2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. 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)).

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

NEP162

NEP162 Chemical Structure

CAS No. : 3031840-36-2

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NEP162 Related Antibodies

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Description

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))[1].

IC50 & Target[1]

BRD4

 

In Vitro

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.

NEP162 Related Antibodies

Western Blot Analysis[1]

Cell Line: GID4 WT and siRNA knockdown SW480 cells
Concentration: 2 μM
Incubation Time: 18 h
Result: BRD4 remained stable in the GID4 knockdown cells.

Cell Proliferation Assay[1]

Cell Line: U2OS cells
Concentration: 2 μM
Incubation Time: 0, 24, 48 and 72 h
Result: Notably inhibited U2OS cell proliferation in a dose-dependent manner at 48 and 72 h.

Apoptosis Analysis[1]

Cell Line: U2OS cells
Concentration: 2 μM
Incubation Time: 24 h
Result: Induced a prominent increase in apoptosis in U2OS cells.
In Vivo

NEP162 (5-15 mg/kg, i.p., every other day for 14 days) inhibits tumor growth in mice xenograft tumor model with U2OS cells[1].

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

Animal Model: Xenograft tumor model with U2OS cells established in 5-week-old female BALB/c nude mice[1]
Dosage: 5, 10 and 15 mg/kg
Administration: Intraperitoneal injection (i.p.), every other day for 14 days
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.
Molecular Weight

926.57

Formula

C50H56ClN11O3S
CAS No.
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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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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NEP162 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:

NEP1623031840-36-2NEP 162NEP-162PROTACsEpigenetic Reader DomainApoptosisUbiquitin–proteasome systemGID4Anti-canerXenograft tumor modelU2OS cellsInhibitorinhibitorinhibit

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