DC73309 |
YSR734 |
YSR734 is a first-in-class covalent HDACs inhibitor with IC50 of 0.109 uM, 0.154 uM and 0.143 uM for HDAC1, HDAC2, and HDAC3, sparing other deacetylases (HDAC4-HDAC10, IC50>10 uM). |
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DC73310 |
JG-2016 |
JG-2016 is a small molecule inhibitor of histone acetyltransferase 1 (HAT1) with IC50 of 14.8 uM in the HAT1 acetylation assays. |
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DC73311 |
MC4171 |
MC4171 (KAT8 inhibitor 34) is a first-in-class, selective and reversible lysine acetyltransferase KAT8 inhibitor with IC50 of 8.1 uM and SPR Kd of 2.04 uM. |
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DC73312 |
CBA-1 |
CBA-1 is a small molecule inhibitor of Wnt signaling, specifically targets Jumonji (JmjC) domain-containing demethylase KDM3A with IC50 of 3.9 uM. |
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DC73313 |
EPZ020809 |
EPZ020809 is a potent, specific KDM4C inhibitor with Ki of 31 nM, binds KDM4C in a 2-OG-competitive fashion. |
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DC73314 |
FTO-43 |
FTO-43 (FTO-43 N) is a potent, selective inhibitor of the m6A demethylase fat mass- and obesity-associated protein (FTO) with IC50 of 1.0 uM, no significant acitivity against the homologous m6A RNA demethylase ALKBH5 (IC50>40 uM). |
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DC73315 |
iPHF8 |
iPHF8 (inhibitor of PHF8) is a specific inhibitor of protein demethylase PHF8 with IC50 of 2.01 uM in Succinate-Glo JmjC demethylase assays, and SPR KD value of 240 nM. |
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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). |
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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. |
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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. |
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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). |
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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. |
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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. |
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DC73322 |
DP308
Featured
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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. |
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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. |
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DC73324 |
EML1219 |
EML1219 is a selective small molecule inhibitor of protein arginine methyltransferase isoform PRMT9 with IC50 of 0.2 uM. |
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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. |
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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. |
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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. |
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DC73328 |
EPZ-031686 |
EPZ-031686 (EPZ 031686) is a potent, selective, small molecule SMYD3 inhibitor (Biochem IC50=3 nM, Cell IC50= 36 nM). |
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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). |
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DC73330 |
IHMT-337
Featured
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IHMT-337 (IHMT337) is a potent, highly selective and irreversible EZH2 inhibitor, specifically inhibits the methylation at H3K27. |
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DC73331 |
iPRMT1 |
iPRMT1 is a potent and selective PRMT1 inhibitor with IC50 of 270 nM, shows good selectivity over other PRMTs. |
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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). |
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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. |
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DC73334 |
KTX-1001 |
KTX-1001 is a potent, selective histone methyltransferase NSD2 (WHSC1, MMSET) inhibitor targeting the catalytic SET domain. |
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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. |
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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. |
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DC73337 |
MS1262 |
MS1262 is a highly potent, selective and brain-penetrant inhibitor of G9a/GLP methylase with IC50 of 19/6 nM, respectively. |
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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. |
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