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UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells .
GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.
EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 .
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
GSK-J2 sodium is the sodium form of GSK-J2 (HY-15648A). GSK-J2 is an isomer of GSK-J1, and does not have any specific activity. GSK-J1 (HY-15648) is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A .
EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research .
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1 .
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1 . GSK-J4 induces endoplasmic reticulum stress-related apoptosis .
IHMT-EZH2-426 (compound 38) is an effective covalent EZH2 degrader, with IC50 values of 1.3 nM, 1.2 nM, and 1.7-3.5 nM for EZH2 wild type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 reduces H3K27me3 and EZH2 levels and shows effective anti-proliferative effects in B-cell lymphoma and TNBC cell lines.
D-01 is a dual-targeting inhibitor of HIF-1α and EZH2 (IC50: 4.86 μM and 0.99 μM respectively). D-01 inhibits the expression of H3K27me3 protein. D-01 inhibits the migration, clone and the invasion of A549 cells, and also inhibits tube formation of HUVECs. D-01 can be used for research of lung cancer .
BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 μM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence .
EZH2-IN-9 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-9 has the potential for the research of cancer diseases (extracted from patent WO2021180235A1, compound 17) .
EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259) .
PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .
PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 degrader. PROTAC EZH2 Degrader-3 (5 μM, 24 h) not only potently inhibits the expression of EZH2 protein, but also had a strong inhibits effect on the expression levels of other subunits of PRC2 as well as H3k27me3 protein. PROTAC EZH2 Degrader-3 shows anti-proliferative activity and blocks the cell cycle in the G0-G1 phase and induces cell apoptosis((Blue: cereblon ligand Pomalidomide (HY-10984), Black: linker HY-W361751；Pink: EZH2 inhibitor Tazemetostat (HY-13803)) .
PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity .
PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity .
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects .
EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity .
MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12?nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest .
SPEN-IN-1 (compound X1) is an inhibitor of SPEN which is a protein factor with a Kd value of 47 nM. SPEN-IN-1 has high selectivity for RepA, a 431-nucleotide domain in Xist (a non-coding RNA prototype) that comprises 8.5 units of a GC-rich motif responsible for gene silencing .
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .
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 .
H3K27(Me3) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
H3K27(Me) (15-34), a histone peptide, is a repressive chromatin markderived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
H3K27(Me2) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .
TriMethyl-Histone H3 (Lys27) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 15 kDa, targeting to TriMethyl-Histone H3 (Lys27). It can be used for WB,IHC-F,IHC-P,ICC/IF,IP,ChIP assays with tag free, in the background of Human, Rat.
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