BTK-IN-24

 CAS No.: 2649400-34-8  Cat No.: BP-400195  Purity: 98% by HPLC 4.5  

BTK-IN-24, also known as NX-5948 or bexobrutideg, is a cereblon-recruiting PROTAC degrader targeting Bruton's tyrosine kinase. Public sources describe it as a BTK-directed degrader that induces BTK protein degradation through the cereblon E3 ligase complex and inhibits B-cell activation; some summaries also note activity in models containing wild-type or inhibitor-resistant BTK. In PROTAC design, the BTK ligand provides kinase recognition, the linker defines the spatial arrangement, and the cereblon ligand recruits CRL4-cereblon ubiquitination machinery. Mechanistically, BTK-IN-24 promotes BTK ubiquitination and proteasome-mediated depletion, allowing researchers to examine consequences of BTK protein loss rather than reversible catalytic inhibition alone. It is useful for B-cell receptor signaling studies, BTK resistance research, cereblon-based kinase degrader optimization, immune-cell pathway analysis, and comparison of BTK inhibitors with degradation-based chemical probes.

BTK-IN-24

Structure of 2649400-34-8

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Category
PROTAC
Molecular Formula
C42H54N12O5
Molecular Weight
807.0
Appearance
Off-white to Light Yellow Solid

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

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Purity
98% by HPLC
Appearance
Off-white to Light Yellow Solid
IUPACName
3-[4-[1-[[1-[6-[[(3S)-2,6-dioxopiperidin-3-yl]carbamoyl]pyridin-3-yl]piperidin-4-yl]methyl]piperidin-4-yl]anilino]-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide
Synonyms
NX-5948; NX 5948; NX5948
InChI Key
HPTPDBYCFHFWJG-CWTKIQHKSA-N
InChI
InChI=1S/C42H54N12O5/c1-50-21-22-54(42(50)59)32-3-2-16-53(26-32)35-24-45-37(38(43)56)39(48-35)46-30-6-4-28(5-7-30)29-14-17-51(18-15-29)25-27-12-19-52(20-13-27)31-8-9-33(44-23-31)40(57)47-34-10-11-36(55)49-41(34)58/h4-9,23-24,27,29,32,34H,2-3,10-22,25-26H2,1H3,(H2,43,56)(H,46,48)(H,47,57)(H,49,55,58)/t32-,34+/m1/s1
SMILES
CN1CCN(C1=O)C2CCCN(C2)C3=CN=C(C(=N3)NC4=CC=C(C=C4)C5CCN(CC5)CC6CCN(CC6)C7=CN=C(C=C7)C(=O)NC8CCC(=O)NC8=O)C(=O)N
Mechanism

Target: Targets Bruton tyrosine kinase (BTK) for experimental targeted protein degradation studies.

Binding Site: Binds the BTK ATP-binding pocket and recruited E3 ligase ligand site to support productive ternary complex formation.

Mechanism of Action: BTK-IN-24 is designed for use in PROTAC or targeted protein degradation experiments directed toward Bruton tyrosine kinase (BTK). 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 BTK Degradation: BTK-IN-24 is employed in research to selectively degrade Bruton's tyrosine kinase (BTK) via the PROTAC mechanism. This approach allows for the study of BTK's role in signaling pathways, providing insights into its function and potential as a therapeutic target in diseases such as B-cell malignancies.

• Targeted Protein Degradation Studies: Utilizing BTK-IN-24, researchers can investigate the efficacy of targeted protein degradation in modulating protein levels within cells. This enables the exploration of innovative strategies for drug development, focusing on degrading rather than inhibiting proteins of interest.

• Mechanistic Insights into PROTAC Action: BTK-IN-24 serves as a valuable tool for elucidating the mechanistic aspects of PROTAC-induced protein degradation. Researchers can dissect the cellular processes involved, enhancing the understanding of how PROTACs can be optimized for improved specificity and potency.

• Advancing Drug Discovery Research: By integrating BTK-IN-24 into experimental frameworks, scientists can advance drug discovery efforts aimed at developing novel therapeutics. This compound facilitates the exploration of targeted degradation as a viable strategy for addressing 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

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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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