2. Autophagy Metabolic Enzyme/Protease
  3. p62 E1/E2/E3 Enzyme
  4. Antitumor agent-81

Antitumor agent-81 

目录号: HY-151799 纯度: 98.62%
COA 产品使用指南

摩尔计算器

Antitumor agent-81 (化合物 5 a) 是一种低细胞毒性的 P62-RNF168 激动剂，能促进 P62 与 RNF168 的相互作用。Antitumor agent-81 诱导 RNF168 介导的 H2A 泛素化减少，并损害同源重组介导的 DNA 修复。Antitumor agent-81 还能以剂量依赖的方式抑制小鼠异种移植肿瘤的生长。

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Antitumor agent-81 Chemical Structure

Antitumor agent-81 Chemical Structure

CAS No. : 2765180-17-2

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规格 价格 是否有货 数量
1 mg ￥1670
In-stock
5 mg ￥3850
In-stock
10 mg ￥5780
In-stock
50 mg   询价  
100 mg   询价  

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Antitumor agent-81 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antitumor agent-81 (compound 5a) is a low cytotoxic P62-RNF168 agonist that promotes the interaction of P62 with RNF168. Antitumor agent-81 induces a decrease in RNF168-mediated H2A ubiquitination and impairs homologous recombination-mediated DNA repair. Antitumor agent-81 also inhibits mice xenograft tumor growth in a dose-dependent manner[1].

体外研究
(In Vitro)

Antitumor agent-81 (0-20 µM; 72 h) exhibits antiproliferative activity in cells of the most common cancer types[1].
Antitumor agent-81 (1, 2, 5 µM; 24 h) compromises HR (homologous recombination)-mediated DSB repair in HCT-116 cells[1].
Antitumor agent-81 tethers the interaction between P62 and RNF168 in HCT-116 cells[1].
Antitumor agent-81 inhibits the catalytic activity of RNF168 and RNF168 E3 ligase activity in HCT-116 cells[1].

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

Antitumor agent-81 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A549, HCT-116, A375, HeLa, HepG2, MCF-7, MDA-MB-231, MGC-803, U2OS and MCF-10A cells
Concentration: 0-20 µM
Incubation Time: 72 h
Result: Inhibited A549, HCT-116, A375, HeLa, HepG2, MCF-7, MDA-MB-231, MGC-803, U2OS and MCF-10A cells, with IC50 values of 1.18, 0.36, 1.93, 2.48, 19.61, 2.79, 1.17, 1.88, 3.64 and 6.98, respectively.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 1, 2, 5 µM
Incubation Time: 24 h
Result: Induced a G2/M arrest but no significant accumulation of sub-G1 phase.
Compromised both HR(homologous recombination)- and NHEJ (non-homologous end joining)- mediated DSB repair in a dose-dependent manner, but HR was the more severely impacted process.
体内研究
(In Vivo)

Antitumor agent-81 (5, 10 mg/kg; i.p.; single every 3 days for 22 days) suppresses tumor volumes in a dose-dependent manner in mice[1].
1.19 Pharmacokinetic Parameters of Antitumor agent-81 in Female BALB/c nude mice[1].

Dose T1/2 (h) Cmax (ng/mL) AUC0-t (hng/mL) CL ((mL/h)/kg)
IP (5 mg/kg) 16.17 26.10 215.69 19647.83
IP (10 mg/kg) 31.00 39.87 408.18 16554.30
IP (20 mg/kg) 22.10 52.23 1003.58 14669.81

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

Animal Model: Female BALB/c nude mice (xenograft tumor model)[1].
Dosage: 5, 10 mg/kg
Administration: Intraperitoneal injection; single every 3 days for 22 days
Result: Suppressed tumor growth by promoting apoptosis in xenografted tumorigenesis.
Animal Model: Female BALB/c nude mice[1].
Dosage: 5, 10, 20 mg/kg
Administration: Intraperitoneal injection; single
Result: Exhibited plasma concentration peaked 1 h after administration.
Showed a relatively high maximum concentration (Cmax= 52.23 ng/mL) and exposure (AUC0-t= 1003.58 h•ng/mL) at a dose of 20 mg/kg.
分子量

393.40

Formula

C19H19N7O3
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

纯度 & 产品资料
参考文献

Antitumor agent-81 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Antitumor agent-812765180-17-2Antitumor agent81Antitumor agent 81p62E1/E2/E3 EnzymeSequestosome-1SQSTM1E1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseA549HCT-116A375HeLaHepG2MCF-7MDA-MB-231MGC-803U2OSMCF-10AcancerInhibitorinhibitorinhibit

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