2. PROTAC Immunology/Inflammation NF-κB MAPK/ERK Pathway
  3. PROTACs IRAK NF-κB p38 MAPK
  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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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 IRAK4

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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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

 

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[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
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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FIP22 Related Classifications

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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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