DM-01 is a potent and specific EZH2 inhibitor that may be utilized in the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL) and SNF5/INI-1/SMARCB1 gene-related solid tumors. .

Physicochemical Properties

Molecular Formula	C23H28F3N3O2
Molecular Weight	435.4825
Exact Mass	431.182
CAS #	2355280-00-9
PubChem CID	141741918
Appearance	Typically exists as solid at room temperature
LogP	3.8
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	5
Heavy Atom Count	31
Complexity	767
Defined Atom Stereocenter Count	0
InChi Key	XHYKDXOCUIJBHL-UHFFFAOYSA-N
InChi Code	InChI=1S/C23H24F3N3O2/c1-13-9-15(3)28-21(30)19(13)10-27-22(31)20-14(2)11-29(16(20)4)12-17-5-7-18(8-6-17)23(24,25)26/h5-9,11H,10,12H2,1-4H3,(H,27,31)(H,28,30)
Chemical Name	N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2,4-dimethyl-1-[[4-(trifluoromethyl)phenyl]methyl]pyrrole-3-carboxamide
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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
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	In A549 cells, knockdown of EZH2 reduces the susceptibility of the cells to DM-01 at doses of 50 and 100 μM. DM-01 exhibits similar inhibitory effect against K562 cells, as seen by its IC50 value of 58.706 μM[1]. DM-01 (5 and 10 μM; 24 hours) significantly suppresses EZH2 activity, which eliminates H3K27me expression in K562 cells[1]. Additionally, in a dose-dependent manner, DM-01 (5 and 10 μM) raises the transcription expression of DIRAS3, a tumor suppressor that is downstream of EZH2[1].
Cell Assay	Cell Viability Assay[1] Cell Types: A549 sh-EV and A549 sh-EZH2 cells Tested Concentrations: 1, 5, 10, 50, 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: The IC50s of 72.748 and 269.7 μM for A549 sh-EV and A549 sh-EZH2 cells, respectively. Western Blot Analysis[1] Cell Types: K562 cells Tested Concentrations: 5, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited the activity of EZH2 and resulted in abolished H3K27me expression.
References	[1]. Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents. New Journal of Chemistry. 10 Jan 2020.

Solubility Data

Solubility (In Vitro)

DMSO : 50 mg/mL (115.89 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.79 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 is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2963 mL	11.4816 mL	22.9632 mL
	5 mM	0.4593 mL	2.2963 mL	4.5926 mL
	10 mM	0.2296 mL	1.1482 mL	2.2963 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.