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919403

Sigma-Aldrich

CCW16-C4-BocNH

95%

Szinonimák:

tert-Butyl (4-(4-(4-(N-benzyl-2-chloroacetamido)phenoxy)phenoxy)butyl)carbamate, Crosslinker-E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, RNF4-targeting building block, Template for synthesis of targeted protein degrader

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Összes fotó(2)

About This Item

Tapasztalati képlet (Hill-képlet):
C30H35ClN2O5
CAS-szám:
2361139-85-5
Molekulatömeg:
539.06
MDL-szám:
MFCD34166219
NACRES:
NA.22

ligand

CCW16

Minőségi szint

100

Teszt

95%

Forma

viscous liquid

reakcióalkalmasság

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

funkcionális csoport

amine

tárolási hőmérséklet

2-8°C

SMILES string

O=C(CCl)N(CC1=CC=CC=C1)C2=CC=C(C=C2)OC3=CC=C(OCCCCNC(OC(C)(C)C)=O)C=C3

InChI

1S/C30H35ClN2O5/c1-30(2,3)38-29(35)32-19-7-8-20-36-25-15-17-27(18-16-25)37-26-13-11-24(12-14-26)33(28(34)21-31)22-23-9-5-4-6-10-23/h4-6,9-18H,7-8,19-22H2,1-3H3,(H,32,35)

Alkalmazás

Protein degrader builiding block CCW16-C4-BocNH enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a RING finger protein 4 (RNF4)-recruiting ligand, an alkyl-chain crosslinker, 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 PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Egyéb megjegyzések

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC® Degraders for Targeted Protein Degradation

Targeted Protein Degradation by Small Molecules

Jogi információk

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

kapcsolódó termék

Product No.
Leírás
Árazás

901500

Pomalidomide-C3-CO2H, ≥95%

911658

Pomalidomide-C3-NH2 hydrochloride, ≥95%

911704

C5 Lenalidomine-C3-NH2 hydrochloride, ≥95%

919438

CCW16-C9-BocNH, ≥95%

919470

CCW16-PEG2-butyl-BocNH, ≥95%

919462

CCW16-PEG5-BocNH, ≥95%

919454

CCW16-PEG3-BocNH, ≥95%

919446

CCW16-PEG1-BocNH

919489

CCW16-C6-PEG3-butyl-BocNH

919411

CCW16-C6-BocNH

919381

CCW16, ≥95%

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable

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Analitikai tanúsítványok (COA)

Lot/Batch Number

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Dokumentumtár megtekintése

Carl C Ward et al.
ACS chemical biology, 14(11), 2430-2440 (2019-05-07)
Targeted protein degradation has arisen as a powerful strategy for drug discovery allowing the targeting of undruggable proteins for proteasomal degradation. This approach most often employs heterobifunctional degraders consisting of a protein-targeting ligand linked to an E3 ligase recruiter to
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
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
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

Cikkek

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.

Tudóscsoportunk valamennyi kutatási területen rendelkezik tapasztalattal, beleértve az élettudományt, az anyagtudományt, a kémiai szintézist, a kromatográfiát, az analitikát és még sok más területet.

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