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Home > Inhibitors & Agonists > Epigenetics > Histone Methyltransferase (HMTase)

EEDi-5273

  Cat. No.:  DC47614   Featured
Chemical Structure
2585648-55-9
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More than 5000 active chemicals with high quality for research!
Field of application
EEDi-5273 is an exceptionally potent and orally efficacious embryonic ectoderm development (EED) inhibitor with IC50 of 0.2 nM and inhibits the KARPAS422 cell growth with IC50 of 1.2 nM. EEDi-5273 demonstrates an excellent PK and ADME profile, and its oral administration leads to complete and persistent tumor regression in the KARPAS422 xenograft model with no signs of toxicity.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2585648-55-9
Chemical Name: EEDi-5273
Synonyms: 15-[(5-Fluoro-2,3-dihydro-1-benzofuran-4-yl)methylamino]-9-propan-2-yl-5-(trifluoromethyl)-4,9,12,14;EEDi-5273 （APG-5918）;EEDi-5273
SMILES: FC1C=CC2=C(CCO2)C=1CNC1=NC=C2C3=CN=C(C(F)(F)F)C=C3CN(C(C3=C2N1C=N3)=O)C(C)C
Formula: C26H22F4N6O2
M.Wt: 526.49
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
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MSDS_31464_DC47614_2585648-55-9
COA
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Cat. No. Product name Field of application
DC72779 RK-701 RK-701 is an highly selective and non-genotoxic inhibitor of G9a with IC50 value of 23-27 nM. RK-701 selectively up-regulates HbF, γ- Globin, BGLT3 expression, down-regulates H3K9me2 expression. RK-701 also has inhibition for BCL11A and ZBTB7A.
DC71676 EZM0414 EZM0414 is a potent, selective, and orally bioavailable inhibitor of Histone-lysine N-methyltransferase SETD2.
DC47614 EEDi-5273 EEDi-5273 is an exceptionally potent and orally efficacious embryonic ectoderm development (EED) inhibitor with IC50 of 0.2 nM and inhibits the KARPAS422 cell growth with IC50 of 1.2 nM. EEDi-5273 demonstrates an excellent PK and ADME profile, and its oral administration leads to complete and persistent tumor regression in the KARPAS422 xenograft model with no signs of toxicity.
DC47117 MRTX-1719 MRTX-1719 is a potent first-in-class selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAPDEL SDMA cells.
DC46443 EML741 EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.
DC8662 WDR5-0103 WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.
DC9965 UNC3866 UNC3866 is a potent and selective antagonist of CBX4 and CBX7 chromodomains with (Kd ≈ 100 nM). It is 6- to 63-fold selective for these chromodomains over the other CBX and CDY chromodomains.
DC7332 UNC-1215 UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.
DC10024 UNC-1079 UNC1079 is the piperidine analog of UNC1021, as a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies.
DC7331 UNC-0638 UNC0638 is an inhibitor of protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.
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