Dual EZH2 and EHMT2 histone methyltransferase inhibition increases biological efficacy in breast cancer cells

Clinical Epigenetics

Table 3 Cell growth IC50 inhibitors in a panel of cell lines

(A) Lymphoma cell lines
EZH2 status	WSU-FSCLL	WILL1	DOHH2	SC1	DB	SUDLH8
HKMT-I-005	3.405	5.599	3.257	3.711	<1	<1
GSK343	2.868	17.91	6.151	12.12.	<1	5.11
	W.T.	W.T.	W.T.	W.T.	Mutant Y646N	W.T.
(B) Breast cancer cell lines
IC50 (μM)	MDA-MB-231	MCF-7	T-47D	BT-474	SkBr3	MCF10a
HKMT-I-005	4.3	7.7	8.5	2.1	7.7	>15

Cell growth IC50s (in μM) for a panel of cell lines, after treatment with HKMT-I-005 or GSK343: lymphoma cell lines (A), derived from cell counting following propidium iodide staining, and breast cancer cell lines (B), derived from MTT assays for cell viability. Mutation status of EZH2 is shown for each of the lymphoma cell lines

ISSN: 1868-7083