929360
Opto-pomalidomide
≥95%
别名:
4,5-Dimethoxy-2-nitrobenzyl 3-(4-amino-1,3-dioxoisoindolin-2-yl)-2,6-dioxopiperidine-1-carboxylate
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关于此项目
ligand
pomalidomide
Quality Level
assay
≥95%
form
powder
storage temp.
2-8°C
SMILES string
NC1=C2C(C(N(C2=O)C3C(N(C(CC3)=O)C(OCC4=C(C=C(C(OC)=C4)OC)[N+]([O-])=O)=O)=O)=O)=CC=C1
InChI
1S/C23H20N4O10/c1-35-16-8-11(15(27(33)34)9-17(16)36-2)10-37-23(32)26-18(28)7-6-14(21(26)30)25-20(29)12-4-3-5-13(24)19(12)22(25)31/h3-5,8-9,14H,6-7,10,24H2,1-2H3
InChI key
VIMWIXPVAGZBOD-UHFFFAOYSA-N
Application
Protein degrader building block Opto-pomalidomide enables the synthesis of molecules for light-induced targeted protein degradation and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a Cereblon (CRBN) recruiting ligand, a rigid linker, and a nitroveratryloxycarbonyl group that can undergo photolysis to form a pendant amine for reactivity with a carboxylic acid on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and degrader, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, parallel synthesis can be used to more quickly generate degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
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Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
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Other Notes
Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
signalword
Danger
hcodes
Hazard Classifications
Repr. 1B
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Jing Liu et al.
Science advances, 6(8), eaay5154-eaay5154 (2020-03-05)
By hijacking endogenous E3 ligase to degrade protein targets via the ubiquitin-proteasome system, PROTACs (PRoteolysis TArgeting Chimeras) provide a new strategy to inhibit protein targets that were regarded as undruggable before. However, the catalytic nature of PROTAC potentially leads to
Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of
Kedra Cyrus et al.
Molecular bioSystems, 7(2), 359-364 (2010-10-06)
Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| 929360-50MG | 04065268454091 |