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dBET6

Catalog No. T5130   CAS 1950634-92-0

dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
dBET6 Chemical Structure
dBET6, CAS 1950634-92-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
5 mg In stock $ 98.00
10 mg In stock $ 172.00
25 mg In stock $ 323.00
50 mg In stock $ 518.00
100 mg In stock $ 749.00
200 mg In stock $ 945.00
500 mg In stock $ 1,380.00
1 mL * 10 mM (in DMSO) In stock $ 159.00
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Purity: 99.12%
Purity: 98.76%
Purity: 97.57%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
Targets&IC50 BET:14 nM
In vitro dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4.
In vivo dBET6 (7.5 mg/kg, p.o., BID) decreases the leukemic burden in a disseminated mouse model of T-ALL.
Animal Research MOLT4 human T-ALL cells are intravenously injected into NSG mice (2×106 cells/mouse). Luminescence is utilized to monitor engraftment (evident at day 6), at which point mice are randomized into three cohorts that receive dBET6 (7.5 mg/kg BID, n = 8), JQ1 (20 mg/kg QD, n = 9) or vehicle (captisol, n = 9) treatment for 14 days. Survival of all three cohorts is subsequently monitored using hind limb paralysis caused by a high femoral leukemic burden as a defined endpoint. SUPT11 human T-ALL cells (mCherry+ and Luciferase+) are intravenously injected into NSG mice (2.52×106 cells/mouse). Luminescence is used to monitor successful engraftment, occurring 10 days after injection. At this point, animals are randomized into three cohorts that receive dBET6 (7.5 mg/kg BID, n = 7), JQ1 (7.5 mg/kg BID, n = 7) or vehicle (captisol, n = 7) treatment for 18 days. Treatment burden is assessed via total body luminescence imaging as well as by bone marrow infiltration by mCherry+ T-ALL cells.
Molecular Weight 841.37
Formula C42H45ClN8O7S
CAS No. 1950634-92-0

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mM

TargetMolReferences and Literature

1. Winter GE, et al. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. Mol Cell. 2017 Jul 6;67(1):5-18.e19.

TargetMolCitations

1. Shi Y, Liao Y, Liu Q, et al.BRD4-targeting PROTAC as a unique tool to study biomolecular condensates.Cell Discovery.2023, 9(1): 1-13.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Bioactive Compound Library PPI Inhibitor Library Histone Modification Compound Library Anti-Cancer Compound Library Reprogramming Compound Library Bioactive Compounds Library Max Glutamine Metabolism Compound Library Target-Focused Phenotypic Screening Library Epigenetics Compound Library

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Keywords

dBET6 1950634-92-0 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain dBET-6 PROTACs Inhibitor inhibit dBET 6 inhibitor

 

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