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. |
M58231 | CMP-5 dihydrochloride | CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. |
M55566 | EPIC-0628 | EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. EPIC-0628 EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. |
M29434 | BAY-6035 | BAY-6035 is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC50 of 88 nM. |
M28444 | MM-401 TFA | MM-401 (TFA) is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 µM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia. |
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. |
M13839 | AZ505 | AZ505 is a potent and selective SMYD2 inhibitor with an IC50 of 0.12 μM. |
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. |
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