| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C25H27F2N5O3 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Ep300/CREBBP-IN-8 is a potent, orally active inhibitor of Ep300 and CREBBP with IC50 values of 0.014 and 0.018 μM, respectively, and it can be used in cancer research[1]. It has the molecular formula C25H27F2N5O3 (MW 483.51).
Physical & Chemical Properties
| CAS Number | 2259641-24-0 |
|---|---|
| Molecular Formula | C25H27F2N5O3 |
| Molecular Weight | 483.51 g/mol |
| SMILES | O=C([C@@H]1N(C(C2(C3=CC=C(OC)C(F)=C3)CCCCC2)=O)C[C@H](F)C1)NC4=CC=C(NN=C5)C5=N4 |
| Target | EP300, CREBBP |
| Signaling Pathway | Epigenetics |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
EP300 0.014 μM (IC50) |
CREBBP 0.018 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[1]. NAITO Hiroyuki, et al. EP300 / CREBBP inhibitor. Patent JPWO2018235966A1.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
Ep300/CREBBP-IN-8 inhibits intracellular H3K27Ac activity, with an IC50 of 0.016 μM[1]. At 38 nM-10 mM for 3 days, Ep300/CREBBP-IN-8 inhibits the growth of LK2 and TE-8 cells, with GI50s of 85.917 and 112.922 μM, respectively[1].
Cell Viability Assay[1]
| Cell Line | LK2 and TE-8 cells |
|---|---|
| Concentration | 38 nM-10 mM |
| Incubation Time | 3 days |
| Result | Inhibited LK2 and TE-8 cell growth with GI50s of 85.917 and 112.922 μM, respectively. |
In Vivo
In mice, Ep300/CREBBP-IN-8 (Example 37; 6.25 mg/kg/day; oral; twice daily for 11 days) suppresses tumor proliferation[1].
| Animal Model | Female BALB/c-nu/nu mice, LK2 cell subcutaneous transplant model[1] |
|---|---|
| Dosage | 6.25 mg/kg/day |
| Administration | Oral administration, twice a day for 11 days |
| Result | Inhibited tumor volume by 42%. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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