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Referencia número: 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).

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₅₁H₅₄N₈O₉
Peso molecular:923.02

Almacenamiento:

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

Actividad biológica
- Descripciòn
- In Vitro
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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).

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas Epigenetic Reader Domain :

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

Peso molecular 923.02
Fòrmula 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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (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)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Calculators

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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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100 mg

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EBET-1055

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas Epigenetic Reader Domain

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

EBET-1055 Related Classifications

HY-161346 Related Classifications