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Cat. No.: HY-188148

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ETS transcription factor-IN-1

ETS transcription factor-IN-1 is an inhibitor of ETS transcription factor. ETS transcription factor-IN-1 blocks the binding of the ETS DNA-binding domain to consensus ETS DNA-binding sites, thereby inhibiting the function of ETS transcription factors such as ETV6, ERG, and FLI1. ETS transcription factor-IN-1 inhibits angiogenesis and tumor cell proliferation in cancer cell lines with ETS abnormalities. ETS transcription factor-IN-1 can be used in research related to prostate cancer and breast cancer.

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

CAS No.: 158437-84-4
Formula: C₂₄H₂₅F₂N₅O
Molecular Weight:437.49

Storage:

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

ETS transcription factor-IN-1 Chemical Structure

CAS No.: 158437-84-4

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

All DNA/RNA Synthesis Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
VCaP	IC50	1-10 μM	Inhibition of proliferation of human VCaP prostate carcinoma cells assessed as reduction in cell viability incubated for 5 days by Cell Titer-Blue reagent based assay. Inhibition of proliferation of human VCaP prostate carcinoma cells assessed as reduction in cell viability incubated for 5 days by Cell Titer-Blue reagent based assay.	40214124
SK-ES1	IC50	1-10 μM	Inhibition of proliferation of human SK-ES-1 Ewing sarcoma cells assessed as reduction in cell viability incubated for 5 days by Cell Titer-Blue reagent based assay. Inhibition of proliferation of human SK-ES-1 Ewing sarcoma cells assessed as reduction in cell viability incubated for 5 days by Cell Titer-Blue reagent based assay.	40214124

In Vitro

OthersAnti-cancerCardiovascular Regulation

Others

ETS transcription factor-IN-1 (compound A) (30 min) inhibits DNA binding of the ETS transcription factors ETV6, ERG, and FLI1, but not JUN^[1].

Anti-cancer

ETS transcription factor-IN-1 (1-5 μM; 5 days) significantly inhibits the proliferation of VCaP and SK-ES-1 tumor cell lines, with minimal effects on normal HUVECs^[1].

Cardiovascular Regulation

ETS transcription factor-IN-1 (5 μM; 16 h) causes minimal DNA damage in human induced pluripotent stem cell-derived cardiomyocytes^[1].

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

Cell Viability Assay^[1]

Cell Line:

VCaP, SK-ES-1, and HUVECs
Concentration:

1, 2.5, 5 μM
Incubation Time:

5 days
Result:

Significantly suppressed the proliferation of VCaP and SK-ES-1 cancer cell lines, each showing half-maximal inhibitory concentration values in the 1-10 μM range.
Did not significantly block the proliferation of normal primary HUVECs to the same degree as the tumour cells.

Immunofluorescence^[1]

Cell Line:

human-induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CM)
Concentration:

5 μM
Incubation Time:

16 h
Result:

Exhibited relatively minimal levels of DNA damage in the hiPSC-CMs.

In Vivo

Local Vascular RegulationAnti-cancer

Local Vascular Regulation

ETS transcription factor-IN-1 (compound A) (10 μM; egg water; 16 h) disrupts angiogenesis in zebrafish embryos^[1].

Anti-cancer

ETS transcription factor-IN-1 (10 μM; culture water; 3 days) significantly reduces breast cancer cell dissemination in zebrafish xenograft experiments^[1].

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

Animal Model:

Tg(fli1:gfp) transgenic line (Four hundred mCherry fluorescently labelled human breast
cancer MDA-MB-231 cells were microinjected into the duct of Cuvier of 48 h embryos)^[1]
Dosage:

10 μM
Administration:

culture water; 3 days
Result:

Significantly reduced the dissemination of breast cancer cells towards the head and tail.

Related Protocols :

Chemical Information

CAS No. 158437-84-4
Molecular Weight 437.49
Formula C₂₄H₂₅F₂N₅O
SMILES

O=C1C2=CN(C3CC3)C4=C(C2=NN1CCN(C)C)C=C(F)C(C5=CC(C)=NC(C)=C5)=C4F
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

Handling Instructions (2659 KB)

References

[1]. Abdalla S, et al. Identification of novel small molecule inhibitors of ETS transcription factors. FEBS letters. 2025 Jun;599(12):1733-1748.

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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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100 mg

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