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915572

Sigma-Aldrich

Pomalidomide-dipiperazine-NH2 hydrochloride

≥95%

Synonym(s):

4-(4-(4-(2-Aminoethyl)piperazine-1-carbonyl)piperazin-1-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride, Crosslinker−E3 ligase ligand conjugate, Pomalidomide conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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About This Item

Empirical Formula (Hill Notation):
C24H31N7O5 · xHCl
Molecular Weight:
497.55 (free base basis)
UNSPSC Code:
12352101
NACRES:
NA.22

ligand

pomalidomide

Quality Level

100

Assay

≥95%

form

powder

reaction suitability

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

functional group

amine

storage temp.

2-8°C

SMILES string

O=C(N(C1CCC(NC1=O)=O)C2=O)C3=C2C=CC=C3N4CCN(C(N5CCN(CCN)CC5)=O)CC4

Related Categories

Application

Protein degrader building block Pomalidomide-dipiperazine-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a rigid linker, and a pendant amine for reactivity with an acid on the target warhead. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, 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 PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Other Notes

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC® Degraders for Targeted Protein Degradation

Targeted Protein Degradation by Small Molecules

Small-Molecule PROTACS: New Approaches to Protein Degradation

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Legal Information

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

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Pomalidomide-PEG5-CO2H, ≥95%

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Pomalidomide-PEG4-CO2H

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(S,R,S)-AHPC-PEG6-NH2 hydrochloride, ≥95%

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(S,R,S)-AHPC-PEG4-Alkyne

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(S,R,S)-AHPC-PEG5-NH2 hydrochloride

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(S,R,S)-AHPC-PEG4-NH2 hydrochloride, ≥95%

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(S,R,S)-AHPC-PEG3-azide, ≥95%

904724

Pomalidomide-PEG2-butyl iodide, ≥95%

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(S,R,S)-AHPC-PEG2-azide

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(S,R,S)-AHPC-C6-PEG3-butyl azide, ≥95%

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(S,R,S)-AHPC-C6-PEG1-C3-PEG1-butyl azide, ≥95%

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Pomalidomide-C6-PEG1-C3-PEG1-butyl iodide, ≥95%

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6F,C5-Pomalidomide-4-piperidine-C1-piperazine hydrochloride

923931

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5-Amino-Thalidomide, ≥95%

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Articles

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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