RJS308 TFA
Based on 1 Customer Validation
RJS308 TFA is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 TFA 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 TFA exhibits anti-HIV-1 and anti-HCV activities. RJS308 TFA can be used in studies related to viral infections.
(Pink: Cyclophilin A ligand (HY-173012); Blue: VHL ligand (HY-112078); Black: linker (HY-W123015)).
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: 98.36%
- 分子式: C65H76F3N13O13S
- 分子量:1336.44
-
保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
生物活性
RJS308 TFA 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) TFA degrades CypA in Jurkat cells[1].
RJS308 (1-5 μM; 48 h) TFA 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) TFA 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.
-
Cell Line:Jurkat human T cells
-
Concentration:0.01, 0.1, 1, 5, 10 μM
-
Incubation Time:0, 1, 2, 3, 4, 5, 6 days
-
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.
化学情報
-
性状 Solid
-
分子量 1336.44
-
分子式 C65H76F3N13O13S
-
Color White to off-white
-
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.OC(C(F)(F)F)=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 100 mg/mL (74.83 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and light). 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
-
データシート (279 KB)
-
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)
-
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 (sealed storage, away from moisture and 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 | 0.7483 mL | 3.7413 mL | 7.4826 mL | 18.7064 mL |
| 5 mM | 0.1497 mL | 0.7483 mL | 1.4965 mL | 3.7413 mL | |
| 10 mM | 0.0748 mL | 0.3741 mL | 0.7483 mL | 1.8706 mL | |
| 15 mM | 0.0499 mL | 0.2494 mL | 0.4988 mL | 1.2471 mL | |
| 20 mM | 0.0374 mL | 0.1871 mL | 0.3741 mL | 0.9353 mL | |
| 25 mM | 0.0299 mL | 0.1497 mL | 0.2993 mL | 0.7483 mL | |
| 30 mM | 0.0249 mL | 0.1247 mL | 0.2494 mL | 0.6235 mL | |
| 40 mM | 0.0187 mL | 0.0935 mL | 0.1871 mL | 0.4677 mL | |
| 50 mM | 0.0150 mL | 0.0748 mL | 0.1497 mL | 0.3741 mL | |
| 60 mM | 0.0125 mL | 0.0624 mL | 0.1247 mL | 0.3118 mL |