Histone Methyltransferase Degrader

Histone Methyltransferase Isoform Comparison

Histone Methyltransferase Degraders (22):

Cat. No.	Product Name	Effect	Purity

HY-162749A

G9D-4 TFA	Degrader
G9D-4 (TFA) 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 (TFA) 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-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 K_d 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 is a PROTAC EZH2 inhibitor. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner. PROTAC EZH2 Degrader-2 induces apoptosis and reduces mitochondrial membrane potential in SU-DHL-6 cells. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity. (Pink: EZH2 ligand (HY-15335), Blue: MDM2 Ligand (HY-147230), Black: Linker (HY-175707), EZH2 ligand-linker conjugate (HY-175706)).

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-157251A

UNC8153	Degrader	99.13%
UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a K_d 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-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-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-178114

SKLB-0124	Degrader
SKLB-0124 is a selective PRMT6 degrader with DC₅₀s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC₅₀ on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer.

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 D_max is closed to 80 %.

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-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 D_max is closed to 80 %.

HY-178322

UNC10415667	Degrader
UNC10415667 is a NSD2 degrader, with a DC₅₀ values of 460 nM. UNC10415667 can be used for the study of cancers driven by NSD2 overexpression or dysregulation, such as multiple myeloma, acute lymphocytic leukemia, and prostate cancer.

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.

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