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Chromatin/Epigenetic Epigenetic Reader Domain dBET6

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.

dBET6, CAS 1950634-92-0
Pack Size Availability Price/USD Quantity
1 mg In stock 52.00
5 mg In stock 136.00
10 mg In stock 223.00
25 mg In Stock 450.00
1 mL * 10 mM (in DMSO) In stock 159.00
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Purity 98.76%
Purity 99.12%
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
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) reduces 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

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References 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.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-cancer Compound Library Apoptosis Compound Library Epigenetics Compound Library Anti-cancer Metabolism Compound Library Anti-aging Compound Library Anti-cancer Active Compound library PPI Inhibitors Library Target-Focused Phenotypic Screening Library Ubiquitination Compound Library Anti-COVID-19 Compound Library 3CLpro-Targeted compound library (CADD) ACE2-Targeted compound library (CADD) RBD-Targeted compound library (CADD) nsp16-Targeted compound library (CADD) PLpro-Targeted compound library (CADD) X Domain-Targeted compound library (CADD) Glutamine Metabolism Compound Library

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