PROTAC IRAK4 degrader-1

 CAS No.: 2360533-90-8  Cat No.: BP-400185  Purity: ≥95% 4.5  

PROTAC IRAK4 degrader-1, also described as compound I-210, is a cereblon-based PROTAC targeting interleukin-1 receptor-associated kinase IRAK4. Public sources describe a modular structure containing an IRAK4 ligand, a pomalidomide-derived cereblon ligand, and a linker that connects these components. The exact IRAK4 binding-site details are not fully disclosed in product summaries, but the design places the IRAK4-recognition element and cereblon recruiter in a geometry suitable for ternary-complex formation. Mechanistically, the compound recruits IRAK4 to cereblon, enabling ubiquitination and subsequent proteasomal degradation of IRAK4 in cellular systems. It is valuable for interrogating IRAK4 scaffolding versus kinase functions, innate immune signaling, inflammatory pathway dependencies, and degrader optimization for kinase targets where protein removal may produce biological effects distinct from catalytic inhibition.

PROTAC IRAK4 degrader-1

Structure of 2360533-90-8

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Category
PROTAC
Molecular Formula
C44H39F3N12O7
Molecular Weight
904.85
Appearance
Solid

* For research and manufacturing use only. Not for human or clinical use.

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Purity
≥95%
Solubility
Soluble in DMSO
Appearance
Solid
Storage
Store at -20°C
IUPACName
2-[2-(cyclopropylmethylamino)pyridin-4-yl]-N-[1-[4-[3-[4-[[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]methyl]imidazol-1-yl]propylcarbamoyl]phenyl]-3-(trifluoromethyl)pyrazol-4-yl]-1,3-oxazole-4-carboxamide
Synonyms
2-{2-[(Cyclopropylmethyl)amino]-4-pyridinyl}-N-{1-[4-({3-[4-({[2-(2,6-dioxo-3-piperidinyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}methyl)-1H-imidazol-1-yl]propyl}carbamoyl)phenyl]-3-(trifluoromethyl)-1H-pyrazol-4-yl}-1,3-oxazole-4-carboxamide; 4-Oxazolecarboxamide, 2-[2-[(cyclopropylmethyl)amino]-4-pyridinyl]-N-[1-[4-[[[3-[4-[[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]methyl]-1H-imidazol-1-yl]propyl]amino]carbonyl]phenyl]-3-(trifluoromethyl)-1H-pyrazol-4-yl]-
Density
1.6±0.1 g/cm3
InChI Key
YXSXFMHKDNIZFS-UHFFFAOYSA-N
InChI
InChI=1S/C44H39F3N12O7/c45-44(46,47)37-31(53-39(62)32-22-66-41(54-32)26-13-15-48-34(17-26)51-18-24-5-6-24)21-58(56-37)28-9-7-25(8-10-28)38(61)49-14-2-16-57-20-27(52-23-57)19-50-30-4-1-3-29-36(30)43(65)59(42(29)64)33-11-12-35(60)55-40(33)63/h1,3-4,7-10,13,15,17,20-24,33,50H,2,5-6,11-12,14,16,18-19H2,(H,48,51)(H,49,61)(H,53,62)(H,55,60,63)
SMILES
C1CC1CNC2=NC=CC(=C2)C3=NC(=CO3)C(=O)NC4=CN(N=C4C(F)(F)F)C5=CC=C(C=C5)C(=O)NCCCN6C=C(N=C6)CNC7=CC=CC8=C7C(=O)N(C8=O)C9CCC(=O)NC9=O
Mechanism

Target: Targets IRAK4 kinase scaffolding protein for experimental targeted protein degradation studies.

Binding Site: Binds the IRAK4 kinase domain and cereblon thalidomide-binding pocket to support productive ternary complex formation.

Mechanism of Action: PROTAC IRAK4 degrader-1 is designed for use in PROTAC or targeted protein degradation experiments directed toward IRAK4 kinase scaffolding protein. The bifunctional molecule links a target-recognition element to cereblon, promoting proximity between the protein of interest and ubiquitination machinery. Productive ternary-complex formation can drive polyubiquitination and proteasome-dependent target depletion, allowing researchers to compare pharmacological inhibition with protein removal. It is suitable for evaluating degradation potency, kinetics, pathway selectivity, and downstream signaling consequences in engineered or disease-relevant cellular models.

Applications

• PROTAC-Mediated IRAK4 Degradation: This PROTAC IRAK4 degrader-1 is designed for the targeted degradation of interleukin-1 receptor-associated kinase 4 (IRAK4). It is instrumental in studying the modulation of IRAK4-dependent signaling pathways, offering insights into inflammatory responses and immune system regulation.

• Inflammation Pathway Investigation: Utilize PROTAC IRAK4 degrader-1 to dissect the role of IRAK4 in inflammation-related pathways. By selectively degrading IRAK4, researchers can elucidate its function and interaction with other proteins, facilitating the exploration of novel anti-inflammatory therapeutic strategies.

• Signal Transduction Analysis: Employ PROTAC IRAK4 degrader-1 to examine the impact of IRAK4 degradation on signal transduction processes. This application aids in understanding the downstream effects of IRAK4 removal, providing a deeper comprehension of cellular communication mechanisms in immune responses.

• Immune System Research: Leverage the targeted degradation capabilities of PROTAC IRAK4 degrader-1 to study immune system dynamics. By depleting IRAK4, researchers can investigate its role in innate immunity and its potential as a target for modulating immune functions in various diseases.

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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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