Name: AK-1690
Brand: BOC Sciences
Rating: 5 (1 reviews)

Size

Price

Stock

Quantity

$--

In stock

Appearance

White to off-white solid

Storage

Store at 4 °C

IUPACName

[[2-[[(2S)-1-[(2S,4S)-4-[7-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-4-yl]hept-6-ynoxy]-2-[(2R)-2-phenylmorpholine-4-carbonyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl]-1-benzothiophen-5-yl]-difluoromethyl]phosphonic acid

Synonyms

AK 1690; AK1690

InChI Key

BOMRVPKXCINUMI-STKXJIFCSA-N

InChI

InChI=1S/C51H56F2N5O11PS/c1-50(2,3)44(55-46(61)42-26-33-25-34(18-20-41(33)71-42)51(52,53)70(65,66)67)49(64)57-28-35(27-39(57)48(63)56-22-24-69-40(30-56)32-14-9-7-10-15-32)68-23-11-6-4-5-8-13-31-16-12-17-36-37(31)29-58(47(36)62)38-19-21-43(59)54-45(38)60/h7,9-10,12,14-18,20,25-26,35,38-40,44H,4-6,11,19,21-24,27-30H2,1-3H3,(H,55,61)(H,54,59,60)(H2,65,66,67)/t35-,38?,39-,40-,44+/m0/s1

SMILES

CC(C)(C)[C@@H](C(=O)N1C[C@H](C[C@H]1C(=O)N2CCO[C@@H](C2)C3=CC=CC=C3)OCCCCCC#CC4=C5CN(C(=O)C5=CC=C4)C6CCC(=O)NC6=O)NC(=O)C7=CC8=C(S7)C=CC(=C8)C(F)(F)P(=O)(O)O

Mechanism

Target: AK-1690 selectively targets signal transducer and activator of transcription 6.

Binding site: Its STAT6 ligand binds the SH2-domain phosphotyrosine-recognition pocket of STAT6.

Mechanism of action: AK-1690 is a potent and selective STAT6 PROTAC degrader developed from a STAT6-binding ligand and a cereblon-recruiting element. By simultaneously engaging STAT6 and CRBN, AK-1690 promotes ternary-complex formation, STAT6 ubiquitination, and proteasome-dependent protein depletion. This degradation mechanism provides a research tool for suppressing STAT6 abundance rather than transiently blocking STAT6 signaling interfaces. AK-1690 is useful for investigating STAT6-selective transcriptional programs, cytokine pathway dependence, degradation selectivity across STAT family members, cellular response kinetics, and the structural basis of ligand-driven STAT6 recognition.

Applications

• PROTAC-Mediated Cancer Research: AK-1690 is instrumental in studying cancer biology through targeted protein degradation. By selectively degrading oncogenic proteins, researchers can investigate the underlying mechanisms of tumor progression and identify potential therapeutic targets, advancing the understanding of cancer pathophysiology.

• Neurodegenerative Disease Models: Utilizing AK-1690 allows researchers to explore the degradation of pathogenic proteins involved in neurodegenerative diseases. This application aids in deciphering disease pathways and developing innovative strategies for therapeutic intervention by eliminating toxic protein aggregates.

• Drug Resistance Studies: AK-1690 facilitates the examination of drug resistance mechanisms by targeting proteins implicated in resistance pathways. This approach enables scientists to uncover novel targets and develop strategies to overcome resistance in various disease models, enhancing the efficacy of existing treatments.

• Signal Transduction Pathway Analysis: Researchers employ AK-1690 to dissect complex signal transduction pathways through selective protein degradation. By modulating specific pathway components, this application provides insights into cellular signaling dynamics and potential intervention points for therapeutic development.

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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