1. PROTAC Immunology/Inflammation Anti-infection
  2. PROTACs Cyclophilin HIV HCV
  3. RJS308 TFA

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)).

For research use only. We do not sell to patients.

RJS308 TFA

RJS308 TFA Chemical Structure

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Based on 1 publication(s) in Google Scholar

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  • Customer Review

Description

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[1]. (Pink: Cyclophilin A ligand (HY-173012); Blue: VHL ligand (HY-112078); Black: linker (HY-W123015)).

In Vitro

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.

Western Blot Analysis[1]

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.
Molecular Weight

1336.44

Formula

C65H76F3N13O13S

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.7483 mL 3.7413 mL 7.4826 mL
5 mM 0.1497 mL 0.7483 mL 1.4965 mL
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
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 (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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
RJS308 TFA
Cat. No.:
HY-173011A
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