We do not sell to patients.
- Purity: 99.62%
- Formula: C63H75N13O11S
- Molecular Weight:1222.42
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
|
VHL |
CypA |
HIV-1 |
RJS308 binds to recombinant full-length human CypA in SPR binding assays with a KD value of 108 nM, and also binds to N-terminally truncated human CypB with a KD value of 320 nM[1].
RJS308 (0.01-10 μM; 0-6 days) degrades CypA in Jurkat cells[1].
RJS308 (1-5 μM; 48 h) exhibits anti-HIV-1 activity in primary activated human CD4+ T cells, and this activity depends on VHL-mediated CypA degradation[1].
RJS308 (1-5 μM; 48 h) exhibits anti-HCV activity in Huh7 human hepatocellular carcinoma cells, and this activity depends on VHL-mediated CypA degradation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat human T cells
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Concentration:0.01, 0.1, 1, 5, 10 μM
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Incubation Time:0, 1, 2, 3, 4, 5, 6 days
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Result:Almost completely degraded CypA within 24 h at 5 μM.
Caused dose-dependent CypA degradation with a DC50 of 284 nM and a maximum degradation (Dmax) of 98% after 48 h treatment.
Chemical Information
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Appearance Solid
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Molecular Weight 1222.42
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Formula C63H75N13O11S
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Color White to off-white
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SMILES
C[C@@H](C1=CC=C(C2=C(C)N=CS2)C=C1)NC([C@H]3N(C[C@@H](C3)O)C([C@H](C(C)(C)C)NC(CCCCCN4N=NC(C[C@H]5C(N6N[C@@H](CCC6)C(O[C@H](C)C7=CC=C8C(C=C(C=C8)/C=C/CC(N[C@H](C(N5)=O)CC9=CC=C([N+]([O-])=O)C=C9)=O)=N7)=O)=O)=C4)=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (81.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light). 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 (protect from light). 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)
Purity & Documentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 (protect from light). 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 | 0.8180 mL | 4.0902 mL | 8.1805 mL | 20.4512 mL |
| 5 mM | 0.1636 mL | 0.8180 mL | 1.6361 mL | 4.0902 mL | |
| 10 mM | 0.0818 mL | 0.4090 mL | 0.8180 mL | 2.0451 mL | |
| 15 mM | 0.0545 mL | 0.2727 mL | 0.5454 mL | 1.3634 mL | |
| 20 mM | 0.0409 mL | 0.2045 mL | 0.4090 mL | 1.0226 mL | |
| 25 mM | 0.0327 mL | 0.1636 mL | 0.3272 mL | 0.8180 mL | |
| 30 mM | 0.0273 mL | 0.1363 mL | 0.2727 mL | 0.6817 mL | |
| 40 mM | 0.0205 mL | 0.1023 mL | 0.2045 mL | 0.5113 mL | |
| 50 mM | 0.0164 mL | 0.0818 mL | 0.1636 mL | 0.4090 mL | |
| 60 mM | 0.0136 mL | 0.0682 mL | 0.1363 mL | 0.3409 mL | |
| 80 mM | 0.0102 mL | 0.0511 mL | 0.1023 mL | 0.2556 mL |
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