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

APH02174 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 通过抑制 IL-6 的释放来阻断炎症信号。APH02174 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：CRBN 配体 (HY-45512); 黑色：连接子; CRBN 配体+连接子 (HY-174796))

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APH02174

APH02174 Chemical Structure

CAS No. : 3065494-66-5

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APH02174 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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IRAK1 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

APH02174 is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells. APH02174 blocks inflammatory signals by inhibiting IL-6 release. APH02174 can be used for research on inflammatory conditions such as psoriasis vulgaris and rheumatoid arthritis. (Pink: IRAK4 Ligand (HY-174470); Blue: CRBN Ligand (HY-45512); Black: Linker; CRBN Ligand+Linker (HY-174796))[1]

IC50 & Target[1]

IRAK4

4.01 nM (DC50)

IL-6

 

体外研究
(In Vitro)

APH02174 (0.24-1000 nM) 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) 显著抑制 hPBMCs 中 LPS 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 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.

Animal Model: Collagen-induced psoriasis male DBA/1 mice (7 weeks)[1]
Dosage: 30 or 100 mg/kg
Administration: Oral administration (p.o.); once daily for 14 days
Result: Significantly improved arthritis score and reduced inflammation.
Significantly reduced pathological scores and improved pathological structural changes.
Significantly degraded IRAK4 in mouse PBMCs.
分子量

870.00

Formula

C49H55N7O8
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

APH02174 相关分类

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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:

APH021743065494-66-5APH 02174APH-02174PROTACsIRAKInterleukin RelatedInterleukin-1 receptor associated kinaseIL-1R associated kinaseILIRAK4PROTACIL-6InflammationInhibitorinhibitorinhibit

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APH02174
目录号：
HY-174455
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