NEP162
NEP162 is a BRD4 PROTAC degrader with DC50s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc. (Pink: BRD4 ligand : (HY-78695), Blue: E3 ligase Ligand (HY-D2259), BLACK: Linker, E3 ligase ligand-linker conjugate (HY-174997)).
(Pink: BRD4 ligand (HY-78695); Blue: Ligands for E3 Ligase ligand (HY-D2259); Black: linker).
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- CAS. Nr.: 3031840-36-2
- Formel: C50H56ClN11O3S
- Molecular Weight:926.57
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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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Chemical Information
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Biologische Aktivität
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BRD4 |
NEP162 (2 μM, 12-18 h) degrades BRD4 via GID4 and UPS in SW480, siRNA knockdown SW480 and GID4 WT cells[1]. NEP162 (2 μM, 0-72 h) inhibits U2OS cells proliferation and induce apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GID4 WT and siRNA knockdown SW480 cells
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Concentration:2 μM
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Incubation Time:18 h
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Result:BRD4 remained stable in the GID4 knockdown cells.
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Cell Line:U2OS cells
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Concentration:2 μM
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Incubation Time:0, 24, 48 and 72 h
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Result:Notably inhibited U2OS cell proliferation in a dose-dependent manner at 48 and 72 h.
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Cell Line:U2OS cells
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Concentration:2 μM
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Incubation Time:24 h
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Result:Induced a prominent increase in apoptosis in U2OS cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Xenograft tumor model with U2OS cells established in 5-week-old female BALB/c nude mice[1]
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Dosage:5, 10 and 15 mg/kg
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Administration:Intraperitoneal injection (i.p.), every other day for 14 days
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Result:Weekly at 5 mg/kg and notably suppressed tumor growth at 10 and 15 mg/kg.
Did not affect mouse body weight, and hematoxylin and eosin (H&E) staining of vital organs revealed no apparent physiological damage.
Notably increased TUNEL-positive apoptotic cells and reduced Ki67-positive proliferative cells in a dose-dependent manner.
Reduced the BRD4 levels in tumor tissues.
Chemical Information
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CAS. Nr. 3031840-36-2
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Molecular Weight 926.57
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Formel C50H56ClN11O3S
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SMILES
O=C(N[C@@H]1CC[C@H](C2=NC(C=CC(OCCCN3CCN(C(C[C@H]4C5=NN=C(C)N5C(SC(C)=C6C)=C6C(C7=CC=C(Cl)C=C7)=N4)=O)CC3)=C8)=C8N2)CC1)CNCC(N9)=CC%10=C9C=CC=C%10
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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)
NEP162 Related Classifications
HY-174996 Related Classifications
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