2. PROTAC PI3K/Akt/mTOR
  3. PROTACs Akt
  4. INY-03-041 trihydrochloride

INY-03-041 trihydrochloride 

目录号: HY-133120A 纯度: 99.27%
COA 产品使用指南

摩尔计算器

INY-03-041 trihydrochloride 是一种有效的、高选择性的、基于 PROTAC 的泛-AKT 降解剂，由ATP 竞争性 AKT 抑制剂Ipatasertib (HY-15186) 结合 Lenalidomide (HY-A0003，Cereblon 配体)组成。INY-03-041 trihydrochloride 可抑制 AKT1，AKT2 和 AKT3，IC50 分别为 2.0 nM，6.8 nM 和 3.5 nM。

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INY-03-041 trihydrochloride Chemical Structure

INY-03-041 trihydrochloride Chemical Structure

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规格 价格 是否有货 数量
1 mg ￥7900
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Customer Review

Other Forms of INY-03-041 trihydrochloride:

INY-03-041 trihydrochloride 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively[1].

IC50 & Target

Akt1

2.0 nM (IC50)

Akt3

3.5 nM (IC50)

Akt2

6.8 nM (IC50)

Cereblon

 

体外研究
(In Vitro)

INY-03-041 (10-1000 nM; 0-24 hours) induces potent degradation of all three AKT isoforms in MDA-MB-468 cells[1].
INY-03-041 exhibits potent in vitro inhibition of S6K1 (IC50 =37.3 nM) and PKG1 (IC50 = 33.2 nM)[1].
INY-03-041 displays enhanced anti-proliferative effects compared with Ipatasertib (HY-15186) in MDA-MB-468 and HCC1937 cells[1].
INY-03-041 (250 nM, 12 h) promotes sustained AKT degradation and inhibition of downstream signaling effects for up to 96 h, even after compound washout[1].

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

INY-03-041 trihydrochloride 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0, 10, 50, 100, 250, 500, and 1000 nM
Incubation Time: 0, 2, 4, 6, 8. 10, 12, and 24 h
Result: Induced potent degradation of all three AKT isoforms in a dose-dependent manner after a 12-h treatment, with maximal degradation observed between 100 and 250 nM. At concentrations of 500 nM and greater, AKT degradation is diminished. Treatment with 250 nM of INY-03-041 over time reveals partial degradation of all AKT isoforms within 4 h and progressive loss of AKT abundance out to 24 h.
分子量

907.80

Formula

C44H59Cl4N7O5
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

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

纯度 & 产品资料
参考文献

INY-03-041 trihydrochloride 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:

INY-03-041 trihydrochloridePROTACsAktPKBProtein kinase BCRBNMDA-MB-468HCC1937 cellsZR-75-1 cellsPC3 cellsInhibitorinhibitorinhibit

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目录号：
HY-133120A
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