2. Apoptosis Stem Cell/Wnt Neuronal Signaling Epigenetics Cell Cycle/DNA Damage
  3. Apoptosis Notch PARP Caspase
  4. NEURL1B-IN-1

NEURL1B-IN-1 是一种 NEURL1B 降解剂，其 Kd 为 46.2 nM。NEURL1B-IN-1 可结合 NEURL1B NHR2 结构域内的 Arg422，触发其自身泛素化及蛋白酶体降解，破坏其与 DLL1 的相互作用，减弱 Notch 信号通路。NEURL1B-IN-1 可诱导肝癌细胞发生细胞周期阻滞、凋亡 (apoptosis)，并抑制其迁移。NEURL1B-IN-1 可用于肝细胞癌的相关研究。

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NEURL1B-IN-1

NEURL1B-IN-1 Chemical Structure

CAS No. : 3068938-30-4

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NEURL1B-IN-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NEURL1B-IN-1 is a NEURL1B degrader with a Kd value of 46.2 nM. NEURL1B-IN-1 binds to Arg422 within the NHR2 domain of NEURL1B, triggers its autoubiquitination and proteasomal degradation, disrupts its interaction with DLL1, and attenuates the Notch signaling pathway. NEURL1B-IN-1 induces cell cycle arrest and apoptosis, and inhibits migration of hepatocellular carcinoma cells. NEURL1B-IN-1 is applicable to research related to hepatocellular carcinoma[1].

体外研究
(In Vitro)

NEURL1B-IN-1 (compound 1) 可强效抑制 HepG2、Huh-7 和 SK-Hep-1 肝癌细胞的活力[1]。
NEURL1B-IN-1 (7.5 μM) 可强烈抑制 SK-Hep-1 (抑制率 93.6%) 和 Huh-7 (抑制率 83.9%) 肝癌细胞的集落形成[1]。
NEURL1B-IN-1 (7.5 μM) 可显著降低 SK-Hep-1 (降低 83.9%) 和 Huh-7 (降低 66.3%) 肝癌细胞的 DNA 合成[1]。
NEURL1B-IN-1 (2.5-7.5 μM) 可在 SK-Hep-1 和 Huh-7 肝癌细胞中诱导 G2/M 期细胞周期阻滞和凋亡，抑制细胞迁移与侵袭[1]。

NEURL1B-IN-1 (2.5-7.5 μM) 可下调 SK-Hep-1 和 Huh-7 肝癌细胞中 CyclinB1 及磷酸化 cdc2 (Tyr17) 的蛋白表达水平[1]。
NEURL1B-IN-1 (2.5-7.5 μM) 可上调 SK-Hep-1 和 Huh-7 肝癌细胞中 cleaved-PARP-1 及 Bax 蛋白的表达[1]。
NEURL1B-IN-1 (7.5 μM) 通过改变 SK-Hep-1 和 Huh-7 肝癌细胞中 E-cadherin、Vimentin 及 Slug 的蛋白表达来调控上皮间质转化 (EMT)[1]。

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

NEURL1B-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: HepG2, Huh-7, SK-Hep-1 and THLE-2 cells
Concentration: /
Incubation Time: /
Result: Potently inhibited the viability of HepG2, Huh-7, and SK-Hep-1 hepatocellular carcinoma cells with IC50 values of 5.6, 4.8, and 4.6 μM respectively, and had cytotoxicity to normal THLE-2 liver cells with a CC50 of 5.5 μM
体内研究
(In Vivo)

NEURL1B-IN-1 (30-60 mg/kg; 腹腔注射，每日 1 次，连续 60 天) 可抑制 SK-Hep-1 异种移植裸鼠的肝癌肿瘤生长[1]。

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

Animal Model: BALB/c nude mice treated SK-Hep-1 cells (4-week-old)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: i.p.; daily; 60 days
Result: Reduced tumor volume by 57% and tumor weight by 37% on day 60 at 30 mg/kg.
Reduced tumor volume by 69% and tumor weight by 69% on day 60 at 60 mg/kg.
Caused no significant changes in mouse body weight or liver histopathology at either dose.
Reduced proliferation marker Ki67 expression, increased apoptosis marker cleaved caspase-3 expression, downregulated NEURL1B, Notch components NICD and HES1, and EMT markers α-SMA and Vimentin, while upregulating DLL1 in tumor tissues at 60 mg/kg.
分子量

478.62

Formula

C30H38O5
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

NEURL1B-IN-1 相关分类

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Keywords:

NEURL1B-IN-13068938-30-4ApoptosisNotchPARPCaspasepoly ADP ribose polymeraseArg422liver cancer cellsNotch signalingHepG2Huh-7NHR2 domainNEURL1Bhepatocellular carcinomaxenograft nude miceDLL1Inhibitorinhibitorinhibit

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