1. Antibody-drug Conjugate/ADC Related Epigenetics
  2. Epigenetic Reader Domain ADC Cytotoxin
  3. EBET-1055

EBET-1055 is a bromodomain and extra-terminal (BET) protein degrader (EBET) composed of a BET inhibitor (EBET-590, HY-161387), an E3 ubiquitin ligase ligand and connectors. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures.

For research use only. We do not sell to patients.

EBET-1055 Chemical Structure

EBET-1055 Chemical Structure

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Description

EBET-1055 is a bromodomain and extra-terminal (BET) protein degrader (EBET) composed of a BET inhibitor (EBET-590, HY-161387), an E3 ubiquitin ligase ligand and connectors. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures[1].

In Vitro

EBET-1055 (1 nM, 10 nM; 2 d) inhibits CAF-induced IL-6 and LIF secretion when co-cultured with mouse CAF and PC-3 or PC-42 cancer cells[1].br /EBET-1055 has potential anti-inflammatory or anti-fibrotic activity. STAT3 signaling mediates the inflammatory CAF (iCAF) phenotype, and SMAD signaling mediates the myofibroblast CAF (myCAF) phenotype; and EBET-1055 (1-100 nM; 24 h) may inhibit the interaction of BRD proteins with STAT3 and SMAD3 It inhibits myofibroblast differentiation and reduces the phosphorylation levels of SMAD3 and STAT3 in mouse fibrotic kidneys[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

923.02

Formula

C51H54N8O9

SMILES

OC[C@](OC1CC1)(C2=CC=CC=C2)C3=NC(N4CCC(CN5CCN(C(COC6=CC=CC(C(N7C8CCC(NC8=O)=O)=O)=C6C7=O)=O)CC5)CC4)=NC9=CC=C(C(C=C%10C)=CN(C)C%10=O)C=C93

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
EBET-1055
Cat. No.:
HY-161346
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