Name: PROTAC CBP/P300 Degrader-1
Brand: BOC Sciences
Rating: 5 (1 reviews)

Size

Price

Stock

Quantity

$--

In stock

Purity

≥95%

Solubility

DMSO: 173.33 mg/mL (193.89 mM; Need ultrasonic)

Appearance

Solid

Storage

Store at -20°C, sealed storage, away from moisture and light

IUPACName

3-[7-(difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-1-[1-[6-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]hexanoyl]piperidin-4-yl]-N-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide

Synonyms

5H-Pyrazolo[4,3-c]pyridine-5-carboxamide, 3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1-[1-[6-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-1-oxohexyl]-4-piperidinyl]-1,4,6,7-tetrahydro-N-methyl-

InChI Key

KOXRGDZBEAJAKE-UHFFFAOYSA-N

InChI

InChI=1S/C46H53F2N11O6/c1-49-46(65)56-21-16-35-33(26-56)42(57-18-7-8-27-22-31(28-24-51-54(2)25-28)32(41(47)48)23-37(27)57)53-59(35)29-14-19-55(20-15-29)39(61)11-4-3-5-17-50-34-10-6-9-30-40(34)45(64)58(44(30)63)36-12-13-38(60)52-43(36)62/h6,9-10,22-25,29,36,41,50H,3-5,7-8,11-21,26H2,1-2H3,(H,49,65)(H,52,60,62)

SMILES

CNC(=O)N1CCC2=C(C1)C(=NN2C3CCN(CC3)C(=O)CCCCCNC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O)N7CCCC8=CC(=C(C=C87)C(F)F)C9=CN(N=C9)C

Mechanism

Target: Targets CBP and p300 bromodomain acetyltransferase paralogs for experimental targeted protein degradation studies.

Binding Site: Binds the CBP/p300 bromodomain acetyl-lysine pocket and cereblon ligand module to support productive ternary complex formation.

Mechanism of Action: PROTAC CBP/P300 Degrader-1 is designed for use in PROTAC or targeted protein degradation experiments directed toward CBP and p300 bromodomain acetyltransferase paralogs. 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 CBP/P300 Degradation: This application focuses on utilizing PROTAC CBP/P300 Degrader-1 to selectively degrade CBP and P300 proteins, which are crucial coactivators in transcription regulation. This approach enables researchers to dissect the role of these proteins in gene expression and their implications in various diseases.

• Epigenetic Modulation via Targeted Degradation: By employing PROTAC CBP/P300 Degrader-1, researchers can achieve targeted degradation of CBP/P300, offering a powerful tool for studying epigenetic modifications. This application facilitates the exploration of transcriptional changes and chromatin dynamics influenced by these coactivators.

• Cancer Research and Targeted Degradation: PROTAC CBP/P300 Degrader-1 serves as an invaluable resource in cancer research, enabling the targeted degradation of CBP/P300 to investigate their roles in oncogenesis. This application aids in elucidating potential therapeutic targets for cancers driven by aberrant transcriptional coactivation.

• Mechanistic Studies of Transcriptional Regulation: The targeted degradation of CBP/P300 using PROTAC CBP/P300 Degrader-1 allows for detailed studies of transcriptional regulation mechanisms. Researchers can utilize this tool to understand the interplay between coactivators and other transcription factors in cellular processes.

Stock concentration: *

Desired final volume: *

Desired concentration: *

* 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