(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine

 CAS No.: 2347517-69-3  Cat No.: BP-400167 4.5  

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual-function PROTAC-related molecule reported to promote Smad3 degradation while increasing HIF-α protein levels. Public sources identify the AHPC-derived portion as a VHL-ligand element, while the benzofuranylmethyl-pyridine-containing module contributes to the dual biological profile; detailed public structural information on the complete ternary complex remains limited. In PROTAC design, the compound is notable because it combines targeted ubiquitination of Smad3 with modulation of oxygen-sensing pathway components. Mechanistically, it is reported to induce ubiquitination and degradation of Smad3 and simultaneously elevate HIF-α, creating a multi-pathway antifibrotic research tool. It is useful for studying TGF-β/Smad signaling, HIF pathway modulation, renal fibrosis models, VHL-ligand pharmacology, and design of multifunctional degraders with pathway-coupled effects.

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine

Structure of 2347517-69-3

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Category
PROTAC
Molecular Formula
C41H46N6O6S
Molecular Weight
750.91
Appearance
Solid

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

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Solubility
DMSO: 170 mg/mL (226.39 mM)
Appearance
Solid
Storage
4°C, away from moisture and light
Mechanism

Target: Targets von Hippel-Lindau ligand module for PROTAC construction for experimental targeted protein degradation studies.

Binding Site: Binds the VHL hydroxyproline-binding pocket used as an E3 ligase handle to support productive ternary complex formation.

Mechanism of Action: (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a modular building block for PROTAC and targeted protein degradation research. Rather than defining a single protein-of-interest, it provides an E3 ligase recruiting or conjugation element that can be linked to a target ligand through an optimized spacer. Systematic variation of linker length, exit vector, and attachment chemistry can tune ternary-complex geometry, ubiquitination efficiency, and degradation selectivity. The compound is useful for assembling comparator degraders, negative controls, or structure-activity series that dissect how E3 engagement influences cellular target depletion.

Applications

• PROTAC-Mediated Protein Degradation: (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is utilized in research to induce the selective degradation of target proteins via the ubiquitin-proteasome system. This compound facilitates the recruitment of E3 ligases to proteins of interest, enabling their ubiquitination and subsequent proteasomal degradation.

• Targeted Degradation in Cancer Research: This PROTAC molecule is pivotal in cancer research, allowing scientists to degrade oncogenic proteins that drive tumorigenesis. By specifically targeting and degrading these proteins, researchers can investigate new therapeutic strategies and understand cancer cell biology more deeply.

• Investigating Protein Function: Researchers employ (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine to study the role of specific proteins in cellular pathways. By degrading a target protein, scientists can observe resultant phenotypic changes, providing insights into protein function and signaling pathways.

• Drug Discovery and Development: This PROTAC compound aids in the discovery of novel drug candidates by enabling the degradation of disease-relevant proteins. It serves as a tool for validating potential drug targets and understanding the biochemical pathways involved 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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