2. PROTAC Immunology/Inflammation NF-κB MAPK/ERK Pathway Apoptosis
  3. PROTACs IRAK NF-κB p38 MAPK TNF Receptor Interleukin Related
  4. FIP22

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)).

For research use only. We do not sell to patients.

FIP22

FIP22 Chemical Structure

CAS No. : 3091132-73-6

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Based on 1 publication(s) in Google Scholar

FIP22 Related Antibodies

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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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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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

  • Biological Activity

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Description

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

 

IL-6

 

In Vitro

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.

FIP22 Related Antibodies

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.
Parmacokinetics
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 %
In Vivo

FIP22 (10-30 mg/kg, i.p., once daily for 25 days) exhibits significant therapeutic efficacy in a 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis mouse model[1].

MedChemExpress (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.
Molecular Weight

838.95

Formula

C46H50N10O6
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1920 mL 5.9598 mL 11.9197 mL
5 mM 0.2384 mL 1.1920 mL 2.3839 mL
View the 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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FIP22 Related Classifications

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 MAPKTNF ReceptorInterleukin RelatedInterleukin-1 receptor associated kinaseIL-1R associated kinaseNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRILToll-like receptors (TLRs)atopic dermatitisHEK293T cellsTHP-1 cellsInhibitorinhibitorinhibit

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