Name: PROTAC CRBN Degrader-1
Brand: BOC Sciences
Rating: 5 (1 reviews)

Size

Price

Stock

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$--

In stock

Solubility

10 mM in DMSO

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Synonyms

PROTAC CRBN Degrader 1; (2S,4R)-1-[(2S)-2-[[2-[5-[2-[5-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethylamino]-2-oxoethoxy]pentoxy]ethoxy]pentoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide

InChI Key

PEZCAXDTKNFUCR-CTMFSBKBSA-N

InChI

InChI=1S/C53H72N8O13S/c1-34-46(75-33-57-34)36-16-14-35(15-17-36)29-56-48(66)41-28-37(62)30-60(41)52(70)47(53(2,3)4)58-44(65)32-74-25-10-6-8-23-72-27-26-71-22-7-5-9-24-73-31-43(64)55-21-20-54-39-13-11-12-38-45(39)51(69)61(50(38)68)40-18-19-42(63)59-49(40)67/h11-17,33,37,40-41,47,54,62H,5-10,18-32H2,1-4H3,(H,55,64)(H,56,66)(H,58,65)(H,59,63,67)/t37-,40?,41+,47-/m1/s1

SMILES

CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)COCCCCCOCCOCCCCCOCC(=O)NCCNC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O)O

Mechanism

Target: Targets cereblon (CRBN) within the CRL4CRBN E3 ligase complex for experimental targeted protein degradation studies.

Binding Site: Binds the cereblon thalidomide-binding pocket and matched cereblon-engaging degron surface to support productive ternary complex formation.

Mechanism of Action: PROTAC CRBN Degrader-1 is designed for use in PROTAC or targeted protein degradation experiments directed toward cereblon (CRBN) within the CRL4CRBN E3 ligase complex. The bifunctional molecule links a target-recognition element to cereblon, promoting proximity between the protein of interest and ubiquitination machinery. Productive ternary-complex formation can drive polyubiquitination and proteasome-dependent target depletion, allowing researchers to compare pharmacological inhibition with protein removal. It is suitable for evaluating degradation potency, kinetics, pathway selectivity, and downstream signaling consequences in engineered or disease-relevant cellular models.

Applications

• PROTAC-Mediated Protein Degradation: PROTAC CRBN Degrader-1 is engineered to facilitate the selective degradation of target proteins by recruiting them to the CRBN E3 ubiquitin ligase complex. This enables researchers to study protein function by observing the effects of targeted protein depletion in cellular models.

• Targeted Degradation in Cancer Research: Utilizing PROTAC CRBN Degrader-1 allows for the exploration of oncogenic protein degradation pathways. Researchers can investigate the potential of degrading specific cancer-related proteins to understand their roles in tumor progression and identify novel therapeutic targets.

• Mechanistic Studies of E3 Ligase Activity: By employing PROTAC CRBN Degrader-1, scientists can delve into the mechanistic aspects of E3 ligase function. This includes elucidating the dynamics of ubiquitination processes and the subsequent proteasomal degradation of targeted proteins, enhancing our understanding of cellular protein homeostasis.

• Drug Resistance Mechanism Exploration: PROTAC CRBN Degrader-1 serves as a valuable tool for studying mechanisms of drug resistance. Researchers can evaluate how the degradation of resistance-associated proteins affects cellular sensitivity to various therapeutic agents, aiding in the development of more effective treatment strategies.

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* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂