2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. Histone Methyltransferase Degrader

Histone Methyltransferase Degrader

Histone Methyltransferase Isoform Comparison

Histone Methyltransferase Degraders (17):

Cat. No. Product Name Effect Purity
  • HY-157251
    UNC8153 TFA
    		Degrader 99.92%
    UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2.
  • HY-141877
    MS4322
    		Degrader 99.14%
    MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
  • HY-157844
    NUCC-0226272
    		Degrader 99.68%
    NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research.
  • HY-147090
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH
    		Degrader 99.06%
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) incorporates a ligand for EZH2, and a PROTAC linker, which recruit E3 ligases. Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) can be used for the research of lymphoma.
  • HY-157164
    PROTAC EZH2 Degrader-2
    		Degrader 99.78%
    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.
  • HY-156152A
    CARM1 degrader-1 hydrochloride
    		Degrader 99.44%
    CARM1 degrader-1 hydrochloride is the hydrochloride salt form of CARM1 degrader-1 (HY-156152). CARM1 degrader-1 hydrochloride is a PROTAC degrader for co-activator associated argininemethyltransferase 1 (CARM1), which degrades CARM1 in a VHL- and proteasome-dependent manner with a DC50 of 8.1 nM. CARM1 degrader-1 hydrochloride inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, and thus inhibits breast cancer cell migration.
  • HY-162749
    G9D-4
    		Degrader
    G9D-4 is a potent PROTAC degrader of G9a, with the DC50 value of 0.1 μM in PANC-1 cells and do not directly perturb GLP protein, with the DC50 of ＞10 μM. G9D-4 plays an important role in pancreatic cancer research (Pink: Ligand for target protein G9a/GLP Inhibitor (HY-15273); Black: Linker; Blue: Ligand for E3 ligase (HY-10984)).
  • HY-157251A
    UNC8153
    		Degrader 99.13%
    UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2.
  • HY-173422
    MS2133
    		Degrader
    MS2133 is a DOT1L PROTAC degrader. MS2133 promotes ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells (DC50: 56 nM and 25 nM, respectively), and reduces H3K79 methylation. MS2133 inhibits the growth of MLL-r leukemia cells and has anticancer activity. (Pink: DOT1L ligand (HY-173423); Blue: E3 ligase VHL ligand (HY-47070); Black: Linker (HY-79577); E3 ligase VHL ligand-linker conjugate (HY-173424)).
  • HY-172769
    CM112
    		Degrader
    CM112 is a selective protein arginine methyltransferase 1 (PRMT1) degrader by tethering hydrophobic tag, adamantane, to MS023 with a 5-PEG linker. CM112 induces the degradation of PRMT1 in various solid cancer cell lines. CM112 can also target the nonenzymatic function of PRMT1 by downregulating the stability of the orphan receptor TR3. CM112 is promising for research of cancers.
  • HY-168131
    PROTAC EZH2 Degrader-3
    		Degrader
    PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 PROTAC 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)).
  • HY-169761
    (rac)-dWIZ-1
    		Degrader
    WIZ-IN-1 (Example 2) is a Wiz inhibitor (DC50: 0.36 μM). WIZ-IN-1 can be used for research of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta- hemoglobinopathies), such as sickle cell disease and beta-thalassemia.
  • HY-170674
    ND-L11B free base
    		Degrader
    ND-L11B is a potent degrader of nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with the DC50 of 1.48 and 0.8 μM, the Dmax is closed to 80 %.
  • HY-159728
    PROTAC PRMT3 degrader 1
    		Degrader
    PROTAC PRMT3 degrader 1 (compound 11) is a PROTAC degrader targeting PRMT3. PROTAC PRMT3 degrader 1 can inhibit the growth of acute leukemia cells.
  • HY-170674A
    ND-L11B TFA
    		Degrader
    ND-L11B TFA is a potent degrader of nuclear receptor binding SET domain protein 2 (NSD2) and RE-IIBP, with the DC50 of 1.48 and 0.8 μM, the Dmax is closed to 80 %.
  • HY-163818
    WIZ degrader 2
    		Degrader
    WIZ degrader 2 (Compound 142) is a degrader for widely interspaced zinc finger motifs with an AC50 of 0.011 μM. WIZ degrader 2 induces the expression of fetal hemoglobin (HbF) with an EC50 of 0.038 μM. WIZ degrader 2 can be used in research about inherited blood disorders.
  • HY-174445
    C199
    		Degrader
    C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity (Pink: Target protein ligand (HY-111109); Blue: E3 ligase ligand (HY-112078), E3 ligase ligand + linker (HY-174474); black: Linker).