EZH2-IN-6 is an EZH2 inhibitor with enhanced antitumor activity.
分子量
563.75
Formula
C31H41N5O3S
CAS 号
2702269-27-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Khanna A, et al. Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time. ACS Med Chem Lett. 2020 Mar 26;11(6):1205-1212.
(R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nm for EZH2-Y641F. (R)-HH2853 can be used for cancer and autoimmune diseases (WO2018045971A1; compound 201)[1].
IC50 & Target[1]
EZH2 Y641F mutant type
<100 nM (IC50)
分子量
611.66
Formula
C31H36F3N7O3
CAS 号
2202678-06-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Xuxing Chen, et al. Pyrido five-element aromatic ring compound, preparation method therefor and use thereof. WO2018045971A1.
MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines[1].
IC50 & Target[1]
EZH2
120 nM (IC50)
体外研究 (In Vitro)
MS1943 (0.625-5 μM; 3 days) inhibits cell growth with an GI50 of 2.2 µM[1]. MS1943 (0.625-5 μM; 4 days) induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells[1]. MS1943 (1.25-5.0 μM; 2 days) inhibits EZH2 and SUZ12 protein levels in a concentration- and timedependent manner, without affecting EED protein levels, whereas the H3K27me3 mark was also suppressed[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
MDA-MB-468 cells
Concentration:
0.625, 1.25, 2.5, 5 μM
Incubation Time:
3 days
Result:
Inhibits cell growth with an GI50 of 2.2 µM.
Western Blot Analysis[1]
Cell Line:
MDA-MB-468 cells
Concentration:
1.25, 2.5, 5.0 μM
Incubation Time:
2 days
Result:
Reduced EZH2 protein levels in a concentration- and time-dependent manner.
体内研究 (In Vivo)
MS1943 (150 mg/kg body weight; i.p.; once daily for 36 days) suppresses tumor growth[1]. MS1943 induces apoptosis in the MDA-MB-468 xenograft model[1]. A single i.p. injection of MS1943 at 50 mg/kg body weight achieved a peak plasma concentration (Cmax) of 2.9 µM and resulted in plasma concentrations above its cellular IC50 value for ~2h. A single 150 mg/kg body weight p.o. dose achieved Cmax of 1.1 µM, but plasma concentrations were below the cellular IC50 value[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase. IC50 value: < 3 nM ( Ki for wt EZH2, EZH2 Y646) Target: EZH2 inhibitor In vitro: EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. This functional response translates to activity in a long-term proliferation assay where EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. In vivo: The LCC parameter, when corrected for plasma protein-binding, predicts an efficacious plasma level in mouse for EPZ011989 of 158 ng/mL. The pharmacokinetics in SCID mice following oral administration of 125, 250, 500, and 1000 mg/kg indicated that the 1000 mg/kg dose provided coverage over the LCC for 24 h, while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
分子量
605.81
Formula
C35H51N5O4
CAS 号
1598383-40-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495.
Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination[1].
IC50 & Target
EZH2[1]
分子量
630.77
Formula
C38H46O8
CAS 号
173932-75-7
中文名称
新藤黄酸
运输条件
Room temperature in continental US; may vary elsewhere.
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes[1].
IC50 & Target[1]
EZH2
1.1 μM (IC50)
体外研究 (In Vitro)
GNA002 (10 μM; 72 hours) clearly inhibits the proliferation of numerous cancer cell lines with IC50s of 0.070 μM and 0.103 μM for MV4-11 and RS4-11[1]. GNA002 (2 μM; 24 hours) demonstrates an elevated capacity to induce cell death in human cancer cells[1]. GNA002 (0.1-4 μM; 48 hours) efficiently reduces EZH2-mediated H3K27 trimethylation in Cal-27 head and neck cancer cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
Cell Line:
Numerous cancer cell lines
Concentration:
10 μM
Incubation Time:
72 hours
Result:
Inhibited the proliferation of numerous cancer cell lines with IC50s of 0.070 μM and 0.103 μM for MV4-11 and RS4-11.
Apoptosis Analysis[1]
Cell Line:
HN-4 and Cal-27 head and neck cancer cells
Concentration:
2 μM
Incubation Time:
24 hours
Result:
Induced cellular apoptosis in human cancer cells.
Western Blot Analysis[1]
Cell Line:
Cal-27 head and neck cancer cells
Concentration:
0.1, 0.2, 0.5, 1, 2, 4 μM
Incubation Time:
48 hours
Result:
Reduced H3K27Me3 levels.
体内研究 (In Vivo)
GNA002 (oral administration; 100 mg/kg; daily) significantly decreases the volumes of Cal-27-derived tumors and reduces H3K27Me3 levels in tumor tissues. GNA002 also significantly suppresses the in vivo tumor growth derived from the xenografted A549 lung cancer cells, Daudi and Pfeiffer cells. GNA002 inhibits the aberrant oncogenic functions of EZH2, thus inhibiting tumor growth in vivo, at least in the xenograft experimental model[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male BALB/C Nude mice aged 30-35 days and weighing 18-22 g, bearing Cal-27 xenograft tumors[1]
Dosage:
100 mg/kg
Administration:
Oral administration; daily
Result:
Decreased the size and weight of tumors formed by Cal-27 cells.
分子量
701.89
Formula
C42H55NO8
CAS 号
1385035-79-9
运输条件
Room temperature in continental US; may vary elsewhere.
CPI-360 is a potent, selective EZH2inhibitor with IC50 of 0.5 nM and 2.5 nM nM for wt EZH2 and Y641N EZH2, respectively. IC50 value: 0.5 nM, 2.5 nM Target: EZH2 in vitro: CPI-360 functions on the basis of S-adenosyl-Lmethionine (SAM)-competition, inhibits EZH1 about 100-fold less and shows exquisite selectivity across a large panel of histone lysine and arginine, and DNA methyltransferases. CPI-360 potently reduced global H3K27me3 and H3K27me2 levels in a dosedependent manner. CPI-360 effectively suppressed heavy H3K27me3 incorporation in KARPAS-422 cells without affecting total histone turnover. CPI-360 treatment causes time-dependent transcriptional changes in germinal center B cell-like diffuse large B cell lymphoma. in vivo: Twice daily, subcutaneous administration of 200 mg/kg of CPI-360 reduced tumor growth (TGI 44%) of KARPAS-422 xenografts in mice without affecting body weight or causing any overt adverse effects. CPI-360 completely inhibits EZH2 catalytic activity, since we entirely suppress H3K27me3 turnover over time.
分子量
437.53
Formula
C25H31N3O4
CAS 号
1802175-06-9
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Bradley WD, et al. EZH2 inhibitor efficacy in non-Hodgkin’s lymphoma does not require suppression of H3K27 monomethylation. Chem Biol. 2014 Nov 20;21(11):1463-1475.
[2]. Bruno NC, et al. Design and Preparation of New Palladium Precatalysts for C-C and C-N Cross-Coupling Reactions. Chem Sci. 2013;4:916-920.
PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes[1].
IC50 & Target
EZH2
2.7 nM (IC50)
分子量
942.15
Formula
C54H67N7O8
CAS 号
2641601-67-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Juan Xia, et al. Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects. J Med Chem. 2022 May 26;65(10):7016-7043.
EPZ011989 trifluoroacetate is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase. IC50 value: < 3 nM ( Ki for wt EZH2, EZH2 Y646) Target: EZH2 inhibitor In vitro: EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. This functional response translates to activity in a long-term proliferation assay where EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. In vivo: The LCC parameter, when corrected for plasma protein-binding, predicts an efficacious plasma level in mouse for EPZ011989 of 158 ng/mL. The pharmacokinetics in SCID mice following oral administration of 125, 250, 500, and 1000 mg/kg indicated that the 1000 mg/kg dose provided coverage over the LCC for 24 h, while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
分子量
719.83
Formula
C37H52F3N5O6
CAS 号
1598383-41-5
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495.
UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM[1][2].
IC50 & Target[1]
EZH2
17 nM (IC50)
体外研究 (In Vitro)
UNC2399 (1-1000 nM) displays high in vitro potency (IC50=17±2 nM) in the EZH2 radioactive biochemical assay[1]. UNC2399 (100 μM) enriches EZH2 from HEK293T cell lysates[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
927.17
Formula
C48H66N10O7S
CAS 号
2412791-72-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Konze KD, et, al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013; 8(6): 1324-34.
[2]. Ma A, et, al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.
UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM[1][2].
IC50 & Target[1]
EZH2
17 nM (IC50)
体外研究 (In Vitro)
UNC2399 (1-1000 nM) displays high in vitro potency (IC50=17±2 nM) in the EZH2 radioactive biochemical assay[1]. UNC2399 (100 μM) enriches EZH2 from HEK293T cell lysates[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
927.17
Formula
C48H66N10O7S
CAS 号
2412791-72-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Konze KD, et, al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013; 8(6): 1324-34.
[2]. Ma A, et, al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.
UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM[1][2].
IC50 & Target[1]
EZH2
17 nM (IC50)
体外研究 (In Vitro)
UNC2399 (1-1000 nM) displays high in vitro potency (IC50=17±2 nM) in the EZH2 radioactive biochemical assay[1]. UNC2399 (100 μM) enriches EZH2 from HEK293T cell lysates[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
927.17
Formula
C48H66N10O7S
CAS 号
2412791-72-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Konze KD, et, al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013; 8(6): 1324-34.
[2]. Ma A, et, al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.
EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity[1].
IC50 & Target[1]
WT 5-mer EZH2
0.923 nM (IC50)
mut 5-mer EZH2
2.65 nM (IC50)
体外研究 (In Vitro)
EZH2-IN-4 (example 38) shows a cell H3K27me3 IC50 of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells[1]. EZH2-IN-4 shows an IC50 of 10.1 nM in Plate Kj«pas-422 cells[1]. EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC50s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC50>20 μM)[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) results in 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1]. EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
511.72
Formula
C29H41N3O3S
CAS 号
2088132-99-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Esteban DOMINGUEZ, et al. Inhibitors of ezh2. WO2017035060A1.
EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity[1].
IC50 & Target[1]
WT 5-mer EZH2
0.923 nM (IC50)
mut 5-mer EZH2
2.65 nM (IC50)
体外研究 (In Vitro)
EZH2-IN-4 (example 38) shows a cell H3K27me3 IC50 of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells[1]. EZH2-IN-4 shows an IC50 of 10.1 nM in Plate Kj«pas-422 cells[1]. EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC50s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC50>20 μM)[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) results in 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1]. EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
511.72
Formula
C29H41N3O3S
CAS 号
2088132-99-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Esteban DOMINGUEZ, et al. Inhibitors of ezh2. WO2017035060A1.
EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity[1].
IC50 & Target[1]
WT 5-mer EZH2
0.923 nM (IC50)
mut 5-mer EZH2
2.65 nM (IC50)
体外研究 (In Vitro)
EZH2-IN-4 (example 38) shows a cell H3K27me3 IC50 of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells[1]. EZH2-IN-4 shows an IC50 of 10.1 nM in Plate Kj«pas-422 cells[1]. EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC50s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC50>20 μM)[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) results in 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1]. EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
511.72
Formula
C29H41N3O3S
CAS 号
2088132-99-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Esteban DOMINGUEZ, et al. Inhibitors of ezh2. WO2017035060A1.
EPZ011989-d8 is the deuterium labeled EPZ011989. EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
613.86
Formula
C35H43D8N5O4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495.
EPZ011989-d8 is the deuterium labeled EPZ011989. EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
613.86
Formula
C35H43D8N5O4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495.
