929433

Opto-pomalidomide-C₂-NH₂ hydrochloride

≥95%

• Synonyma: 4,5-Dimethoxy-2-nitrobenzyl 3-(4-((2-aminoethyl)amino)-1,3-dioxoisoindolin-2-yl)-2,6-dioxopiperidine-1-carboxylate hydrochloride
• Empirický vzorec (Hillův zápis): C₂₅H₂₅N₅O₁₀ · xHCl
• Molekulová hmotnost: 555.49 (free base basis)
• UNSPSC Code: 12352101
• NACRES: NA.21

Vlastnosti

• ligand: pomalidomide
• Quality Segment: 100
• assay: ≥95%
• form: powder
• technique(s): targeted protein degradation: suitable
• functional group: amine
• storage temp.: 2-8°C
• SMILES string: COC1=CC(COC(N2C(CCC(N3C(C4=CC=CC(NCCN)=C4C3=O)=O)C2=O)=O)=O)=C(C=C1OC)[N+]([O-])=O
• InChI: 1S/C25H25N5O10/c1-38-18-10-13(17(30(36)37)11-19(18)39-2)12-40-25(35)29-20(31)7-6-16(23(29)33)28-22(32)14-4-3-5-15(27-9-8-26)21(14)24(28)34/h3-5,10-11,16,27H,6-9,12,26H2,1-2H3
• InChI key: QEGZOUGKLQLVHL-UHFFFAOYSA-N

Popis

Application

Protein degrader building block Opto-pomalidomide-C₂-NH₂ hydrochloride 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 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

Other Notes

Impact of linker length on the activity of PROTACs

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Small-Molecule PROTACS: New Approaches to Protein Degradation

Light-induced control of protein destruction by opto-PROTAC

Targeted Protein Degradation by Small Molecules

Legal Information

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

Bezpečnostní informace

• Piktogramy: GHS08
• Výstražné slovo: Danger
• Kódy nebezpečí: H360D
• Bezpečnostní pokyny: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Hazard Classifications: Repr. 1B
• Skladovací třída: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Co se děje?: WGK 3
• Bod vzplanutí (°F): Not applicable
• Bod vzplanutí (°C): Not applicable