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

Size

Price

Stock

Quantity

$--

In stock

Purity

98%

Solubility

DMSO: 33.33 mg/mL (33.36 mM)

Appearance

Solid

Storage

Store at -20°C

IUPACName

2-[(2S)-4-[2-[[(2S,4R)-4-[2-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]-1-methylpyrrolidin-2-yl]methoxy]-7-naphthalen-1-yl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]-1-prop-2-enoylpiperazin-2-yl]acetonitrile

Synonyms

PROTAC K-Ras Degrader-1; 2378258-52-5; 2-[(2S)-4-[2-[[(2S,4R)-4-[2-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]-1-methylpyrrolidin-2-yl]methoxy]-7-naphthalen-1-yl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]-1-prop-2-enoylpiperazin-2-yl]acetonitrile; SCHEMBL21459082; EX-A3964; AKOS040740885; MS-31852; HY-129523; CS-0106329; 2-((2S)-1-acryloyl-4-(2-(((2S,4R)-4-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethoxy)ethoxy)-1-methylpyrrolidin-2-yl)methoxy)-7-(naphthalen-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile

InChI Key

KGFCORDWMRCVAC-VYIZRSQBSA-N

InChI

InChI=1S/C53H62N10O10/c1-3-47(65)62-22-21-61(31-36(62)16-18-54)49-40-17-20-60(44-13-6-9-35-8-4-5-10-39(35)44)33-43(40)56-53(58-49)73-34-37-30-38(32-59(37)2)72-29-28-71-27-26-70-25-24-69-23-19-55-42-12-7-11-41-48(42)52(68)63(51(41)67)45-14-15-46(64)57-50(45)66/h3-13,36-38,45,55H,1,14-17,19-34H2,2H3,(H,57,64,66)/t36-,37-,38+,45?/m0/s1

SMILES

CN1CC(CC1COC2=NC3=C(CCN(C3)C4=CC=CC5=CC=CC=C54)C(=N2)N6CCN(C(C6)CC#N)C(=O)C=C)OCCOCCOCCOCCNC7=CC=CC8=C7C(=O)N(C8=O)C9CCC(=O)NC9=O

Mechanism

Target: Targets KRAS mutant oncoproteins for experimental targeted protein degradation studies.

Binding Site: Binds the KRAS switch-II pocket and recruited E3 ligase substrate-recognition domain to support productive ternary complex formation.

Mechanism of Action: PROTAC K-Ras Degrader-1 is designed for use in PROTAC or targeted protein degradation experiments directed toward KRAS mutant oncoproteins. The bifunctional molecule links a target-recognition element to VHL, 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

• K-Ras Oncoprotein Degradation: PROTAC K-Ras Degrader-1 is designed to specifically target and degrade the K-Ras oncoprotein, a pivotal player in various cancers. This application allows researchers to explore the effects of K-Ras depletion on cancer cell signaling pathways and tumorigenesis, offering insights into potential therapeutic strategies.

• Targeted Protein Degradation Studies: Utilizing PROTAC technology, this compound facilitates the study of targeted protein degradation mechanisms. Researchers can investigate the ubiquitin-proteasome system's role in selectively degrading proteins, advancing the understanding of cellular protein homeostasis and its implications in disease.

• Signal Transduction Pathway Analysis: By degrading K-Ras, PROTAC K-Ras Degrader-1 enables detailed examination of downstream signaling pathways. This application aids in dissecting the molecular interactions and networks influenced by K-Ras, providing a deeper understanding of oncogenic signaling and potential intervention points.

• Cancer Biology Research: This PROTAC product serves as a tool for probing the biological functions of K-Ras in cancer cells. Researchers can study the impact of K-Ras degradation on cell proliferation, survival, and metastasis, contributing to the development of novel anti-cancer strategies.

Hello, I hope you can explain the machanism of action of PROTAC K-Ras Degrader-1 to me? Thanks.

E3 ubiquitin ligases are responsible for tagging proteins for degradation by the proteasome. When PROTAC K-Ras Degrader-1 binds to mutant KRAS G12C, it recruits E3 ubiquitin ligase to the mutant protein. This causes the mutant protein to be tagged for degradation by the proteasome, which leads to the inhibition of cell growth.

7/2/2018

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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