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

Histone Methyltransferase Degrader

Histone Methyltransferase Degraders (33):

Cat. No. 상품명 효과 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-156152A
    CARM1 degrader-1 hydrochloride
    		Degrader
    CARM1 degrader-1 hydrochloride is a CARM1 PROTAC degrader (DC50 = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 hydrochloride degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 hydrochloride downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 hydrochloride inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 hydrochloride can be used in breast cancer research.
  • HY-162749A
    G9D-4 TFA
    		Degrader 99.44%
    G9D-4 TFA is a G9a PROTAC degrader. G9D-4 TFA induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 TFA exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 TFA can be used for research on pancreatic cancer.
  • HY-157251A
    UNC8153
    		Degrader 99.61%
    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-178321
    UNC10088
    		Degrader
    UNC10088 is a molecular glue targeting NSD2. UNC10088 mediates the formation of a stable ternary complex between SCFFBXO22 and the NSD2 PWWP1 domain. UNC10088 promotes ubiquitination of the SCFFBXO22-dependent NSD2 PWWP1 domain through reversible covalent bonding with the C326 region of FBXO22. UNC10088 could be used in cancer research.
  • 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-181307
    PROTAC EZH2 Degrader-12
    		Degrader
    PROTAC EZH2 Degrader-12 (compound 3) is a CRBN-recruiting PROTAC-based EZH2 degrader with an EZH2 IC50 of 3.90 nM and EZH1 IC50 of 5.24 μM.
  • HY-181359
    PROTAC EZH2 Degrader-30
    		Degrader
    PROTAC EZH2 Degrader-30 (compound 67) is ais a PROTAC protein degrader targeting EZH2 with an IC50 of 6.22 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-30 can be used for the research of diffuse large B-cell lymphoma.
  • HY-181300
    PROTAC EZH2 Degrader-17
    		Degrader
    PROTAC EZH2 Degrader-17 (compound 52) is a PROTAC protein degrader targeting EZH2 with an antiproliferative IC50 of 18.32 μM in lymphoma cells. PROTAC EZH2 Degrader-17 exhibits antiproliferative activity against lymphoma cells. PROTAC EZH2 Degrader-17 can be used for the research of lymphoma.
  • 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-181309
    PROTAC EZH2 Degrader-15
    		Degrader
    PROTAC EZH2 Degrader-15 (compound 5) is an EZH2-targeting PROTAC. PROTAC EZH2 Degrader-15 functionally inhibits EZH2 methyltransferase activity.
  • HY-181305
    PROTAC EZH2 Degrader-10
    		Degrader
    PROTAC EZH2 Degrader-10 is a selective PROTAC protein degrader targeting EZH2. PROTAC EZH2 Degrader-10 can be used for the research of cancer.
  • HY-181392
    PROTAC EZH2 Degrader-35
    		Degrader
    PROTAC EZH2 Degrader-35 (compound U3i (44)) is a PROTAC protein degrader targeting EZH2 with a human EZH2 Ka of 16.19 nM. PROTAC EZH2 Degrader-35 exhibits antiproliferative activity in triple-negative breast cancer cells and minimal cytotoxicity in normal human epithelial, hepatic, renal cells.PROTAC EZH2 Degrader-35 can be used for the research of triple-negative breast cancer.
  • 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-181332
    PROTAC EZH2 Degrader-37
    		Degrader
    PROTAC EZH2 Degrader-37 (compound 16) is a PROTAC protein degrader targeting EZH2 with a target IC50 of 144 nM. PROTAC EZH2 Degrader-37 is applicable to lymphoma-related research.
  • HY-181355
    PROTAC EZH2 Degrader-28
    		Degrader
    PROTAC EZH2 Degrader-28 is an EZH2 PROTAC degrader. PROTAC EZH2 Degrader-28 promotes the ubiquitination and degradation of EZH2. PROTAC EZH2 Degrader-28 can be used for lymphoma-related research.
  • HY-181318
    PROTAC EZH2 Degrader-20
    		Degrader
    PROTAC EZH2 Degrader-20 (compound 54) is an EZH2-target PROTAC degrader with antiproliferative activity and IC50 values of about 10 μM against lymphoma cells. PROTAC EZH2 Degrader-20 can be used for the research of lymphoma.
  • HY-181296
    PROTAC EZH2 Degrader-16
    		Degrader
    PROTAC EZH2 Degrader-16 (compound 51) is a PROTAC protein degrader targeting EZH2 with an IC50 of 13.74 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-16 exerts antiproliferative activity against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-16 can be used for the research of diffuse large B-cell lymphoma.
  • HY-181360
    PROTAC EZH2 Degrader-31
    		Degrader
    PROTAC EZH2 Degrader-31 is an EZH2 PROTAC degrader. PROTAC EZH2 Degrader-31 promotes the ubiquitination and degradation of EZH2. PROTAC EZH2 Degrader-31 can be used for lymphoma-related research.