| DC73316 |
WS-384 |
WS-384 is a specific, small-molecule inhibitor dually targeting LSD1 (IC50=338.8 nM) and the DCN1-UBC12 interaction (IC50=14.8 uM). |
|
| DC73317 |
ZY0511 |
ZY0511 is a highly selective and potent inhibitor of lysine-specific histone demethylase 1 (LSD1) with IC50 of 1.7 nM and SPR Kd of 2.42 nM. |
|
| DC73318 |
BBDDL2059 |
BBDDL2059 (BBDDL 2059) is a potent, selective and covalent inhibitor of EZH2 with IC50 of 1.5 nM (EZH2-Y641F), targeting the Cys663 of EZH2. |
|
| DC73319 |
BN104 |
BN104 (BNM-1192) is a potent, highly selective small molecule menin-MLL inhibitor, BNM-1192 is very potent against leukemia cell lines with MLL-fusion protein and NPM1 mutant (MV-4-11 (AF4 fusion), IC50=3.5 nM). |
|
| DC73320 |
C220 |
C220 (PRMT5 inhibitor C220) is a highly potent, selective and SAM cpmpetitive inhibitor of protein arginine methyltransferase 5 (PRMT5) with IC50 of 2.4 nM. |
|
| DC73321 |
CDIBA |
CDIBA is an allosteric inhibitors of m6A-RNA methyltransferase, METTL3 -14 complex with IC50 of 17.3 uM, also reported as a cytosolic phospholipase A2 (cPLA2) inhibitor. |
|
| DC73322 |
DP308
Featured
|
DP308 is a novel and effective 53BP1 tandem Tudor domain (TTD) inhibitor, disrupts the binding between 53BP1 and H4K20me2 peptide with IC50 of 1.69 uM. |
|
| DC73323 |
DS-1594a |
DS-1594a (Emilumenib) is a highly potent Menin-MLL1 inhibitor with IC50 of 1.4 nM in cell-free AlphaLISA assays, displays selective growth inhibition against AML and ALL cells with MLL1-r or NPM1c. |
|
| DC73324 |
EML1219 |
EML1219 is a selective small molecule inhibitor of protein arginine methyltransferase isoform PRMT9 with IC50 of 0.2 uM. |
|
| DC73325 |
EML734 |
EML734 is a selective small molecule inhibitor of protein arginine methyltransferase isoforms, PRMT7 and PRMT9 with IC50 of 0.32 and 0.89 uM, respectively. |
|
| DC73326 |
EPIC-0307 |
EPIC-0307 is a selective small-molecule inhibitor of PRADX-EZH2 interaction, inhibits GBM cell lines with IC50 of 12.13-17.69 uM, enhances temozolomide (TMZ) sensitivity to glioblastoma. |
|
| DC73327 |
EPZ028862 |
EPZ028862 is a potent, selective inhibitor of SMYD3 with biochemical IC50 of 1.8 nM, and function of cellular methylation IC50 of 32 nM. |
|
| DC73328 |
EPZ-031686 |
EPZ-031686 (EPZ 031686) is a potent, selective, small molecule SMYD3 inhibitor (Biochem IC50=3 nM, Cell IC50= 36 nM). |
|
| DC73329 |
HKMTI-1-005 |
HKMTI-1-005 is a potent, substrate-competitive dual inhibitor of EZH2 and the closely related G9A/GLP H3K9 methyltransferases with IC50 of 0.1 uM (EHMT2). |
|
| DC73330 |
IHMT-337
Featured
|
IHMT-337 (IHMT337) is a potent, highly selective and irreversible EZH2 inhibitor, specifically inhibits the methylation at H3K27. |
|
| DC73331 |
iPRMT1 |
iPRMT1 is a potent and selective PRMT1 inhibitor with IC50 of 270 nM, shows good selectivity over other PRMTs. |
|
| DC73332 |
JS1310 |
JS1310 (JS-1310) is a specific small-molecule PRMT7 inhibitor with IC50 of 5 uM (human PRMT7), displays no acitivity against type I PRMTs (PRMT1, 3, 4, 6, and 8, IC50 >100 uM) or the type II PRMT5 (IC50=50 uM). |
|
| DC73333 |
KMI169 |
KMI169 (KMI-169) is a potent and selective lysine methyltransferase 9 (KMT9) inhibitor with ITC Kd of 25 nM and enzymatic IC50 of 50 nM. |
|
| DC73334 |
KTX-1001 |
KTX-1001 is a potent, selective histone methyltransferase NSD2 (WHSC1, MMSET) inhibitor targeting the catalytic SET domain. |
|
| DC73335 |
M-808 |
M-808 (M808) is a highly potent, selective and covalent inhibitor of menin-MLL interaction with binding IC50 of 2.6 nM, forms a covalent bond with Cys329 in menin. |
|
| DC73336 |
MS-049 |
A potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50 of 34±10 nM and 43±7 nM, respectively. |
|
| DC73337 |
MS1262 |
MS1262 is a highly potent, selective and brain-penetrant inhibitor of G9a/GLP methylase with IC50 of 19/6 nM, respectively. |
|
| DC73338 |
PF-06821497 S enantiomer |
PF-06821497 S enantiomer is a novel potent, selective, orally bioavailable EZH2 inhibitor with Ki of <0.1 and 1.15 nM aginast both wt and mutant Y641N EZH2, respectively. |
|
| DC73339 |
PFI-2 |
A first-in-class, potent and selective inhibitor of SETD7 methyltransferase with Ki app/IC50 of 0.33/2 nM. |
|
| DC73340 |
PRT382 |
PRT382 (PRT-382) is a potent, selective and SAM-competitive PRMT5 inhibitor with IC50 of 2.8 nM in filtration binding assays with recombinant human PRMT5/MEP50 and histone H2A as the protein substrate. |
|
| DC73341 |
PRT543 |
PRT543 is a highly potent, selective and SAM cpmpetitive inhibitor of protein arginine methyltransferase 5 (PRMT5) with IC50 of 10.8 nM. |
|
| DC73342 |
SETDB1 activator (R,R)-59 |
(R,R)-59 is a small-molecule ligand activator for methyltransferase SETDB1 Triple Tudor Domain (3TD reader domain) with binding IC50 of 1.2 uM in TR-FRET assays, specifically promotes in vitro SETDB1-mediated methylation of lysine 64 of protein kinase Akt |
|
| DC73343 |
SKLB-03220 |
SKLB-03220 (SKLB03220) is a potent, selective EZH2 covalent inhibitor with IC50 of 1.72 nM (EZH2 WT). |
|
| DC73344 |
UNC7648 |
UNC7648 is a small molecule inhibitor of the methyl-lysine reader p53 binding protein 1 (53BP1) tandem Tudor domain (TTD) with TR-FRET IC50 of 8.6 uM. |
|
| DC73345 |
UNC9512 |
UNC9512 is a selective methyl-lysine reader p53 binding protein 1 (53BP1) antagonist, binds the 53BP1 tandem Tudor domain (TTD) with TR-FRET IC50 of 0.46 uM, and SPR/ITC Kd vfalues of 0.17/0.41 uM respectively. |
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