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

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.

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of RJS308:

RJS308 Related Antibodies

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  • Biological Activity

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Description

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

IC50 & Target[1]

VHL

 

CypA

 

HIV-1

 

In Vitro

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.

RJS308 Related Antibodies

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

1222.42

Formula

C63H75N13O11S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8180 mL 4.0902 mL 8.1805 mL
5 mM 0.1636 mL 0.8180 mL 1.6361 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 (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.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
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 (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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RJS308 Related Classifications

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.

Keywords:

RJS308RJS 308RJS-308PROTACsCyclophilinHIVHCVHuman immunodeficiency virusHepatitis C virusubiquitinJurkat human T cellsTHP-1 human monocytic cellscyclophilinHuh7 human hepatoma cellsCypAprimary human cellsHIV-1VHL E3 ligase complexInhibitorinhibitorinhibit

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