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.
All DNA/RNA Synthesis Isoforms
More
Biological Activity
Description
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
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].
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].
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 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.
-
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
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.
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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)