EPIC-0628 is an inhibitor of HOTAIR-EZH2 interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with EZH2, the catalytic subunit of PRC2. EPIC-0628 EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) and can enhance its efficacy in vivo.

Physicochemical Properties

Molecular Formula	C20H17F4N3O
Molecular Weight	391.36
Appearance	Solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	EZH2
ln Vitro	EPIC-0628 (20 μM; 48 h) can arrest the cell cycle of U87 cells at the G1 phase [1].
References	[1]. EPIC-0628 abrogates HOTAIR/EZH2 interaction and enhances the temozolomide efficacy via promoting ATF3 expression and inhibiting DNA damage repair in glioblastoma. Cancer Lett. 2024 Apr 28;588:216812.

Solubility Data

Solubility (In Vitro)

DMSO : 200 mg/mL (511.04 mM; with sonication)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 5 mg/mL (12.78 mM)(saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution This solution produces a clear solution of ≥ 5 mg/mL (saturation unknown). For example, if 1 mL of working solution, add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then add 450 μL saline to make up to 1 mL. *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (12.78 mM)(Saturation unknown) in 10% DMSO 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution, add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.5552 mL	12.7760 mL	25.5519 mL
	5 mM	0.5110 mL	2.5552 mL	5.1104 mL
	10 mM	0.2555 mL	1.2776 mL	2.5552 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.