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Histone Methyltransferase

Histone methyltransferases (HMT) are histone-modifying enzymes , that catalyze the transfer of one, two, or three methyl groups to lysine and arginine residues of histone proteins. The attachment of methyl groups occurs predominantly at specific lysine or arginine residues on histones H3 and H4.
Signaling Pathways | Target | TargetMol
Cat. No. Product name CAS No. Purity Chemical Structure
T79741 CARM1 degrader-1 98%
CARM1 degrader-1
PROTAC CARM1 degrader-1 (compound 3b) serves as a highly potent degrader (DC50=8.1 nM) of the co-activator associated arginine methyltransferase (CARM1). This co...
T79742 CARM1 degrader-2 98%
CARM1 degrader-2
PROTAC CARM1 degrader-2 (compound 3e), with a DC50 value of 8.8 nM, is a VHL- and proteasome-dependent degrader of co-activator associated argininemethyltransfer...
T79776 ZZM-1220 98%
ZZM-1220
ZZM-1220, a covalent inhibitor of histone lysine methyltransferase G9a/GLP, exhibits IC50 values of 458 nM for G9a and 924 nM for GLP. It effectively inhibits H3...
T79780 IHMT-EZH2-426 98%
IHMT-EZH2-426
IHMT-EZH2-426 (compound 38) is a potent, covalent degrader of EZH2, demonstrating IC50 values of 1.3 nM for EZH2 wild-type, 1.2 nM for EZH2-A687V, and 1.7-3.5 nM...
T79849 Igermetostat 2409538-60-7 98%
Igermetostat
Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [1].
T79873 TNG-462 2760483-96-1 98%
TNG-462
TNG-462 (Compound 1143) is a PRMT5 inhibitor with oral activity, being investigated for use in MTAP-deficient and/or MTA-accumulating cancers [1].
T81175 SETD7-IN-1 98%
SETD7-IN-1
SETD7-IN-1 (compound 7), a PFI-2 analogue, acts as both a substrate and inhibitor of histone lysine methyltransferase SETD7, exhibiting an inhibitory concentrati...
T13279 Valemetostat tosylate 1809336-93-3 98%
Valemetostat tosylate
Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.
T12886 SGC-iMLLT 2255338-25-9 98%
SGC-iMLLT
SGC-iMLLT is a potent and selective MLLT1/3-histone interactions inhibitor(IC50 = 0.26 μM),and is a first-in-class chemical probe displaying cellular target enga...
T12428 PF-06726304 acetate 2080306-28-9 98%
PF-06726304 acetate
PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
T12939 SMYD2-IN-1 2023788-96-5 98%
SMYD2-IN-1
SMYD2-IN-1 is an inhibitor of SMYD2 (IC50 of 4.45 nM).
T74542 YM458 2770108-93-3 98%
YM458
YM458, a potent dual inhibitor of EZH2 and BRD4, exhibits IC50 values of 490 nM and 34 nM, respectively. This compound effectively hinders cell proliferation and...
T11185 EML741 2328074-38-8 98%
EML741
EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barri...
T36798L SW2_110A acetate 98%
SW2_110A acetate
SW2_110A acetate is a selective, cell-permeable chromobox inhibitor of homologue CBX8 (Kd = 800 nM) bound to CBX8 N-terminal color gamut (ChD). SW2_110A acetate ...
T11500 GSK3368715 1629013-22-4 98%
GSK3368715
GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: ...
T11082 Dot1L-IN-2 1940206-71-2 98%
Dot1L-IN-2
Dot1l-in-2 is an effective, selective and oral bioutilization inhibitor of histone methyltransferase Dot1L, with IC50 and Ki of 0.4 nM and 0.08 nM, respectively....
T15240 Tazemetostat trihydrochloride 1403255-00-4 98%
Tazemetostat trihydrochloride
Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing ...
T11081 Dot1L-IN-1 2088518-50-5 98%
Dot1L-IN-1
The Ki value of DOT1L-in-1 is 2pm.It is a highly effective, selective and novel Dot1L inhibitor.
T12541 PRMT5-IN-1 2366149-83-7 98%
PRMT5-IN-1
PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).
T68378 PRMT4-IN-1 912970-79-7 98%
PRMT4-IN-1
PRMT4-IN-1 is a selective inhibitor of PRMT4, demonstrating an IC50 value of 3.2 nM, and has been shown to reduce the relative viability of MCF7 cells [1].
CARM1 degrader-1
T79741
PROTAC CARM1 degrader-1 (compound 3b) serves as a highly potent degrader (DC50=8.1 nM) of the co-activator associated arginine methyltransferase (CARM1). This co...
CARM1 degrader-2
T79742
PROTAC CARM1 degrader-2 (compound 3e), with a DC50 value of 8.8 nM, is a VHL- and proteasome-dependent degrader of co-activator associated argininemethyltransfer...
ZZM-1220
T79776
ZZM-1220, a covalent inhibitor of histone lysine methyltransferase G9a/GLP, exhibits IC50 values of 458 nM for G9a and 924 nM for GLP. It effectively inhibits H3...
IHMT-EZH2-426
T79780
IHMT-EZH2-426 (compound 38) is a potent, covalent degrader of EZH2, demonstrating IC50 values of 1.3 nM for EZH2 wild-type, 1.2 nM for EZH2-A687V, and 1.7-3.5 nM...
Igermetostat
T79849
Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [1].
TNG-462
T79873
TNG-462 (Compound 1143) is a PRMT5 inhibitor with oral activity, being investigated for use in MTAP-deficient and/or MTA-accumulating cancers [1].
SETD7-IN-1
T81175
SETD7-IN-1 (compound 7), a PFI-2 analogue, acts as both a substrate and inhibitor of histone lysine methyltransferase SETD7, exhibiting an inhibitory concentrati...
Valemetostat tosylate
T13279
Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.
SGC-iMLLT
T12886
SGC-iMLLT is a potent and selective MLLT1/3-histone interactions inhibitor(IC50 = 0.26 μM),and is a first-in-class chemical probe displaying cellular target enga...
PF-06726304 acetate
T12428
PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
SMYD2-IN-1
T12939
SMYD2-IN-1 is an inhibitor of SMYD2 (IC50 of 4.45 nM).
YM458
T74542
YM458, a potent dual inhibitor of EZH2 and BRD4, exhibits IC50 values of 490 nM and 34 nM, respectively. This compound effectively hinders cell proliferation and...
EML741
T11185
EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barri...
SW2_110A acetate
T36798L
SW2_110A acetate is a selective, cell-permeable chromobox inhibitor of homologue CBX8 (Kd = 800 nM) bound to CBX8 N-terminal color gamut (ChD). SW2_110A acetate ...
GSK3368715
T11500
GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: ...
Dot1L-IN-2
T11082
Dot1l-in-2 is an effective, selective and oral bioutilization inhibitor of histone methyltransferase Dot1L, with IC50 and Ki of 0.4 nM and 0.08 nM, respectively....
Tazemetostat trihydrochloride
T15240
Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing ...
Dot1L-IN-1
T11081
The Ki value of DOT1L-in-1 is 2pm.It is a highly effective, selective and novel Dot1L inhibitor.
PRMT5-IN-1
T12541
PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).
PRMT4-IN-1
T68378
PRMT4-IN-1 is a selective inhibitor of PRMT4, demonstrating an IC50 value of 3.2 nM, and has been shown to reduce the relative viability of MCF7 cells [1].
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