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Cat. No.: HY-161346

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EBET-1055

EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. 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.
(Pink: BET ligand (HY-161387); Blue: Cereblon ligand (HY-14658); Black: linker).

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

Formula: C₅₁H₅₄N₈O₉
Molecular Weight:923.02

Storage:

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

Data Sheet (268 KB)

EBET-1055 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. 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]. (Pink: BET ligand (HY-161387); Blue: Cereblon ligand (HY-14658); Black: linker).

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

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.

Western Blot Analysis^[1]

Cell Line:

PC-3 cells or mouse CAFs
Concentration:

0.1, 1, 10, 100 nM
Incubation Time:

24 h
Result:

Decreased the phosphorylation levels of STAT3Y705, SMAD2S465/467, and SMAD3S423/425 24 h after addition.

Chemical Information

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Nakazawa Y, et al. Delivery of a BET protein degrader via a CEACAM6-targeted antibody-drug conjugate inhibits tumour growth in pancreatic cancer models. Nat Commun. 2024 Mar 11;15(1):2192. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References

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EBET-1055

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EBET-1055 Related Classifications

HY-161346 Related Classifications