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Chemical Structure| 1628830-21-6 Chemical Structure| 1628830-21-6

Structure of EZM 2302
CAS No.: 1628830-21-6

Chemical Structure| 1628830-21-6

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EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC50 value of 6 nM.

Synonyms: GSK3359088

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Product Details of EZM 2302

CAS No. :1628830-21-6
Formula : C29H37ClN6O5
M.W : 585.09
SMILES Code : O=C(N(CC1)CCC21CN(C3=NC(C4=CC(OC[C@H](O)CNC)=CC=C4Cl)=NC(C5=C(C)ON=C5C)=C3C)C2)OC
Synonyms :
GSK3359088
MDL No. :MFCD31657380
InChI Key :OWCOTUVKROVONT-HXUWFJFHSA-N
Pubchem ID :90425581

Safety of EZM 2302

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

Related Pathways of EZM 2302

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
10T1/2 cells 1 μM 72 hours To evaluate the effect of EZM2302 on cell growth, results showed that EZM2302 inhibited cell proliferation. PMC11415932
MCF7 cells 1 μM 72 hours To evaluate the effect of EZM2302 on cell growth, results showed that EZM2302 inhibited cell proliferation. PMC11415932
RPMI-8226 0.0003 to 5 µM 96 hours To assess the effect of EZM2302 on cellular methylation levels, results showed significant decrease in methylation of PABP1 and SmB PMC5740082
NCI-H929 0.0003 to 5 µM 96 hours To assess the effect of EZM2302 on cellular methylation levels, results showed significant decrease in methylation of PABP1 and SmB PMC5740082
U266B1 0.0003 to 5 µM 96 hours To assess the effect of EZM2302 on cellular methylation levels, results showed significant decrease in methylation of PABP1 and SmB PMC5740082
10T1/2 cells 100 nM 72 hours To investigate the effect of EZM 2302 on DRP1 methylation, results showed that EZM 2302 treatment reduced DRP1 methylation. PMC11179627
MEFs 100 nM 96 h To investigate the effect of CARM1 on Pontin methylation under glucose starvation, it was found that the CARM1-specific inhibitor EZM2302 significantly reduced Pontin methylation. PMC7722926
LoVo cells 10 ×10−9m 24 hours Inhibited CARM1 activity, blocking methylation and degradation of ACSL4 protein PMC10754121
HCT116 cells 10 ×10−9m 24 hours Inhibited CARM1 activity, blocking methylation and degradation of ACSL4 protein PMC10754121
PC9 cells 10 nM 48 hours Inhibition of CARM1 enzymatic activity significantly reduced the proliferative and colony-forming abilities of PC9 and HCC827 cells, indicating that the inhibition of CARM1 enzymatic activity suppresses NSCLC progression by repressing CCNE2 expression. PMC7346078
HCC827 cells 10 nM 48 hours Inhibition of CARM1 enzymatic activity significantly reduced the proliferative and colony-forming abilities of PC9 and HCC827 cells, indicating that the inhibition of CARM1 enzymatic activity suppresses NSCLC progression by repressing CCNE2 expression. PMC7346078

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Immunocompetent mouse model and humanized mouse model Oral 0.05–0.4 mg/kg Single dose, measured after 24 hours The combination of EZM2302 and an anti-PD-1 antibody exerted promising synergistic effects in a preclinical model. PMC9077876
CB-17 SCID mice multiple myeloma xenograft model oral 50 mg/kg 5 injections each week for 5 weeks To evaluate the anti-tumor activity of EZM2302 in vivo, results showed dose-dependent tumor growth inhibition PMC5740082
C57 mice MC38 xenograft model Oral 3 mg/kg twice daily for 2 weeks Enhanced immunotherapy efficacy and promoted ferroptosis PMC10754121

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.71mL

0.34mL

0.17mL

8.55mL

1.71mL

0.85mL

17.09mL

3.42mL

1.71mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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