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Formula | C42H45ClN8O7S |
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Molecular Weight | 841.37 | CAS No. | 1950634-92-0 | ||||
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (118.85 mM) | ||||
Ethanol | 33 mg/mL (39.22 mM) | ||||||
Water | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis. | ||
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Targets |
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In vitro | dBET6 is a highly cell-permeable degrader of BET bromodomains. It is potent in most cancer cell lines. dBET6 features highly increased cellular potency with evident degradation in the sub-nanomolar range. Treatment with 100 nM dBET6 leads to degradation of BRD4 after 1 hr, prompting subsequent downregulation of c-MYC and induction of apoptosis. dBET6 disrupts global productive transcription elongation. dBET6 treatment leads to a widespread decrease in steady-state mRNA levels, but observed an incommensurate impact on expression of members of the core regulatory circuitry of leukemogenic transcription factors. The collapse of the core transcriptional machinery prompted by BET degradation precedes a robust apoptotic response, of apparent translational significance[1]. |
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In vivo | dBET6 is well tolerated. Upon dBET6 treatment, a significant reduction of leukemic burden is observed in a disseminated mouse model of T-ALL. Moreover, mice treated with dBET6 (7.5 mg/kg BID) exhibits a significant survival benefit compared to mice treated with vehicle control or JQ1 (20 mg/kg QD)[1]. |
Cell Assay: |
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Animal Study: |
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Cell-type-specific tumour sensitivity identified with a bromodomain targeting PROTAC in adenoid cystic carcinoma [ J Pathol, 2024, 262(1):37-49] | PubMed: 37792636 |
Increased expression of BRD4 isoforms long (BRD4-L) and short (BRD4-S) promotes chemotherapy resistance in high-grade serous ovarian carcinoma [ Genes Cancer, 2023, 10.18632/genesandcancer.233] | PubMed: 37705995 |
Increased expression of BRD4 isoforms long (BRD4-L) and short (BRD4-S) promotes chemotherapy resistance in high-grade serous ovarian carcinoma [ Genes Cancer, 2023, 14:56-76] | PubMed: 37705995 |
BRD2 inhibition blocks SARS-CoV-2 infection by reducing transcription of the host cell receptor ACE2 [ Nat Cell Biol, 2022, 24(1):24-34] | PubMed: 35027731 |
Structure-guided discovery of novel potent and efficacious proteolysis targeting chimera (PROTAC) degrader of BRD4 [ Bioorg Chem, 2021, 115:105238] | PubMed: 34390970 |
Epigenomic landscape and 3D genome structure in pediatric high-grade glioma [ Sci Adv, 2021, 7(23)eabg4126] | PubMed: 34078608 |
BRD2 inhibition blocks SARS-CoV-2 infection in vitro by reducing transcription of the host cell receptor ACE2 [ bioRxiv, 2021, 2021.01.19.427194] | PubMed: 33501440 |
Viral E Protein Neutralizes BET Protein-Mediated Post-Entry Antagonism of SARS-CoV-2 [ bioRxiv, 2021, 2021.11.14.468537] | PubMed: 34816261 |
Kinetic Detection of E3:PROTAC:Target Ternary Complexes Using NanoBRET Technology in Live Cells [ Methods Mol Biol, 2021, 2365:151-171] | PubMed: 34432243 |
ASXL3 bridges BRD4 to BAP1 complex and governs enhancer activity in small cell lung cancer [ Genome Med, 2020, 12(1):63] | PubMed: 32669118 |
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Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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