Name: KT-474
Brand: BOC Sciences
Rating: 5 (1 reviews)

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$--

In stock

Appearance

Off-white to yellow solid

Storage

Store at -20 °C

IUPACName

N-[3-(difluoromethyl)-1-[4-[[4-[3-[1-(2,6-dioxopiperidin-3-yl)-3-methyl-2-oxobenzimidazol-4-yl]prop-2-ynoxy]piperidin-1-yl]methyl]cyclohexyl]pyrazol-4-yl]-5-[(1R,4R)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamide

Synonyms

KT 474; KT474; KYM-001; PROTAC IRAK4 degrader-7; N-[3-(Difluoromethyl)-1-[trans-4-[[4-[[3-[1-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-3-methyl-2-oxo-1H-benzimidazol-4-yl]-2-propyn-1-yl]oxy]-1-piperidinyl]methyl]cyclohexyl]-1H-pyrazol-4-yl]-5-(1R,4R)-2-oxa-5-azabicyclo[2.2.1]hept-5-ylpyrazolo[1,5-a]pyrimidine-3-carboxamide

InChI Key

NQGKNAVUMAHSQN-PKIOHZLWSA-N

InChI

InChI=1S/C44H49F2N11O6/c1-52-39-27(4-2-6-34(39)57(44(52)61)35-11-12-37(58)50-43(35)60)5-3-19-62-30-13-16-53(17-14-30)22-26-7-9-28(10-8-26)56-24-33(38(51-56)40(45)46)48-42(59)32-21-47-55-18-15-36(49-41(32)55)54-23-31-20-29(54)25-63-31/h2,4,6,15,18,21,24,26,28-31,35,40H,7-14,16-17,19-20,22-23,25H2,1H3,(H,48,59)(H,50,58,60)/t26?,28?,29-,31-,35?/m1/s1

SMILES

CN1C2=C(C=CC=C2N(C1=O)C3CCC(=O)NC3=O)C#CCOC4CCN(CC4)CC5CCC(CC5)N6C=C(C(=N6)C(F)F)NC(=O)C7=C8N=C(C=CN8N=C7)N9C[C@H]1C[C@@H]9CO1

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: KT-474 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 Inflammation Research: KT-474 is a potent PROTAC designed to target and degrade specific inflammatory proteins, providing researchers with a tool to explore the molecular mechanisms underlying inflammation. By selectively degrading these proteins, KT-474 aids in dissecting their roles in immune responses and inflammatory pathways.

• Targeted Protein Degradation in Autoimmunity: KT-474 facilitates the study of autoimmune disorders by enabling the targeted degradation of proteins implicated in autoimmune responses. This application allows researchers to investigate the therapeutic potential of protein degradation strategies in modulating immune system dysregulation.

• Signal Transduction Pathway Analysis: Utilizing KT-474, researchers can achieve targeted degradation of key signaling proteins, thereby elucidating their functional roles within complex signal transduction networks. This approach enhances the understanding of cellular signaling dynamics and their implications in disease states.

• Drug Discovery and Development: KT-474 serves as a valuable tool in the drug discovery process, enabling the identification and validation of novel drug targets through PROTAC-mediated protein degradation. This application supports the development of innovative therapeutic strategies by focusing on previously undruggable targets.

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* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂