Name: PROTAC BRD9 Degrader-1
Brand: BOC Sciences
Rating: 5 (1 reviews)

Size

Price

Stock

Quantity

$--

In stock

Solubility

Soluble in DMSO (150 mg/mL; 165.93 mM; Need ultrasonic)

Storage

Store at 2-8°C for short term (days to weeks) or -20°C for long term (months to years)

Shipping

Room temperature in continental US; may vary elsewhere

IUPACName

2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxy-N-[4-[[2-[4-[2-[N-(1,1-dioxothian-4-yl)carbamimidoyl]-5-methyl-4-oxothieno[3,2-c]pyridin-7-yl]-2-methoxyphenoxy]acetyl]amino]butyl]acetamide

Synonyms

Acetamide, N-[4-[[2-[4-[4,5-dihydro-2-[imino[(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)amino]methyl]-5-methyl-4-oxothieno[3,2-c]pyridin-7-yl]-2-methoxyphenoxy]acetyl]amino]butyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-; N-[4-[[2-[4-[4,5-Dihydro-2-[imino[(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)amino]methyl]-5-methyl-4-oxothieno[3,2-c]pyridin-7-yl]-2-methoxyphenoxy]acetyl]amino]butyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetamide; 2-(4-(2-(N-(1,1-Dioxidotetrahydro-2H-thiopyran-4-yl)carbamimidoyl)-5-methyl-4-oxo-4,5-dihydrothieno[3,2-c]pyridin-7-yl)-2-methoxyphenoxy)-N-(4-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)butyl)acetamide

Density

1.56±0.1 g/cm3

InChI Key

LOLHUPGCPDURJG-UHFFFAOYSA-N

InChI

InChI=1S/C42H45N7O12S2/c1-48-20-27(37-26(40(48)54)19-32(62-37)38(43)46-24-12-16-63(57,58)17-13-24)23-8-10-29(31(18-23)59-2)60-21-34(51)44-14-3-4-15-45-35(52)22-61-30-7-5-6-25-36(30)42(56)49(41(25)55)28-9-11-33(50)47-39(28)53/h5-8,10,18-20,24,28H,3-4,9,11-17,21-22H2,1-2H3,(H2,43,46)(H,44,51)(H,45,52)(H,47,50,53)

SMILES

CN1C=C(C2=C(C1=O)C=C(S2)C(=NC3CCS(=O)(=O)CC3)N)C4=CC(=C(C=C4)OCC(=O)NCCCCNC(=O)COC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)OC

Mechanism

Target: Targets BRD9 bromodomain protein for experimental targeted protein degradation studies.

Binding Site: Binds the BRD9 acetyl-lysine recognition pocket and recruited E3 ligase ligand site to support productive ternary complex formation.

Mechanism of Action: PROTAC BRD9 Degrader-1 is designed for use in PROTAC or targeted protein degradation experiments directed toward BRD9 bromodomain protein. 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 BRD9 Degradation: This product is designed to selectively degrade the BRD9 protein, a component of the SWI/SNF chromatin remodeling complex. It enables researchers to study the functional role of BRD9 in gene regulation and its potential as a therapeutic target in diseases such as cancer.

• Targeted Protein Degradation in Epigenetic Studies: By employing PROTAC technology, this degrader facilitates the investigation of epigenetic mechanisms involving BRD9. It offers a powerful tool for dissecting the influence of chromatin remodelers on transcriptional regulation and cellular differentiation.

• Functional Genomics with PROTAC: Utilizing PROTAC BRD9 Degrader-1 allows scientists to perform functional genomics studies, providing insights into the consequences of BRD9 depletion. This approach aids in identifying novel pathways and interactions critical for cellular processes and disease pathogenesis.

• Drug Discovery and Development Applications: This PROTAC degrader serves as a valuable asset in drug discovery research, especially in validating BRD9 as a drug target. It supports the development of targeted therapeutics by enabling the exploration of BRD9's role in various pathological contexts.

1. Degradation of the BAF complex factor BRD9 by heterobifunctional ligands.

Remillard, D., Buckley, D.L., Paulk, J., Brien, G.L., Sonnett, M., Seo, H.S., Dastjerdi, S., Wühr, M., Dhe-Paganon, S., Armstrong, S.A. and Bradner, J.E., 2017. Angewandte Chemie International Edition, 56(21), pp.5738-5743.

The bromodomain-containing protein BRD9, a subunit of the human BAF (SWI/SNF) nucleosome remodeling complex, has emerged as an attractive therapeutic target in cancer. Despite the development of chemical probes targeting the BRD9 bromodomain, there is a limited understanding of BRD9 function beyond acetyl-lysine recognition. We have therefore created the first BRD9-directed chemical degraders, through iterative design and testing of heterobifunctional ligands that bridge the BRD9 bromodomain and the cereblon E3 ubiquitin ligase complex. Degraders of BRD9 exhibit markedly enhanced potency compared to parental ligands (10- to 100-fold). Parallel study of degraders with divergent BRD9-binding chemotypes in models of acute myeloid leukemia resolves bromodomain polypharmacology in this emerging drug class. Together, these findings reveal the tractability of non-BET bromodomain containing proteins to chemical degradation, and highlight lead compound dBRD9 as a tool for the study of BRD9.

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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂