924229
(S,R,S)-AHPC-Me
95%
Sinónimos:
(2S,4R)-1-((S)-2-amino-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide, PROTAC® research ligand, VH032 methyl derivative
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About This Item
Fórmula empírica (notación de Hill):
C23H32N4O3S
Número de CAS:
Peso molecular:
444.59
MDL number:
UNSPSC Code:
12352101
NACRES:
NA.22
Productos recomendados
ligand
VH032
Quality Level
assay
95%
form
powder
storage temp.
2-8°C
SMILES string
C([C@H](C(C)(C)C)N)(=O)N1[C@H](C(N[C@@H](C)C2=CC=C(C=C2)C3=C(C)N=CS3)=O)C[C@@H](O)C1
Application
(S,R,S)-AHPC-Me is a VH032 derivative used in the recruitment of the von Hippel-Lindau (VHL) protein for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This was previously listed under ATEH961B8E6E.
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Targeted protein degradation
Other Notes
Discovery of ERD-308 as a highly potent proteolysis targeting chimera (PROTAC) degrader of estrogen receptor (ER)
Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer
Design, Synthesis, and Biological Evaluation of MEK PROTACs
Antibody–PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4
Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader
Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity
Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression
A caged E3 ligase ligand for PROTAC-mediated protein degradation with light
Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs
Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer
Design, Synthesis, and Biological Evaluation of MEK PROTACs
Antibody–PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4
Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader
Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity
Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression
A caged E3 ligase ligand for PROTAC-mediated protein degradation with light
Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs
Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
related product
Referencia del producto
Descripción
Precios
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificados de análisis (COA)
Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»
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Marı A Maneiro et al.
ACS chemical biology, 15(6), 1306-1312 (2020-04-28)
Targeting protein degradation with Proteolysis-Targeting Chimeras (PROTACs) is an area of great current interest in drug discovery. Nevertheless, although the high effectiveness of PROTACs against a wide variety of targets has been established, most degraders reported to date display limited
Jiantao Hu et al.
Journal of medicinal chemistry, 62(3), 1420-1442 (2019-04-17)
The estrogen receptor (ER) is a validated target for the treatment of estrogen receptor-positive (ER+) breast cancer. Here, we describe the design, synthesis, and extensive structure-activity relationship (SAR) studies of small-molecule ERα degraders based on the proteolysis targeting chimeras (PROTAC)
Cyrille S Kounde et al.
Chemical communications (Cambridge, England), 56(41), 5532-5535 (2020-04-17)
With the intent of achieving greater spatiotemporal control of PROTAC-induced protein degradation, a light-activated degrader was designed by photocaging an essential E3 ligase binding motif in a BRD4 targeting PROTAC. Proteolysis was triggered only after a short irradiation time, the
Stefan Vollmer et al.
Journal of medicinal chemistry, 63(1), 157-162 (2019-12-06)
PROteolysis TArgeting Chimeras (PROTACs) targeting the degradation of MEK have been designed based on allosteric MEK inhibitors. Inhibition of the phosphorylation of ERK1/2 was less effective with the PROTACs than a small-molecule inhibitor; the best PROTACs, however, were more effective
Mingliang Wang et al.
Journal of medicinal chemistry, 63(14), 7510-7528 (2020-05-22)
Src homology 2 domain-containing phosphatase 2 (SHP2) is an attractive therapeutic target for human cancers and other human diseases. Herein, we report our discovery of potent small-molecule SHP2 degraders whose design is based upon the proteolysis-targeting chimera (PROTAC) concept. This
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