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ligand
pomalidomide
品質水準
アッセイ
≥95%
フォーム
powder
保管温度
2-8°C
SMILES記法
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
アプリケーション
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
Protein Degrader Building Blocks
Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks
その他情報
法的情報
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
シグナルワード
Danger
危険有害性情報
危険有害性の分類
Repr. 1B
保管分類コード
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
929360-50MG:
929360-VAR:
929360-BULK:
最新バージョンのいずれかを選択してください：
試験成績書（COA）
Lot/Batch Number
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
Momar Toure et al.
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is
Philipp M Cromm et al.
Cell chemical biology, 24(9), 1181-1190 (2017-06-27)
Traditional pharmaceutical drug discovery is almost exclusively focused on directly controlling protein activity to cure diseases. Modulators of protein activity, especially inhibitors, are developed and applied at high concentration to achieve maximal effects. Thereby, reduced bioavailability and off-target effects can
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