Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor with Ki and IC50 of 2.5 and 11 nM, respectively.
PRMT5-IN-25 (compound 503) is a potent PRMT5 inhibitor with an Ki value of 0.06 nM. PRMT5-IN-25 shows antiproliferative[1].
LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively[1].
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours[1].
PRMT7-IN-1 (Compound 14) is a PRMT7 inhibitor with an IC50 of 2.1 μM. PRMT7-IN-1 shows anticancer activity against different cancer cells[1].
Dot1L-IN-7 (compound 25) is a potent and selective disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 1.0 μM. Dot1L-IN-7 selectively killed Mixed Lineage Leukemia (MLL)-AF9 without showing any effect on the growth of E2A-HLF cells[1].
PR5-LL-CM01 is a novel selective, small-molecule inhibitor of PRMT5 methyltransferase with IC50 of 7.5 uM; displays >10-fold selectivity over PRMT3, and no inhibitory activity over PRMT1/4/6/8; exhibits cell viability inhibition with IC50 of 2-4 uM in PDAC cells, IC50 of 10-11 uM in CRC cells, more potent than EPZ015666; significantly inhibits NF-κB activation in PDAC and CRC cells, and shows dramatic anti-tumor efficacy in vivo.
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity[1].
UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM[1][2].
EPZ015666 is an orally available inhibitor of PRMT5 with an IC50 of 22 nM.
EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8.IC50 value: 10 nMTarget: PRMT6in vitro: EPZ020411 inhibits methylation of PRMT6 substrates in cells. EPZ020411 does-dependently inhibits H3R2 methylation in PRMT6-overexpressing cells.in vivo: EPZ020411 shows good bioavailability following subcutaneous (SC) dosing in rats making it a suitable tool for in vivo studies.
EZH2-IN-6 is an EZH2 inhibitor with enhanced antitumor activity.
EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer[1].
MS177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.MS177 exhibited half-maximal degradation concentration (DC50) values of 0.2 ± 0.1 μM and 1.5 ± 0.2 μM, and maximum degradation (Dmax) values of 82% and 68%, respectively, in EOL-1 and MV4;11 cells.MS177 efficiently suppresses EZH2-PRC2 functions, also efficiently induces Myc degradation in cancer cells, suppresses EZH2-PRC2 functions.MS177 efficiently induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest, which is more effective than EZH2 inhibitors. MS177 (i.p. injection, 50-1 g/kg) represses AML growth without apparent toxicity in PDX models.
UNC6934 is a potent and selective drug-like chemical probe to interrogate the function of NSD2-PWWP1 with Kd of 91 nM.UNC6934 disrupts the NSD2-PWWP1 interaction with H3K36me2 nucleosomes in U2OS cells as measured by a NanoBret assay with an IC50 of 1.09 ± 0.23 microM. UNC7145, a closely-related control compound, with an iso-propyl group replacing a cyclo-propyl group, is inactive by SPR and NanoBret assays.
Tazemetostat (EPZ-6438) hydrochloride is a potent, selective and orally active EZH2 inhibitor with IC50 values of 11 and 16 nM for EZH2 peptide and nucleosome, respectively. Tazemetostat hydrochloride can be used for cancer research[1].
AZ505 is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
PROTAC EED degrader-2 is a PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit[1].
PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition[1].
AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
PRMT5-IN-13 is a selective inhibitor of protein arginine methyltransferase 5 (prmt5).
GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5[1].
EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
PRMT5-IN-16 (Compound 20) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification[1].
C21 is a potent, irreversible, and selective PRMT1 inhibitor with an IC50 of 1.8 μM. C21 inhibits PRMT6 with an IC50 of 8.8 μM[1].
NSD3-IN-2 is a potent NSD3 inhibitor with an IC50 value of 17.97 μM. NSD3-IN-2 inhibits the growth and proliferation of non-small cell lung cancer cell lines H460, H1299 and H1650 with anti-cancer activity[1].
Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].
MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 (HY-130614) and PROTAC EED degrader-2 (HY-130615)[1].
DZNep (3-Deazaneplanocin A) is a potent histone methyltransferase EZH2 inhibitor.