EED-IN-3
EED-IN-3 is an orally active EED inhibitor. EED-IN-3 effectively inhibits PRC2 by binding to EED (IC50 = 0.62 μM for EED) and downregulates H3K27me3. EED-IN-3 can efficiently and selectively inhibit PC3 cells with the IC50 of 3.69 μΜ and could significantly suppress colony formation and migration. EED-IN-3 can be used for research on prostate cancer.
For research use only. We do not sell to patients.
- CAS No.: 3051817-48-9
- Formula: C25H29N3O5
- Molecular Weight:451.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
Description
In Vitro
EED-IN-3 (Compound 39) (7 days) exhibits highly selective anticancer activity against PC3 cells and low toxicity against normal cells, including PC3 (IC50 = 3.69 μM), EC109 (IC50 = 26.8 μM), KYSE150 (IC50 = 24.53 μM) and PC9 (IC50 = 18.43 μM)[1].
EED-IN-3 (0-16 μM) significantly reduce the level of H3K27me3 in PC3 cells[1].
EED-IN-3 (0-16 μM, 24 or 48 h) can inhibit PC3 cell migration and invasion in a time-and concentration dependent manner[1].
EED-IN-3 (8-16 μM, 12 days) significantly inhibits the formation of cell colonies in PC3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:PC3 cells
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Concentration:3 μM or 6 μM
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Incubation Time:4 days
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Result:Effectively upregulated the expression of E-Cadherin and downregulated the expression of N-Cadherin.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | p.o. | 2.23 h | 1.50 h | 20.0 ng/mL | 73.8 ng·h/mL | 81.3 ng·h/mL | 2.66 h | 3.42 h |
In Vivo
EED-IN-3 (50 mg/kg-100 mg/kg; i.g.; once daily; for 14 days) has a significant inhibitory effect on tumor growth in the PC3 cells injected BALB/C-nu mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 wild-type mice (8-12 weeks)[1]
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Dosage:Single dose 2 g/kg
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Administration:Oral gavage (i.g.)
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Result:Did not cause any abnormal weight changes and did not cause histopathological changes in important organs.
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Animal Model:1×107 PC3 cells injected the BALB/C-nu mice[1]
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Dosage:50 mg/kg or 100 mg/kg
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Administration:Oral gavage (i.g.); once daily for 14 days
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Result:Inhibited tumor growth by nearly 50% in the 50 mg/kg/day group and nearly 80 % in the 100 mg/kg/day group, steadily increased body weight.
Chemical Information
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CAS No. 3051817-48-9
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Molecular Weight 451.51
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Formula C25H29N3O5
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SMILES
COC1=CC=C(C=C1)C2=NN(C(C(C(NCCCOC(C)C)=O)=C2)=O)C3=CC=C(C=C3)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Soft Agar Colony Formation Assay
Soft agar colony formation assay measures anchorage-independent growth, in which transformed or tumorigenic cells proliferate as colonies in a semisolid agar matrix while many non-transformed adherent cells fail to proliferate without attachment; classic studies showed that growth in semisolid medium correlates with tumorigenicity in nude mice, and later protocol papers describe the method as a stringent in vitro assay for malignant transformation. The readout is the number, size, morphology, or signal intensity of colonies formed within agar after incubation; published formats include manual colony counting after staining, 96-well or 384-well quantitative formats, DNA-binding dye detection, MTT/tetrazolium-based detection, digital image analysis, and PCR-based marker detection from soft agar cultures.
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Colony Formation (Clonogenic) Assay
The clonogenic (colony formation) assay measures the ability of a single cell to retain reproductive viability and form a macroscopic colony, typically defined as a cluster derived from one progenitor cell after a defined growth period. This assay is widely used to evaluate cell survival after exposure to ionizing radiation or cytotoxic treatments and is considered a standard method in radiation biology for generating dose-response relationships of reproductive cell death. Colony formation reflects long-term proliferative capacity rather than short-term metabolic activity, and survival is quantified by comparing treated versus untreated conditions based on colony number and derived survival fractions.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)