Description
DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors.
Product information
CAS Number: 2355280-00-9
Molecular Weight: 435.48
Formula: C23H28F3N3O2
Chemical Name: N-[(4,6-dimethyl-2-oxopiperidin-3-yl)methyl]-2,4-dimethyl-1-{[4-(trifluoromethyl)phenyl]methyl}-1H-pyrrole-3-carboxamide
Smiles: CC1=C(C(=O)NCC2C(C)CC(C)NC2=O)C(C)=CN1CC1C=CC(=CC=1)C(F)(F)F
InChiKey: RSSWOJJWSHTZKF-UHFFFAOYSA-N
InChi: InChI=1S/C23H28F3N3O2/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/h5-8,11,13,15,19H,9-10,12H2,1-4H3,(H,27,31)(H,28,30)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (115.89 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Knockdown EZH2 in A549 cells results in the decrease of cell sensitivity to DM-01 at 50 and 100 μM concentrations. DM-01 also shows comparable inhibitory activity for K562 cells with an IC50 value of 58.706 μΜ. DM-01 (5 and 10 μM; 24 hours) strongly inhibits the activity of EZH2 and results in abolished H3K27me expression in K562 cells. DM-01 (5 and 10 μM) also increases the transcription expression of DIRAS3 in a dose dependent manner, a tumor suppressor in downstream of EZH2.
Products are for research use only. Not for human use.
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