Name: AK-2292
Brand: BOC Sciences
Rating: 5 (1 reviews)

Size

Price

Stock

Quantity

$--

In stock

Purity

98% by HPLC

Appearance

Off-white to Light Yellow Solid

IUPACName

[[2-[[(2S)-1-[(2S)-2-[[3-[5-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]pent-4-ynyl-methylamino]-3-oxopropyl]-[4-(1,3-thiazol-2-yl)phenyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl]-1-benzothiophen-5-yl]-difluoromethyl]phosphonic acid

Synonyms

AK 2292; AK2292

InChI Key

LOPYPDQOHNOVBM-QOIUHGAOSA-N

InChI

InChI=1S/C52H54F2N7O10PS2/c1-51(2,3)44(57-46(65)41-29-33-28-34(16-20-40(33)74-41)52(53,54)72(69,70)71)50(68)60-25-9-13-39(60)49(67)59(35-17-14-32(15-18-35)47-55-23-27-73-47)26-22-43(63)58(4)24-7-5-6-10-31-11-8-12-36-37(31)30-61(48(36)66)38-19-21-42(62)56-45(38)64/h8,11-12,14-18,20,23,27-29,38-39,44H,5,7,9,13,19,21-22,24-26,30H2,1-4H3,(H,57,65)(H,56,62,64)(H2,69,70,71)/t38?,39-,44+/m0/s1

SMILES

CC(C)(C)C(C(=O)N1CCCC1C(=O)N(CCC(=O)N(C)CCCC#CC2=C3CN(C(=O)C3=CC=C2)C4CCC(=O)NC4=O)C5=CC=C(C=C5)C6=NC=CS6)NC(=O)C7=CC8=C(S7)C=CC(=C8)C(F)(F)P(=O)(O)O

Mechanism

Target: AK-2292 selectively targets STAT5A and STAT5B transcription factor isoforms.

Binding site: Its STAT5 ligand binds the SH2-domain phosphotyrosine-recognition interface.

Mechanism of action: AK-2292 is a selective small-molecule PROTAC degrader of STAT5A and STAT5B. The compound combines a STAT5-recognition ligand with an E3 ligase-recruiting module, enabling proximity-dependent ubiquitination and proteasomal degradation of both STAT5 isoforms. This approach removes STAT5 proteins rather than only interfering with phosphorylation-dependent signaling, allowing more complete interrogation of STAT5-dependent transcriptional networks. In research applications, AK-2292 supports analysis of STAT5 isoform redundancy, pathway selectivity over other STAT proteins, degradation kinetics, downstream gene-expression changes, and target dependency in hematologic cell models.

Applications

• PROTAC-Mediated Kinase Degradation: AK-2292 is designed to facilitate the selective degradation of specific kinase proteins, thereby providing researchers a powerful tool to study kinase signaling pathways and their roles in disease mechanisms. This approach allows for the exploration of kinase function by transiently removing the protein from cellular systems.

• Targeted Degradation in Oncology Research: By employing AK-2292, scientists can investigate the degradation of oncogenic proteins, offering insights into the potential vulnerabilities of cancer cells. This targeted approach aids in understanding protein dependencies and could guide the development of novel therapeutic strategies.

• Exploring Protein-Protein Interactions: AK-2292 enables the study of protein-protein interactions by selectively degrading target proteins involved in complex cellular networks. This application is crucial for dissecting the dynamic roles of proteins and their interactions in various biological processes.

• Advancing Neurodegenerative Disease Models: Utilizing AK-2292, researchers can target and degrade proteins implicated in neurodegenerative diseases. This helps in elucidating the pathological roles of these proteins and provides a platform for developing potential therapeutic interventions.

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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