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Art. -Nr.: HY-174996

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NEP162

Name: NEP162
Brand: MedChemExpress
SKU: HY-174996
Price: 810.00 USD
Availability: InStock
Rating: 5 (1 reviews)

NEP162 is a BRD4 PROTAC degrader based on the E3 ubiquitin ligase GID4, with DC₅₀ values of 1.2 μM and 1.6 μM in SW480 and U2OS cells, respectively, and a K_d value of 0.13 µM for GID4. NEP162 bridges the E3 ligase GID4 and BRD4 to form a ternary complex, promotes polyubiquitination and subsequent degradation of BRD4 via the ubiquitin-proteasome system, reduces the proliferation capacity of tumor cells and induces apoptosis. NEP162 can be used for research on cancers such as osteosarcoma, colorectal cancer and non-small cell lung cancer.
(Pink: BRD4 ligand (HY-78695); Blue: GID4 ligand (HY-D2259); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3031840-36-2
Formel: C₅₀H₅₆ClN₁₁O₃S
Molecular Weight:926.57

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (285 KB)

NEP162 Chemical Structure

CAS. Nr.: 3031840-36-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

NEP162 is a BRD4 PROTAC degrader based on the E3 ubiquitin ligase GID4, with DC₅₀ values of 1.2 μM and 1.6 μM in SW480 and U2OS cells, respectively, and a K_d value of 0.13 µM for GID4. NEP162 bridges the E3 ligase GID4 and BRD4 to form a ternary complex, promotes polyubiquitination and subsequent degradation of BRD4 via the ubiquitin-proteasome system, reduces the proliferation capacity of tumor cells and induces apoptosis. NEP162 can be used for research on cancers such as osteosarcoma, colorectal cancer and non-small cell lung cancer^[1]. (Pink: BRD4 ligand (HY-78695); Blue: GID4 ligand (HY-D2259); Black: linker).

IC₅₀ & Target

^[1]

BRD4

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Cellular Effect

Cell Line	Type	Value	Description	References
SW480	DC₅₀	1.2 μM	Half-maximal degradation of endogenous BRD4 in human SW480 colon cancer cells after 18 h treatment, measured via immunoblotting assay. Half-maximal degradation of endogenous BRD4 in human SW480 colon cancer cells after 18 h treatment, measured via immunoblotting assay.	40295770
U2OS	DC₅₀	1.6 μM	Half-maximal degradation of endogenous BRD4 in human U2OS osteosarcoma cells after 18 h treatment, measured via immunoblotting assay. Half-maximal degradation of endogenous BRD4 in human U2OS osteosarcoma cells after 18 h treatment, measured via immunoblotting assay.	40295770

In Vitro

Anti-cancerApoptosisOthers

Anti-cancer

NEP162 (0.1-20 μM; 6-24 h) induces dose- and time-dependent degradation of BRD4 protein in U2OS and SW480 cells, while it shows no obvious degradation effect in H3122, H520 and HEC-1-A cells^[1].

Anti-cancer

Apoptosis

NEP162 (0.5-5 μM; 24 h-7 days) inhibits cell viability, induces apoptosis, and significantly suppresses colony formation in U2OS cells^[1].

Others

NEP162 (31.25 nM-3 µM; 180 s association, 180 s dissociation) binds directly to purified recombinant GID4 protein, with a K_d value of 0.13 µM. It induces the formation of a stable ternary complex between purified recombinant GID4 and BRD4BD1 protein, with a K_d value of 0.30 µM^[1].
NEP162 (2 μM; 18 h) loses its ability to degrade BRD4 protein in GID4-knockdown SW480 cells^[1].
NEP162 (0.2-10 μM; 18 h) promotes the polyubiquitination of BRD4 in U2OS cells that are pre-transfected to express Flag-BRD4 and HA-Ub and pre-treated with MG132 (HY-13259), and it exerts a BRD2-degrading effect without degrading BRD3 protein^[1].

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

Western Blot Analysis^[1]

Cell Line:

U2OS and SW480 cells
Concentration:

0.1, 0.2, 0.5, 1, 2, 5, 10, 20 μM
Incubation Time:

6, 12, 18, 24 h
Result:

Decreased endogenous BRD4 protein levels in a dose-dependent manner.
Significantly reduced BRD4 protein levels over time, especially at 18 and 24 hours.

Western Blot Analysis^[1]

Cell Line:

U2OS cells
Concentration:

0.2, 0.5, 1, 2, 5, 10 μM
Incubation Time:

18 h
Result:

Reduced BRD2 protein levels, but did not alter BRD3 protein expression levels.
Significantly increased the polyubiquitination levels of BRD4.

Cell Viability Assay^[1]

Cell Line:

U2OS cells
Concentration:

0.5, 2, 5 μM
Incubation Time:

24, 48, 72 h
Result:

Significantly inhibited cell viability and proliferation in a dose- and time-dependent manner.

Cell Proliferation Assay^[1]

Cell Line:

U2OS cells
Concentration:

2 μM
Incubation Time:

24 h
Result:

Significantly reduced the percentage of EdU-positive cells, effectively inhibiting cell proliferation.

Immunofluorescence^[1]

Cell Line:

U2OS cells
Concentration:

2 μM
Incubation Time:

24 h
Result:

Significantly increased the percentage of TUNEL-positive cells, inducing tumor cell apoptosis.

Cell Proliferation Assay^[1]

Cell Line:

U2OS cells
Concentration:

2 μM
Incubation Time:

7 days
Result:

Significantly inhibited the colony-forming ability of cells and reduced the number of colonies.

Real Time qPCR^[1]

Cell Line:

U2OS cells
Concentration:

2 μM
Incubation Time:

18 h
Result:

Had no significant effect on the mRNA transcription levels of BRD2, BRD3, and BRD4.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_last	AUC_inf
Mice^[1]	10 mg/kg	i.p.	1.76 h	0.83 h	2.68 μM	6.68 μM·h	6.96 μM·h

In Vivo

Anti-cancerApoptosis

Anti-cancer

Apoptosis

NEP162 (5-15 mg/kg; i.p.; once every other day; treatment for 14 days) exerts effects of inhibiting tumor growth, inducing apoptosis in tumor tissues and reducing intratumoral BRD4 protein levels in U2OS xenograft mice^[1].

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

Animal Model:

BALB/c nude mice were injected subcutaneously with 5×10⁶ U2OS cells^[1]
Dosage:

5 mg/kg; 10 mg/kg; 15 mg/kg
Administration:

i.p.; every other day; 14 days
Result:

Showed modest tumor growth inhibition at 5 mg/kg.
Notably suppressed tumor growth at 10 mg/kg and 15 mg/kg, with near-complete inhibition at 15 mg/kg.
Increased TUNEL-positive apoptotic cells and reduced Ki67-positive proliferative cells in a dose-dependent manner.
Markedly reduced BRD4 levels in tumor tissues at 10 mg/kg and 15 mg/kg.
Did not affect mouse body weight.
Showed no apparent physiological damage to vital organs via H&E staining.

Related Protocols :

Chemical Information

CAS. Nr. 3031840-36-2
Molecular Weight 926.57
Formel C₅₀H₅₆ClN₁₁O₃S
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Li Y, et al. Design of PROTACs utilizing the E3 ligase GID4 for targeted protein degradation. Nature structural & molecular biology. 2025 Sep;32(9):1825-1837. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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NEP162

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