JV8
JV8 is a BRD4 PROTAC degrader with a target Kd of 0.65 μM. JV8 preferentially induces BRD4 degradation in the cytoplasm via the ubiquitin-proteasome system. JV8 exhibits dose-dependent and time-dependent BRD4 degradation activity and is capable of inducing cell apoptosis. JV8 inhibits tumor growth in a dose-dependent manner and induces BRD4 degradation in tumor tissues in vivo. JV8 can be used in research related to various cancers such as breast cancer and pancreatic cancer.
(Pink: BRD4 ligand (HY-78695); Blue: Ligands for E3 Ligase ligand (HY-173435); Black: linker (HY-33366)).
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- CAS. Nr.: 2841716-61-6
- Formel: C50H62ClN9O8S2
- Molecular Weight:1016.67
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
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BRD4 0.65 μM (Kd) |
JV8 (1-100 nM; 24 h) dose-dependently degrades cytoplasmic and total BRD4 in 4T1 cells via the ubiquitin-proteasome system, with minimal nuclear BRD4 degradation at concentrations up to 100 nM, and induces more apoptosis than JQ1(HY-13030)[1].
JV8 (1-100 nM; 24 h) dose-dependently reduces JQ1-NR fluorescence signals in 4T1 cells, correlating with decreased cytoplasmic BRD4 levels[1].
JV8 binds to purified BRD4 (BD1 and BD2) protein with a Kd of 0.65 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:4T1 cells
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Concentration:1, 5, 10, 50, 100 nM
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Incubation Time:24 h
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Result:Induced dose-dependent decreases in BRD4 levels in total 4T1 cells and cytoplasm, with minimal BRD4 degradation in the nucleus even at 100 nM.
Co-treatment with MG132 (HY-13259) blocked JV8-mediated BRD4 degradation, confirming dependence on the ubiquitin-proteasome system.
JV8 (5-10 mg/kg; i.p.; once every 2 days for a total of 5 administrations) induces dose-dependent tumor suppression in subcutaneous 4T1 tumors of BALB/c mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (subcutaneous 4T1/HeLa/KPC/Hepa 1-6/CT26 tumor model, tumors grown to ~100-150 mm3 prior to treatment)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single injection
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Result:Induced complete degradation of BRD4 protein in subcutaneous 4T1, HeLa, KPC, Hepa 1-6, and CT26 tumors in BALB/c mice.
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Animal Model:BALB/c (subcutaneous 4T1 tumor model, tumors grown prior to treatment initiation)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:i.p.; every other day; 5 total doses
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Result:Exhibited a dose-dependent tumor suppression effect.
Reduced tumor volume and weight significantly in mice treated with 10 mg/kg compared to controls.
Lowered BRD4 levels in tumors from 10 mg/kg treated mice by approximately 4.11-fold compared to PBS-treated mice.
Caused no significant body weight loss in treated groups.
Chemical Information
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CAS. Nr. 2841716-61-6
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Molecular Weight 1016.67
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Formel C50H62ClN9O8S2
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SMILES
O=C(NCCOCCOCCOCC(N[C@H](C(C)(C)C)C(N1[C@H](C(N[C@@H](C)C2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)=O)C[C@@H]4N=C(C5=CC=C(Cl)C=C5)C6=C(SC(C)=C6C)N7C4=NN=C7C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
JV8 Related Classifications
HY-173433 Related Classifications
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