HLCL-61 hydrochloride is a first-in-class small-molecule inhibitor of PRMT5. Target: PRMT5in vitro: HLCL-61 shows effective inhibition of symmetric arginine dimethylation (me2) of histones H3 and H4 in AML samples, starting at 12 h post-treatment and persisting after 48 h. Treatment of AML cell lines (MV4-11 and THP-1) and primary blasts with HLCL-61 also resulted in a decrease of cell viability. HLCL-61 is also effective in promoting apoptosis in MV4-11 and THP-1 cells after 48 h.[1]
PRMT5-IN-2 is a rotein arginine methyltransferase 5 (PRMT5) inhibitor extracted from patent WO2018130840A1, compound 3[1].
MS-0124 is a potent and selective inhibitor of G9a-like Protein (GLP) lysine methyltransferase with IC50 of 13 nM, shows >30-fold selectivity for GLP over G9a and other methyltransferases.
YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma[1].
Amodiaquine dihydrochloride dihydrate is a histamine N-methyltransferase inhibitor, used as an antimalarial and anti-inflammatory agent.Target: histamine N-methyltransferaseAmodiaquine has been shown to be more effective than chloroquine in treating chloroquine-resistant Plasmodium falciparum malaria infections and may afford more protection than chloroquine when used as weekly prophylaxis. Amodiaquine is generally well tolerated.
EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
Furamidine-d8 (DB75-d8) is the deuterium labeled Furamidine. Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent[1][2][3].
UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively.
DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors[1].
A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.
GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.
WM-586 is a covalent WDR5 inhibitor that disrupts the binding of WDR5 to MYC. WM-586 specifically decreases cellular WDR5 and MYC interaction with the IC50 of 101 nM in HTRF assay[1].
PDAT is a noncompetitive Indolethylamine N-methyltransferase inhibitor.
PRMT5-IN-3 is a PRMT5 inhibitor that exhibits synthetic lethality to tumor cells but produce few side effects combined with DNA damaging agents.
PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit[1].
BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8.
PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity[1].
CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].
CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor. CSV0C018875 exhibits lesser cytotoxicity than BIX-01294[1].
WM-662 is a WDR5-MYC interaction inhibitor, with an IC50 of 18 μM. WM-662 has potential for the research of cancer, aging, and neurodegenerative disorders[1].
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)[1].
EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
NSD3-IN-1 (compound B1) is an inhibitor of histone methyltransferase NSD3 with an IC50 value of 28.58 μM[1].
EZH2-IN-3 is a highly selective small molecule inhibitor of EZH2 and EZH1 with IC50 of 21/197/213 nM for wt EZH2/EZH2 Y641N/wt EZH1 respectively; suppresses global histone H3-lysine 27 methylation and cause selective proliferation defects.
TP-064 is a potent, selective, and cell-active inhibitor of PRMT4 with IC50 of <10 nM and Kd of 7.1 nM, shows high selectivity (>100-fold) for PRMT4 over other PRMTs; reduces dimethylation of BAF155 (IC50=340±30 nM) and MED12 (IC50=43±10 nM) in a dose-dependent manner in cell-baed assays; inhibits the proliferation of a subset of multiple myeloma cell lines (NCI-H929, RPMI8226, Cell IC50 of 379 and 886 nM, respectively) with affected cells arrested in G1 phase of the cell cycle, but has no effect on acute myeloid leukemia, colon cancer, or lung cancer cell lines.
OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation .target: Wdr5IC 50: 5 uMIn vitro: OICR-9429 inhibit proliferation and induce differentiation in p30-expressing human AML cells. OICR-9429 cause a significant decrease in viability in the majority of patient cells with mutations in the N-terminal part of the CEBPA gene. OICR-9429 displays exquisite cellular selectivity and specificity in disrupting critical protein-protein interactions between WDR5. [1] reduce the viability of primary human AML cells with N-terminal C/EBPα mutations by about 50% (mean value, n = 8) at 5 μM[2]In vivo:The reference for OICR-9429 to mice (female NOD-SCID) is 3 mg/kg.
SAH-EZH2 is an EZH2/EPP interaction inhibitor (Kd = 320 nM). SAH-EZH2 suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. SAH-EZH2 arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line.
BIX-01294 is an inhibitor of G9a Histone Methyltransferase with IC50 of 1.9 μM.
PRMT5-IN-32 is an inhibitor of PRMT5. PRMT5-IN-32 inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM[1].