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BioChemicals
dBET1
tcsc0021961
dBET1
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AVAILABLE SIZES
2mg
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$
137.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Western blot (WB)
Immunohistochemistry (IHC)
Immunofluorescence (IF)
Immunocytochemistry (ICC)
Immunoprecipitation (IP)
Co-Immunoprecipitation (CoIP)
Chromatin Immunoprecipitation (ChIP)
RNA Binding Protein Immunoprecipitation (RIP)
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Product Description
dBET1 is a potent
BRD4
protein degrader based on
PROTAC
technology with an
EC
50
of 430 nM.
IC50 & Target: EC
50
: 430 nM (BRD4)
[1]
In Vitro:
Treatment with dBET1 down regulates
MYC
and
PIM1
transcription. Degradation of BRD4 by dBET1 is associated with a more potent apoptotic consequence in MV4;11 cell line. Significantly increased apoptosis after only 4 h of dBET1 treatment is enhanced at 8 h. dBET1 also induces a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC
50
= 0.14 μM, compare to IC
50
= 1.1 μM with JQ1)
[1]
.
In Vivo:
Administration of dBET1 attenuates tumor progression as determined by serial volumetric measurement, and decreases tumor weight assessed post-mortem. Acute pharmacodynamic degradation of BRD4 is observed four hours after a first or second daily treatment with dBET1 (50 mg/kg IP). A statistically significant destabilization of BRD4, down regulation of MYC and inhibition of proliferation is observed with dBET1 compare to vehicle control in excised tumors. Two weeks of dBET1 is well tolerated by mice without a meaningful effect on weight, white blood count, hematocrit or platelet count
[1]
.
Information
CAS No
1799711-21-9
Formula
C
38
H
37
ClN
8
O
7
S
Clinical Information
clinicalinformation
Pathway
Epigenetics
PROTAC
Target
Epigenetic Reader Domain
PROTAC
Specifications
Purity / Grade
>98%
Solubility
10 mM in DMSO
Smiles
smiles
Misc Information
Observed Molecular Weight
785.27
related data
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