2. PROTAC Immunology/Inflammation Apoptosis GPCR/G Protein
  3. PROTACs IRAK TNF Receptor IFNAR Interleukin Related CXCR CCR
  4. PROTAC IRAK4 degrader-14

PROTAC IRAK4 degrader-14 是一种口服有效的 IRAK4 PROTAC 降解剂，其 DC50 为 2.4 nM。PROTAC IRAK4 degrader-14 可抑制包括 T 细胞、单核细胞和角质形成细胞在内的多种细胞类型的促炎反应。PROTAC IRAK4 degrader-14 可用于银屑病的相关研究。

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PROTAC IRAK4 degrader-14

PROTAC IRAK4 degrader-14 Chemical Structure

CAS No. : 3113890-51-7

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PROTAC IRAK4 degrader-14 相关抗体

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC IRAK4 degrader-14 is an orally active IRAK4 PROTAC degrader with a DC50 of 2.4 nM. PROTAC IRAK4 degrader-14 inhibits proinflammatory responses in multiple cell types including T cells, monocytes and keratinocytes. PROTAC IRAK4 degrader-14 is applicable to research related to psoriasis[1].

IC50 & Target[1]

IRAK4

2.4 nM (DC50)

IL-6

 

IL-2

 

体外研究
(In Vitro)

PROTAC IRAK4 degrader-14 (Compound Ori-Zim-6) (250 nM; 3-24 h) 可在人单核细胞系 THP-1 中诱导时间依赖性的 IRAK4 降解，在 250 nM 处理条件下，12 h 内降解率超过 90%，24 h 内实现完全降解[1]。
PROTAC IRAK4 degrader-14 (250-500 nM; 12-24 h) 可诱导人单核细胞系 THP-1 中依赖蛋白酶体、NCL 和 MDM2 的 IRAK4 泛素化与降解，并促进 MDM2-NCL-PROTAC-IRAK4 四元复合物的组装[1]。
PROTAC IRAK4 degrader-14 (0.01-1 μM; 24 h) 可浓度依赖性地抑制 LPS 诱导的人单核细胞 THP-1 中促炎介质 (CCL2、CXCL8、IL-6、TNF-α) 的 mRNA 表达[1]。
PROTAC IRAK4 degrader-14 (0.01-1 μM; 24 h) 可浓度依赖性地抑制人 Jurkat T 细胞中促炎细胞因子 (TNF-α、IL-2、IFN-γ) 的 mRNA 表达[1]。
PROTAC IRAK4 degrader-14 (0.01-1 μM; 24 h) 可浓度依赖性地抑制人角质形成细胞 HaCaT 中 IL-1β 诱导的促炎介质 (TNF-α、IL-6、CXCL8、IL-19) mRNA 表达[1]。

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

PROTAC IRAK4 degrader-14 相关抗体:

Real Time qPCR[1]

Cell Line: LPS-Stimulated Human Monocytic THP-1 Cells
Concentration: 0.01, 0.1 and 1 μM
Incubation Time: 24 h
Result: Caused concentration-dependent reductions in mRNA levels of pro-inflammatory mediators CCL2, CXCL8, IL-6, and TNF-α.
Exhibited more potent inhibition of CCL2, IL-6, and TNF-α mRNA expression than the reference degrader KT-474 at equivalent concentrations.

Real Time qPCR[1]

Cell Line: Human Jurkat T Cells
Concentration: 0.01, 0.1 and 1 μM
Incubation Time: 24 h
Result: Suppressed T cell activation via reduced mRNA levels of TNF-α, IL-2, and IFN-γ.
Exhibited more potent suppression of IFN-γ mRNA than KT-474 at equivalent concentrations.

Real Time qPCR[1]

Cell Line: IL-1β-Stimulated Human Keratinocyte HaCaT Cells
Concentration: 0.01-1 μM
Incubation Time: 24 h
Result: Suppressed mRNA levels of TNF-α, IL-6, CXCL8, and IL-19.
Exhibited stronger suppression of IL-6, CXCL8, and IL-19 mRNA levels than KT-474 at equivalent concentrations.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax AUC0-t AUC0-∞ T1/2 CL Vss F
Mice[1] 2 mg/kg i.v. 0.13 h 174.32 ng/mL 452.38 ng·h/mL 549.32 ng·h/mL 5.1 h 60.67 mL/min/kg 24 L/kg /
Mice[1] 20 mg/kg p.o. 0.25 h 73.18 ng/mL 233.51 ng·h/mL 264.66 ng·h/mL 4.0 h 75.36 mL/min/kg 420 L/kg 5 %
体内研究
(In Vivo)

PROTAC IRAK4 degrader-14 (Compound Ori-Zim-6) (20 mg/kg; p.o.; 每日一次共 5 天) 在 Imiquimod (IMQ) (HY-B0180) 诱导的银屑病小鼠模型中展现出显著疗效，同时具有良好的安全性特征，包括体重恢复和血清肝功能指标恢复[1]。

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

Animal Model: BALB/c
(male, 6-8 weeks old)[1]
Dosage: 20 mg/kg
Administration: p.o.; daily; 5 consecutive days
Result: Reduced total Psoriasis Area and Severity Index (PASI) scores, ear thickening, spleen enlargement, and dorsal skin epidermal thickness.
Downregulated mRNA expression of IL-1β, IL-23, Lipocalin-2 (Lcn2), and TNF-α in ear skin tissues.
Prevented IMQ-induced body weight loss.
Significantly restored serum albumin (ALB) and alkaline phosphatase (ALP) levels.
Showed no detectable histopathological damage to major organs (heart, liver, spleen, lung, kidney).
分子量

1074.20

Formula

C59H68FN5O13
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

PROTAC IRAK4 degrader-14 相关分类

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  • 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:

PROTAC IRAK4 degrader-143113890-51-7PROTACsIRAKTNF ReceptorIFNARInterleukin RelatedCXCRCCRInterleukin-1 receptor associated kinaseIL-1R associated kinaseTumor Necrosis Factor ReceptorTNFRInterferon-α/β receptorInterferon-alpha/beta receptor ILCXC chemokine receptorsC-X-C motif chemokine receptorsCC chemokine receptorpsoriasisubiquitin-proteasome systemIRAK4Jurkat T cellsnucleolinTHP-1 cellsT cellsMDM2monocyteskeratinocytesInhibitorinhibitorinhibit

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