(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
Based on 1 publication(s) in Google Scholar
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual-targeting PROTAC molecule. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine not only targets the ubiquitination and degradation of Smad3, but also elevates the protein level of HIF-α, thereby exerting multi-pathway anti-fibrotic and renoprotective effects. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine can be used in a wide range of tumor studies including cancers with KRAS inhibitor resistance, covering pancreatic ductal adenocarcinoma, acute myeloid leukemia, and various soft tissue sarcomas (such as fibrosarcoma, liposarcoma, chondrosarcoma, etc.). (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine can also be applied to research related to various solid tumors and hematological malignancies, involving multiple cancer types such as colon cancer, breast cancer, ovarian cancer, non-small cell lung cancer, glioblastoma, and melanoma.
(Pink: Smad3 Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Purity : 98.62%
- CAS No.: 2347517-69-3
- Formula: C41H46N6O6S
- Molecular Weight:750.91
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications Citing Use of MedChemExpress (MCE) (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
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WB
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
VHL |
Smad3 |
In Vitro
Smad3 is a key transcription factor in the TGF-β signaling pathway, involved in processes such as cell proliferation, differentiation, and fibrosis. Selective degradation of Smad3 avoids the interference with the Smad4 pathway often associated with traditional inhibition methods, offering a novel approach for treating fibrotic diseases and cancer.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CWR22Rv1 cells
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Concentration:0, 10, 20 and 50 μM
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Incubation Time:24 h
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Result:Significantly reduced the protein levels of Smad3, AR, AR-V7.
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Cell Line:CWR22Rv1 cells
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Concentration:0, 10, 20 and 50 μM
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Incubation Time:24 h
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Result:Significantly reduced the mRNA levels of Smad3, AR, AR-V7.
Chemical Information
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CAS No. 2347517-69-3
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Appearance Solid
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Molecular Weight 750.91
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Formula C41H46N6O6S
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Color White to light yellow
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SMILES
O=C(N1[C@@H](C[C@H](C1)O)C(N[C@H](C2=CC=C(C3=C(N=CS3)C)C=C2)C)=O)[C@H](C(C)(C)C)NC(CCC(NC(C4=CN=CC=C4)C5=CC6=CC=CC=C6O5)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nucleic Acids Res
2023 Apr 11;51(6):2655-2670. PMID: 36727462
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2023 Apr 11;51(6):2655-2670. [Abstract]
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine (The SMAD3 PROTAC inhibitor; 10, 20, 50 µM; 24 h) reduces levels of SMAD3 protein in Rv1 cells with concomitant reduction in the levels of AR, AR-V7 and AR targets.
Solvent & Solubility
In Vitro:
DMSO : ≥ 170 mg/mL (226.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (293 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3317 mL | 6.6586 mL | 13.3172 mL | 33.2929 mL |
| 5 mM | 0.2663 mL | 1.3317 mL | 2.6634 mL | 6.6586 mL | |
| 10 mM | 0.1332 mL | 0.6659 mL | 1.3317 mL | 3.3293 mL | |
| 15 mM | 0.0888 mL | 0.4439 mL | 0.8878 mL | 2.2195 mL | |
| 20 mM | 0.0666 mL | 0.3329 mL | 0.6659 mL | 1.6646 mL | |
| 25 mM | 0.0533 mL | 0.2663 mL | 0.5327 mL | 1.3317 mL | |
| 30 mM | 0.0444 mL | 0.2220 mL | 0.4439 mL | 1.1098 mL | |
| 40 mM | 0.0333 mL | 0.1665 mL | 0.3329 mL | 0.8323 mL | |
| 50 mM | 0.0266 mL | 0.1332 mL | 0.2663 mL | 0.6659 mL | |
| 60 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5549 mL | |
| 80 mM | 0.0166 mL | 0.0832 mL | 0.1665 mL | 0.4162 mL | |
| 100 mM | 0.0133 mL | 0.0666 mL | 0.1332 mL | 0.3329 mL |
Keywords
- (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
- 2347517-69-3
- PROTACs
- TGF-beta/Smad
- HIF/HIF Prolyl-Hydroxylase
- osteogenic sarcoma
- acute myeloid leukemia
- pancreatic ductal adenocarcinoma
- SMAD inhibitor
- cancer
- myxosarcoma
- chondrosarcoma
- liposarcoma
- fibrosarcoma
- kras inhibitor-resistant cancers
- Inhibitor
- inhibitor
- inhibit