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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC73348 40569Z
40569Z is a specific SIRT7 inhibitor, significantly inhibits SIRT7 deacetylation activity without effects on SIRT1 and SIRT6 activities, induces apoptosis and increases chemosensitivity to sorafenib in human liver cancer.
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DC73347 2800Z
2800Z is a specific SIRT7 inhibitor, significantly inhibits SIRT7 deacetylation activity without effects on SIRT1 and SIRT6 activities, induces apoptosis and increases chemosensitivity to sorafenib in human liver cancer.
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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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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.
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DC73343 SKLB-03220
SKLB-03220 (SKLB03220) is a potent, selective EZH2 covalent inhibitor with IC50 of 1.72 nM (EZH2 WT).
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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
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DC73341 PRT543
PRT543 is a highly potent, selective and SAM cpmpetitive inhibitor of protein arginine methyltransferase 5 (PRMT5) with IC50 of 10.8 nM.
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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.
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DC73339 PFI-2
A first-in-class, potent and selective inhibitor of SETD7 methyltransferase with Ki app/IC50 of 0.33/2 nM.
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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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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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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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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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DC73334 KTX-1001
KTX-1001 is a potent, selective histone methyltransferase NSD2 (WHSC1, MMSET) inhibitor targeting the catalytic SET domain.
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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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