2. PROTAC Immunology/Inflammation NF-κB MAPK/ERK Pathway
  3. PROTACs IRAK NF-κB p38 MAPK
  4. FIP22

FIP22 是一种强效的、具有选择性的 IRAK4 PROTAC 降解剂 (HEK293T 细胞：DC50 = 3.2 nM；THP-1 细胞：DC50 = 10.6 nM)。FIP22 通过形成 IRAK4-FIP22-CRBN 三元复合物诱导泛素-蛋白酶体系统 (EC50 = 12.63 nM)，从而强效阻断 IRAK4 介导的 NF-κB 和 MAPK 信号通路。FIP22 可用于研究特应性皮炎 (粉色：IRAK4 配体 (HY-175765)；蓝色：CRBN 配体 (HY-W087383)；黑色：连接体 (HY-46871))。

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FIP22

FIP22 Chemical Structure

CAS No. : 3091132-73-6

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FIP22 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 IRAK 亚型特异性产品:

查看所有亚型
IRAK1 IRAK4

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis (Pink: IRAK4 ligand (HY-175765); Blue: CRBN ligand (HY-W087383); Black: Linker (HY-46871))[1].

IC50 & Target[1]

IRAK4

3.2 nM (DC50)

Cereblon

 

NF-κB

 

体外研究
(In Vitro)

FIP22 (0.02 -10 μM, 0-48 h) 可诱导 HEK293T 细胞中 IRAK4 蛋白快速持久降解，但不诱导 CRBN 底物或 IRAK 亚型的降解[1]。
FIP22 (0.02-2 μM) 可在 THP-1 细胞中抑制 LPS（HY-D1056）诱导的 NF-κB 和 MAPK 信号通路中关键蛋白的磷酸化，并减少促炎细胞因子 IL-6、TNF-α 和趋化因子 CXCL8[1]的分泌。
FIP22 (120 μM) 不会诱导对四种正常细胞系 (HEK293T、H2C9、BRL-3A、LO2) 的细胞毒性[1]。

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

FIP22 相关抗体:

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: 0.625, 1.25, 2.5 and 5 μM
Incubation Time: 24 h
Result: Had no effect on the levels of IKZF1, IKZF3 and GSPT1.
Did not induce degradation of other IRAK family subtypes, providing additional evidence for its target-specific effects.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 2 mg/kg i.v. AUC0-t 2865.43 μg/L·h
Rat 20 mg/kg p.o. AUC0-t 682.53 μg/L·h
Rat 2 mg/kg i.v. AUC0-∞ 2887.65 μg/L·h
Rat 20 mg/kg p.o. AUC0-∞ 684.28 μg/L·h
Rat 2 mg/kg i.v. MRT0-t 5.21 h
Rat 20 mg/kg p.o. MRT0-t 7.89 h
Rat 2 mg/kg i.v. MRT0-∞ 5.40 h
Rat 20 mg/kg p.o. MRT0-∞ 8.19 h
Rat 2 mg/kg i.v. T1/2 4.96 h
Rat 20 mg/kg p.o. T1/2 4.30 h
Rat 2 mg/kg i.v. Tmax 0.083 h
Rat 20 mg/kg p.o. Tmax 4.00 h
Rat 2 mg/kg i.v. CL 0.5 L/h/kg
Rat 20 mg/kg p.o. CL 104.70 L/h/kg
Rat 2 mg/kg i.v. Vz 3.52 L/kg
Rat 20 mg/kg p.o. Vz 632.50 L/kg
Rat 2 mg/kg i.v. Cmax 2062.14 ng/mL
Rat 20 mg/kg p.o. F 2.4 %
Rat 20 mg/kg p.o. Cmax 21.68 ng/mL
体内研究
(In Vivo)

FIP22 (10-30 mg/kg，腹腔注射，每日一次，共25天) 在 2,4-二硝基氯苯 (DNCB) 诱发的特应性皮炎小鼠模型中表现出显著的治疗效果[1]。

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

Animal Model: DNCB-induced atopic dermatitis (AD) model established in male BALB/c mice (8 weeks old)[1]
Dosage: 10 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.), every daily for 25 days
Result: significantly improved skin lesions, including erythema, excoriation, scaling and crusting.
No obvious systemic toxicity or weight loss.
Significantly reduced the number of scratching times in mice.
Reduced splenomegaly and reversed epidermal hyperplasia (thickening), hyperkeratosis, and inflammatory cell infiltration in the dermis.
分子量

838.95

Formula

C46H50N10O6
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

FIP22 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:

FIP223091132-73-6FIP 22FIP-22PROTACsIRAKNF-κBp38 MAPKInterleukin-1 receptor associated kinaseIL-1R associated kinaseNuclear factor-κBNuclear factor-kappaBToll-like receptors (TLRs)atopic dermatitisHEK293T cellsTHP-1 cellsInhibitorinhibitorinhibit

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