country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-174996

Copy Link Print Information

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).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 3031840-36-2
화학식: C₅₀H₅₆ClN₁₁O₃S
분자량:926.57

보관:

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

Data Sheet (272 KB)

NEP162 Chemical Structure

CAS No.: 3031840-36-2

사이즈

가격

재고

수량

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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]. (Pink: BRD4 ligand (HY-78695); Blue: Ligands for E3 Ligase ligand (HY-D2259); Black: linker).

IC₅₀ & Target^[1]

BRD4

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

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.

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.

Chemical Information

CAS No. 3031840-36-2
분자량 926.57
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 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)

References

[1]. Li Y, et al. Design of PROTACs utilizing the E3 ligase GID4 for targeted protein degradation. Nat Struct Mol Biol. 2025 Apr 28. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Keywords

MOQ

Minimum order quantity

100 mg

견적 받기 해외재고보유

Other size

견적 받기

Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

NEP162

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

NEP162 Related Classifications

HY-174996 Related Classifications