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924997

Sigma-Aldrich

E7820-C9-NH2 hydrochloride

Synonym(s):

N-(9-Aminononyl)-3-(N-(3-cyano-4-methyl-1H-indol-7-yl)sulfamoyl)benzamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, DCAF15 protein degrader building block

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About This Item

Empirical Formula (Hill Notation):
C26H33N5O3S · xHCl
Molecular Weight:
495.64 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.22

Pricing and availability is not currently available.

ligand

E7820

Quality Level

reaction suitability

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

functional group

amine

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This Item
151367312492427
grade

analytical standard

grade

analytical standard

grade

analytical standard

grade

analytical standard

technique(s)

HPLC: suitable, gas chromatography (GC): suitable

technique(s)

HPLC: suitable, gas chromatography (GC): suitable

technique(s)

HPLC: suitable, gas chromatography (GC): suitable

technique(s)

HPLC: suitable, gas chromatography (GC): suitable

application(s)

cleaning products
cosmetics
food and beverages
personal care

application(s)

cleaning products
cosmetics
food and beverages
personal care

application(s)

cleaning products
cosmetics
food and beverages
personal care

application(s)

cleaning products
cosmetics
food and beverages
personal care

format

neat

format

neat

format

neat

format

neat

assay

≥98.5% (GC)

assay

≥97.0% (HPLC)

assay

≥90% (HPLC)

assay

≥95.0% (HPLC)

shelf life

limited shelf life, expiry date on the label

shelf life

-

shelf life

limited shelf life, expiry date on the label

shelf life

-

Application

Protein degrader building block E7820-C9-NH2 hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a DCAF15-recruiting ligand E7820 (SML2950), an alkyl 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.

Protein Degrader Building Blocks

Technology Spotlight: DCAF15 Degrader Building Blocks for Targeted Protein Degradation

Legal Information

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

related product

Product No.
Description
Pricing

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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    In vivo target protein degradation induced by PROTACs based on E3 ligase DCAF15.
    Liang Li et al.
    Signal transduction and targeted therapy, 5(1), 129-129 (2020-07-28)
    Tasuku Ishida et al.
    SLAS discovery : advancing life sciences R & D, 26(4), 484-502 (2020-11-05)
    Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are a new modality of chemical tools and potential therapeutics to understand and treat human disease. A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to

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