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Merck
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資料

安全性情報

923931

Sigma-Aldrich

Pomalidomide-4-piperidine-C1-piperazine hydrochloride

別名:

2-(2,6-Dioxopiperidin-3-yl)-4-(4-(piperazin-1-ylmethyl)piperidin-1-yl)isoindoline-1,3-dione hydrochloride, Crosslinker−E3 ligase ligand conjugate, Protein degrader building block

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About This Item

実験式（ヒル表記法）:
C23H29N5O4 · xHCl
分子量:
439.51 (free base basis)
NACRES:
NA.21

ligand

pomalidomide

品質水準

100

反応適合性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能基

amine

保管温度

2-8°C

SMILES記法

O=C1C(N2C(C(C=CC=C3N(CC4)CCC4CN5CCNCC5)=C3C2=O)=O)CCC(N1)=O.Cl

アプリケーション

Protein degrader building block Pomalidomide-4-piperidine-C1-piperazine hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a Cereblon (CRBN) recruiting ligand, a rigid linker, and 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

その他情報

Targeted Protein Degradation by Small Molecules

Small-Molecule PROTACS: New Approaches to Protein Degradation

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Impact of linker length on the activity of PROTACs

法的情報

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

関連製品

製品番号
詳細
価格

911771

Lenalidomide-Photoswitch1-NH2 hydrochloride, ≥95%

911763

C5 Lenalidomide-PEG1-piperazine hydrochloride, ≥95%

915572

Pomalidomide-dipiperazine-NH2 hydrochloride, ≥95%

916536

Pomalidomide-piperazine-pyridine-alkyne-NH2 hydrochloride

917729

C5 Lenalidomide-piperazine-pyridine-alkyne-NH2 hydrochloride, ≥95%

919357

(S,R,S)-AHPC-PEG1-piperazine hydrochloride, ≥95%

918350

C5 Lenalidomide-alkyne-piperidine hydrochloride, ≥95%

918687

(S,R,S)-AHPC-alkyne-piperidine hydrochloride

919896

C5 Lenalidomide-dipiperazine-NH2 hydrochloride

920606

(S,R,S)-AHPC-piperazine-pyridine-alkyne-NH2 hydrochloride

920746

Pomalidomide-benzyl-piperazine hydrochloride

920762

(S,R,S)-AHPC-benzyl-piperazine hydrochloride

920754

C5 Lenalidomide-benzyl-piperazine hydrochloride

920789

Pomalidomide-pyridine-PEG1-piperazine hydrochloride

920797

C5 Lenalidomide-pyridine-PEG1-piperazine hydrochloride, ≥95%

920800

C5 Lenalidomide-methylamino-PEG1-NH2 hydrochloride, ≥95%

920843

(S,R,S)-VL285 Phenol-PEG1-piperazine hydrochloride

920827

(S,R,S)-AHPC-methylamino-PEG1-NH2 hydrochloride

921300

C5 Lenalidomide-pyrimidine-piperazine-PEG1-NH2 hydrochloride, ≥95%

921319

Pomalidomide-methylamino-PEG1-NH2 hydrochloride

921432

(S,R,S)-AHPC-pyridine-PEG1-piperazine hydrochloride

922153

(S,R,S)-VL285 Phenol-C3-piperazine hydrochloride

922161

(S,R,S)-VL285 Phenol-methylamino-PEG1-NH2 hydrochloride

921939

(S,R,S)-AHPC-pyrimidine-piperazine-PEG1-NH2 hydrochloride

ピクトグラム

Health hazard
GHS08

シグナルワード

Danger

危険有害性情報

H360D

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

923931-50MG:
923931-VAR:
923931-BULK:

試験成績書（COA）

製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。

以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

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
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
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
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

資料

標的タンパク質分解のための分解物ビルディングブロック

タンパク質分解誘導化合物ビルディングブロックは、標的リガンドと共有結合するペンダント基を持つクロスリンカー-E3リガンド複合体です。

Degrader Building Blocks for Targeted Protein Degradation

Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

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