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About This Item
Empirical Formula (Hill Notation):
C38H37ClN8O7S
CAS Number:
Molecular Weight:
785.27
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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
Related Categories
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.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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