2. PROTAC Anti-infection
  3. PROTACs Enterovirus
  4. PROTAC EV-A71 Degrader-1

PROTAC EV-A71 Degrader-1 is a PROTAC degrader targeting EV-A71 3D polymerase, with broad-spectrum activity against a variety of enteroviruses. PROTAC EV-A71 Degrader-1 induces the degradation of EV-A71 3D polymerase through the ubiquitin-proteasome and autophagy-lysosome pathways, and blocks viral replication. PROTAC EV-A71 Degrader-1 protects infected mice from death, alleviates tissue damage, and exhibits safety profiles. PROTAC EV-A71 Degrader-1 can be used in the research of enterovirus infections. (Pink: EV-A71 ligand (HY-19339); Blue: E3 ligase ligand (HY-W012479); Black: linker (HY-W105744)).

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

PROTAC EV-A71 Degrader-1

PROTAC EV-A71 Degrader-1 Chemical Structure

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PROTAC EV-A71 Degrader-1 Related Antibodies

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Description

PROTAC EV-A71 Degrader-1 is a PROTAC degrader targeting EV-A71 3D polymerase, with broad-spectrum activity against a variety of enteroviruses. PROTAC EV-A71 Degrader-1 induces the degradation of EV-A71 3D polymerase through the ubiquitin-proteasome and autophagy-lysosome pathways, and blocks viral replication. PROTAC EV-A71 Degrader-1 protects infected mice from death, alleviates tissue damage, and exhibits safety profiles. PROTAC EV-A71 Degrader-1 can be used in the research of enterovirus infections. (Pink: EV-A71 ligand (HY-19339); Blue: E3 ligase ligand (HY-W012479); Black: linker (HY-W105744))[1].

In Vitro

PROTAC EV-A71 Degrader-1 (compound N-6) (5-10 μM; 12-24 h) specifically degrades EV-A71 3Dpol in HEK293T cells and exhibits strong binding affinity (Kd = 8.08 nM)[1].
PROTAC EV-A71 Degrader-1 (0.001-10 μM; 24-48 h) potently inhibits EV-A71 replication in RD cells, with an EC50 of 0.149 μM, low cytotoxicity (CC50 = 28.073 μM), and a high selectivity index of 188.409[1].
PROTAC EV-A71 Degrader-1 (48 h) exhibits broad-spectrum, nanomolar anti-enterovirus activity against CV-A16, CV-B1, CV-A21, and EV-D68 in RD cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC EV-A71 Degrader-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: RD cells
Concentration: /
Incubation Time: 48 h
Result: Achieved half-maximal effective concentration (EC50) values of 0.078 μM against CV-A16, 0.052 μM against CV-B1, 0.096 μM against CV-A21, and 0.123 μM against EV-D68.
Had EC90 values of 0.192 μM for CV-A16, 0.188 μM for CV-B1, 0.532 μM for CV-A21, and 0.324 μM for EV-D68.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ CL F
Rat[1] 3 mg/kg i.v. 2.11 h 0.08 h 697 ng/mL 321 ng·h/mL 327 ng·h/mL 154 mL/min/kg /
Rat[1] 8 mg/kg i.p. 12.1 h 6.67 h 14.2 ng/mL 222 ng·h/mL 212 ng·h/mL 629 mL/min/kg 24.3 %
In Vivo

PROTAC EV-A71 Degrader-1 (1-10 mg/kg; i.p.; daily; 4 days) protects 60% of EV-A71-infected neonatal KM mice from mortality, reduces virus-induced body weight loss and multiorgan histopathological damage, and exhibits a favorable safety profile[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Kunming (KM) mice (female, 7 days old, EV-A71 infection model via intraperitoneal injection of 1.0 × 107 PFU mouse-adapted EV-A71 GZ-CII strain)[1]
Dosage: 1 mg/kg (mortality protection, body weight loss alleviation, histopathology improvement); 10 mg/kg (safety assessment)
Administration: i.p.; daily; 4 days
Result: Protected 60% of infected mice from mortality.
Significantly alleviated virus-induced body weight loss.
Attenuated histopathological damage in liver, skeletal muscle, kidney, intestine, and brain (including reduced hepatic steatosis, myocyte necrosis, renal tubular atrophy, intestinal vacuolar degeneration, and neuronal pyknosis).
Caused no acute toxicity or body weight reduction in neonatal mice at 10 mg/kg dose.
Molecular Weight

682.92

Formula

C39H50N6O3S
SMILES

N[C@H](CC1=CNC2=C1C=CC=C2)C(NCCCCCCCCCC(NC3=CC=C(NC(NC(C4=CC=C(C(C)(C)C)C=C4)=O)=S)C=C3)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC EV-A71 Degrader-1 Related Classifications

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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.

Keywords:

PROTAC EV-A71 Degrader-1PROTACsEnterovirusRhinovirusHRVHRVsHEVHEVsCV-B1enterovirusesRD cellsautophagy-lysosomal pathwayHEK293T cellsEV-D68CV-A16CV-A21ubiquitin-proteasome pathwayEV-A71 3D polymeraseInhibitorinhibitorinhibit

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