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. Author manuscript; available in PMC: 2018 Jul 10.
Published in final edited form as: Sci Transl Med. 2017 Jul 12;9(398):eaal5272. doi: 10.1126/scitranslmed.aal5272

Fig. 5. Antiproliferative effects of JQ-EZ-05 on VHL−/− ccRCC are on-target.

Fig. 5

(A) Sequence alignment of EZH1 and EZH2 catalytic SET domains.

(B and C) Immunoblots (B) and crystal violet staining (C) of 786-O cells infected to exogenously produce wild-type or ΔPSET EZH1 and treated with the indicated amounts of JQ-EZ-05 for 3 days and 7 days, respectively.

(D and E) Photomicrographs (D) and immunoblots (E) of 786-O cells infected with a lentivirus encoding GFP, wild-type EZH1, or randomly mutagenized EZH1 (XL-Red) and treated with the indicated concentrations of JQ-EZ-05 for 3 days (E) or with either 4 μM JQ-EZ-05 or DMSO for 21 days (D).

(F) Crystal violet staining of UMRC-2 cells infected to exogenously produce the indicated EZH1 variants and treated with the indicated concentrations of JQ-EZ-05 for 10 days.

(G) Structural model of JQ-EZ-05 bound to wild-type EZH1.

(H) Immunoblots of UMRC-2 cells expressing EZH1 variants as in (F) treated with the indicated concentrations of JQ-EZ-05 for 3 days.