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Histone Methyltransferase Histone methyltransferase

Cat.No.  Name Information
M2358 3-Deazaneplanocin A 3-deazaneplanocin A (DZNeP), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.
M21676 EPZ-719 EPZ-719 is a First-in-Class, novel and potent SET domain-containing protein 2 (SETD2) inhibitor (IC50 = 0.005 μM), with a high selectivity over other histone methyltransferases.
M21487 Valemetostat tosylate Valemetostat tosylate (DS-3201 tosylate) is a first-in-class EZH1/2 inhibitor with IC50 < 10 nM. Valemetostat tosylate can be used in the study of relapsed and refractory peripheral T cell lymphoma.
M21486 CM-579 trihydrochloride CM-579 trihydrochloride is a dual inhibitor of G9a and DNA methyltransferase (DNMT), with IC50 values of 16 nM and 32 nM, respectively, as first-in-class, reversible. It plays an active role in a variety of cancer cells.
M21482 MS117 MS117 is a first-in-class, cell-active, irreversible covalent inhibitor of protein arginine methyltransferase (PRMT6) with an IC50 value of 18 nM.
M13848 MM-102 TFA MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
M13842 BCI-121 BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.
M13841 BAY-598 BAY-598 is selective small molecule inhibitor of SMYD2 with an IC50 of 27 nM.
M13341 VTP50469 VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL Interaction with a Ki value of 104 pM. VTP50469 has anti-leukemia activity.
M11474 EZM0414 EZM0414 is a potent, selective, oral bioavailable SETD2 inhibitor (IN SETD2 biochemical analysis, IC50=18 nM; In cell analysis, IC50=34 nM). EZM0414 can be used to study relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
M11245 PF-06726304 Pf-06726304 is an effective selective EZH2 inhibitor. Pf-06726304 inhibited wild type and Y641N mutant EZH2 with Ki of 0.7 and 3.0 nM, respectively. Pf-06726304 has strong anti-tumor growth activity.
M11243 CPI-169 Cpi-169 (CPI 169 R-Enantiomer) is a novel and effective EZH2 inhibitor, capable of inhibiting the activity of EZH2 WT, EZH2 Y641N and EZH1 with IC50 value of 0.24 nM, respectively. 0.51 nM and 6.1 nM.
M11242 EI1 EI1 (KB-145943) is a novel and effective EZH2 inhibitor, capable of acting on EZH2 (WT) and EZH2 (Y641F) with IC50 values of 15 nM and 13 nM, respectively.
M11241 Gambogenic acid Gambogenic acid is the active ingredient in Huangteng and has anti-cancer activity. Gambogenic acid is an effective EZH2 inhibitor, which specifically covalently binds to Cys668 in the EZH2-SET domain to induce EZH2 ubiquitination.
M11161 EBI-2511 EBI-2511 is an orally active, potent inhibitor of EZH2 in Pfeffiera cells IC50 The value is 6 nM.
M10845 LEM-14
M10532 Tazemetostat hydrobromide Tazemetostat (EPZ-6438) hydrobromide is a first-in-class potent, selective and orally available EZH2 inhibitor.
M9449 PFI-2 hydrochloride PFI-2 hydrochloride is a potent, highly selective and cell-active inhibitor of the methyltransferase activity of SETD7, with IC50 of 2 nM.
M9442 CM-272 CM-272 is a first-in-class, reversible dual small molecule inhibitor of G9a and DNMTs in hematologic malignancies.
M9151 MI-503 MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM.

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