FIP22
Based on 1 Customer Validation
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 Target protein ligand; Blue: Cereblon ligand (HY-W087383); Black: linker (HY-46871)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.53%
- CAS 番号: 3091132-73-6
- 分子式: C46H50N10O6
- 分子量:838.95
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
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IRAK4 3.2 nM (DC50) |
Cereblon |
NF-κB |
IL-6 |
FIP22 (0.02 -10 μM, 0-48 h) induces rapid and durable degradation of IRAK4 protein in HEK293T cells, does not induce the degradation of CRBN neosubstrates or IRAK subtypes[1].
FIP22 (0.02-2 μM) inhibits LPS (HY-D1056)-induced phosphorylation of key proteins in the NF-κB and MAPK signaling pathways, and reduces the secretion of proinflammatory cytokines IL-6, TNF-α, and chemokine CXCL8 in THP-1 cells[1].
FIP22 (120 μM) does not induce cytotoxicity against four normal cell lines (HEK293T, H2C9, BRL-3A, LO2)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells
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Concentration:0.625, 1.25, 2.5 and 5 μM
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Incubation Time:24 h
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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.
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | T1/2 | Tmax | CL | Vz | Cmax | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 2865.43 μg/L·h | 2887.65 μg/L·h | 5.21 h | 5.40 h | 4.96 h | 0.083 h | 0.5 L/h/kg | 3.52 L/kg | 2062.14 ng/mL | / |
| Rat[1] | 20 mg/kg | p.o. | 682.53 μg/L·h | 684.28 μg/L·h | 7.89 h | 8.19 h | 4.30 h | 4.00 h | 104.70 L/h/kg | 632.50 L/kg | 21.68 ng/mL | 2.4 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DNCB-induced atopic dermatitis (AD) model established in male BALB/c mice (8 weeks old)[1]
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Dosage:10 and 30 mg/kg
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Administration:Intraperitoneal injection (i.p.), every daily for 25 days
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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.
化学情報
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CAS 番号 3091132-73-6
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性状 Solid
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分子量 838.95
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分子式 C46H50N10O6
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Color Light yellow to green yellow
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SMILES
CC(NC1=CC(N2C=CC3=CC(C#N)=CN=C32)=NC=C1C(N[C@@H]4CC[C@H](CC4)C(N5CCC6(CC5)CCN(CC6)C7=CC=C(C8=C7)C(N(C8=O)C9C(NC(CC9)=O)=O)=O)=O)=O)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (119.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1920 mL | 5.9598 mL | 11.9197 mL | 29.7992 mL |
| 5 mM | 0.2384 mL | 1.1920 mL | 2.3839 mL | 5.9598 mL | |
| 10 mM | 0.1192 mL | 0.5960 mL | 1.1920 mL | 2.9799 mL | |
| 15 mM | 0.0795 mL | 0.3973 mL | 0.7946 mL | 1.9866 mL | |
| 20 mM | 0.0596 mL | 0.2980 mL | 0.5960 mL | 1.4900 mL | |
| 25 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1920 mL | |
| 30 mM | 0.0397 mL | 0.1987 mL | 0.3973 mL | 0.9933 mL | |
| 40 mM | 0.0298 mL | 0.1490 mL | 0.2980 mL | 0.7450 mL | |
| 50 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5960 mL | |
| 60 mM | 0.0199 mL | 0.0993 mL | 0.1987 mL | 0.4967 mL | |
| 80 mM | 0.0149 mL | 0.0745 mL | 0.1490 mL | 0.3725 mL | |
| 100 mM | 0.0119 mL | 0.0596 mL | 0.1192 mL | 0.2980 mL |
FIP22 関連分類
HY-175764 関連分類
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