2. PROTAC Immunology/Inflammation
  3. PROTACs IRAK Interleukin Related
  4. APH02174 (hemiformic)

APH02174 (hemiformic) 是一种高度选择性和口服有效的 IRAK4 PROTAC 降解剂，在 THP-1 细胞中的 DC50 为 4.01 nM。APH02174 (hemiformic) 通过抑制 IL-6 的释放来阻断炎症信号。APH02174 (hemiformic) 可用于研究炎症性疾病，如银屑病和类风湿性关节炎。
(粉色: IRAK4 配体 (HY-174470)；蓝色: Cereblon 配体 (HY-45512)；黑色: 连接子)。

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APH02174 (hemiformic)

APH02174 (hemiformic) Chemical Structure

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1 mg ￥8500
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Other Forms of APH02174 (hemiformic):

APH02174 (hemiformic) 相关抗体

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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IRAK1 IRAK3 IRAK4

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

APH02174 (hemiformic) is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells. APH02174 (hemiformic) blocks inflammatory signals by inhibiting IL-6 release. APH02174 (hemiformic) can be used for research on inflammatory conditions such as psoriasis vulgaris and rheumatoid arthritis[1]. (Pink: IRAK4 ligand (HY-174470); Blue: Cereblon ligand (HY-45512); Black: linker).

IC50 & Target[1]

Cereblon

 

IRAK4

 

IL-6

 

体外研究
(In Vitro)

APH02174 (0.24-1000 nM) (hemiformic) 可以选择性降解多种细胞中的 IRAK4 蛋白，包括 THP-1 (DC50 = 4.01 nM)，hPBMCs (DC50 = 0.43 nM) 和小鼠 PBMCs (DC50 = 3.57 nM) [1]。
APH02174 (0.03-2000 nM；24 小时) (hemiformic) 显著抑制 hPBMCs 中 LPS (HY-D1056) 诱导的 IL-6 释放 (IC50 = 16.43 nM)[1]。

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

APH02174 (hemiformic) 相关抗体:
体内研究
(In Vivo)

APH02174 (10-100 mg/kg；口服；每日两次；持续 7 天) 可减少 IMQ (HY-B0180) 诱导的银屑病小鼠中皮肤炎症并且降解脾脏的 IRAK4 蛋白水平[1]。
APH02174 (30 或 100 mg/kg；口服；每日一次；持续 14 天) 显著改善类风湿性关节炎小鼠的关节炎[1]。

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

916.03

Formula

C49H55N7O8·1/2CH2O2
性状

固体

运输条件

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

4°C, sealed storage, away from moisture

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

纯度 & 产品资料
参考文献

APH02174 (hemiformic) 相关分类

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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:

APH02174 (hemiformic)PROTACsIRAKInterleukin RelatedInterleukin-1 receptor associated kinaseIL-1R associated kinaseILInhibitorinhibitorinhibit

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产品名称：
APH02174 (hemiformic)
目录号：
HY-174455A
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