Accéder au contenu
MilliporeSigma

Principaux documents

Voir toute la documentation

SML2687

dBET1

≥98% (HPLC)

Synonyme(s) :

(6S)-4-(4-Chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 2-((S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-(2-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yloxy)acetamido)butyl)acetamide

Se connecter pour consulter les tarifs organisationnels et contractuels.

Sélectionner une taille de conditionnement

Changer de vue

A propos de cet article

Formule empirique (notation de Hill) :
C38H37ClN8O7S
Numéro CAS:
1799711-21-9
Poids moléculaire :
785.27
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD31544503
Assay:
≥98% (HPLC)
Form:
powder
Service technique
Besoin d'aide ? Notre équipe de scientifiques expérimentés est là pour vous.
Laissez-nous vous aider

ligand

thalidomide

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

[s]1c2c(c(c1C)C)C(=N[C@H](c7[n]2c(nn7)C)CC(=O)NCCCCNC(=O)COc4c5c(ccc4)C(=O)N(C5=O)C6CCC(=O)NC6=O)c3ccc(cc3)Cl

InChI key

LKEGXJXRNBALBV-PMCHYTPCSA-N

Biochem/physiol Actions

A JQ1-and-phthalimide conjugate that causes the degradation of BRD4 protein
dBET1 is a JQ1-and-phthalimide conjugate that causes the degradation of BRD4 protein, a transcriptional coactivator that regulates the expression of genes that promote cancer cell proliferation and survival. JQ1 is a selective BET bromodomain (BRD) inihbitor. The phthalimide portion is a derivative of the drug thalidomide, which is known to bind to cereblon (CRBN), part of an ubiquitin E3 ligase complex resulting in ubiquitylation and degradation by the proteasome. The conjugate dBET1 induced highly selective cereblon-dependent BET protein degradation both in vitro and in vivo. It induced complete CRBN-dependent proteosomal degradation of BRD4 in a human acute myeloid leukaemia (AML) cell line and delayed leukemia progression in mice.

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Faites votre choix parmi les versions les plus récentes :

Certificats d'analyse (COA)

Lot/Batch Number

It looks like we've run into a problem, but you can still download Certificates of Analysis from our Documents section.

Si vous avez besoin d'assistance, veuillez contacter Service Clients

Déjà en possession de ce produit ?

Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

Afua A Akuffo et al.
The Journal of biological chemistry, 293(16), 6187-6200 (2018-02-17)
Upon binding to thalidomide and other immunomodulatory drugs, the E3 ligase substrate receptor cereblon (CRBN) promotes proteosomal destruction by engaging the DDB1-CUL4A-Roc1-RBX1 E3 ubiquitin ligase in human cells but not in mouse cells, suggesting that sequence variations in CRBN may
Georg E Winter et al.
Science (New York, N.Y.), 348(6241), 1376-1381 (2015-05-23)
The development of effective pharmacological inhibitors of multidomain scaffold proteins, notably transcription factors, is a particularly challenging problem. In part, this is because many small-molecule antagonists disrupt the activity of only one domain in the target protein. We devised a
Kelly M DeMars et al.
Neurochemistry international, 127, 94-102 (2019-03-16)
Neuroinflammation after stroke significantly contributes to neuronal cell death. Bromodomain and Extra Terminal Domain (BET) proteins are essential to inflammatory gene transcription. BET proteins (BRD2, BRD3, BRD4, and BRDT) have varied effects including chromatin remodeling, histone acetyltransferase activity, and as