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Chemical Structure| 2083627-02-3 Chemical Structure| 2083627-02-3

Structure of EED226
CAS No.: 2083627-02-3

Chemical Structure| 2083627-02-3

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EED226 is a potent and selective PRC2 inhibitor that directly binds to the H3K27me3 binding pocket of EED.

Synonyms: MAK683

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Product Details of EED226

CAS No. :2083627-02-3
Formula : C17H15N5O3S
M.W : 369.40
SMILES Code : O=S(C1=CC=C(C2=CN=C(NCC3=CC=CO3)N4C2=NN=C4)C=C1)(C)=O
Synonyms :
MAK683
MDL No. :MFCD30738018
InChI Key :DYIRSNMPIZZNBK-UHFFFAOYSA-N
Pubchem ID :123132228

Safety of EED226

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of EED226

epigenetics

Isoform Comparison

Biological Activity

Target
  • bromodomain

    PRC2, Kd:114 nM

    EED, Kd:82 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
KARPAS422 0.18 μM 7 days to evaluate the effect of EED inhibitors on cell growth; EED226 has an IC50 value of 0.18 μM in inhibition of KARPAS422 cell growth PMC8859984
Female Germline Stem Cells (FGSCs) 1, 5, 10 µM 24 hours and 48 hours EED226 significantly increased the survival rate of FGSCs by decreasing the enrichment of H3K27me3 on the Oct4 promoter and exon, enhancing OCT4 expression, and inhibiting P53 and P63 expression. PMC9874982
Murine renal tubular epithelial cells (mRTECs) 10 μM 48 hours To investigate the effect of EED226 on cisplatin-induced apoptosis in mRTECs, the results showed that EED226 significantly inhibited cisplatin-induced apoptosis. PMC9279598
HeLa cells 5 μM 24 hours To evaluate the degradation effect of UNC6852 on PRC2 components, results showed that UNC6852 significantly degraded EED and EZH2. PMC7004250
DB cells 10 μM 24 hours To evaluate the degradation effect of UNC6852 on PRC2 components, results showed that UNC6852 significantly degraded EED, EZH2, and SUZ12. PMC7004250
SK-HEP-1 cells 5 μM 72 hours EED226 treatment increases CXCL10 expression PMC8325240
PLC/PRF/5 cells 5 μM 72 hours EED226 treatment increases CXCL10 expression PMC8325240

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice KARPAS422 human B cell lymphoma xenograft model Oral gavage 300 mg/kg twice a day to determine the efficacy of EED226 in tumor regression; achieved complete KARPAS422 cell tumor regression. PMC8859984
C57BL/6J mice Cisplatin-induced acute kidney injury model Intragastric administration 40 mg/kg Twice a day for 48 hours To investigate the protective effect of EED226 on cisplatin-induced acute kidney injury, the results showed that EED226 significantly improved renal function, attenuated renal tubular cell apoptosis and inflammatory response. PMC9279598
Mice hepatic tumor model Intraperitoneal injection 20 mg/kg 5 days a week for 28 days EZH2 inhibitor GSK343 induces tumor suppression through reexpression of CXCL10 PMC8325240

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02900651 Diffuse Large B-cell Lymphoma PHASE1 TERMINATED 2024-10-09 UCSF ., San Francisco, Califor... More >>nia, 94115, United States|UCLA Santa Monica Hematology Oncology, Santa Monica, California, 90404, United States|Uni Of TX MD Anderson Cancer Cntr Dept of Onc, Houston, Texas, 77030, United States|Novartis Investigative Site, Toronto, Ontario, M5G 2M9, Canada|Novartis Investigative Site, Chengdu, Sichuan, 610041, China|Novartis Investigative Site, Shanghai, 200032, China|Novartis Investigative Site, Villejuif, 94800, France|Novartis Investigative Site, Freiburg, 79106, Germany|Novartis Investigative Site, Koeln, 50937, Germany|Novartis Investigative Site, Hong Kong, Hong Kong|Novartis Investigative Site, Milano, MI, 20133, Italy|Novartis Investigative Site, Rozzano, MI, 20089, Italy|Novartis Investigative Site, Fukuoka-city, Fukuoka, 811-1395, Japan|Novartis Investigative Site, Sunto Gun, Shizuoka, 411 8777, Japan|Novartis Investigative Site, Singapore, 168583, Singapore|Novartis Investigative Site, Madrid, 28041, Spain Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.54mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL

References

 

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