2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. NEP162

NEP162 是一种 BRD4 PROTAC 降解剂，在 SW480 和 U2OS 细胞中的 DC50 值分别为 1.2 和 1.6 μM。NEP162 具有抗增殖活性，能有效抑制肿瘤生长并诱导细胞凋亡 (apoptosis)。NEP162 可用于研究骨肉瘤、结直肠癌和非小细胞肺癌等癌症。 (粉色：BRD4 配体 (HY-78695)，蓝色：E3 连接酶配体 (HY-D2259)，黑色：Linker，E3 连接酶配体-Linker 复合物 (HY-174997))。

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NEP162

NEP162 Chemical Structure

CAS No. : 3031840-36-2

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NEP162 相关抗体

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

NEP162 (2 μM, 12-18 h) 在 SW480，siRNA 敲除的 SW480 细胞和 GID WT 细胞中通过 GID4 和 UPS 降解了 BRD4[1]。 NEP162 (2 μM, 0-72 h) 抑制 U2OS 细胞增殖，诱导了凋亡和集落形成[1]。

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

NEP162 相关抗体:

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.
体内研究
(In Vivo)

NEP162 (5-15 mg/kg, i.p., 2 天 1 次, 共 14 天) 在使用 U2OS 细胞构建的小鼠异种移植瘤模型中抑制了肿瘤生长[1]。

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.
分子量

926.57

Formula

C50H56ClN11O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NEP162 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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

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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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目录号：
HY-174996
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