RO-2443
RO-2443 is a dual MDM2/MDMX-p53 antagonist with an IC50 value of 33 nM for MDM2 and an IC50 value of 41 nM for MDMX. RO-2443 binds to the ZMP domain of ZMP-RNase L, inducing its dimerization. RO-2443 can be used for research on cancer and innate immune responses.
For research use only. We do not sell to patients.
- CAS No.: 1416663-79-0
- Formula: C20H14ClF2N3O2
- Molecular Weight:401.80
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
MDMX 41 nM (IC50) |
MDM2 33 nM (IC50) |
In Vitro
RO-2443 is a dual p53-MDM2/p53-MDMX antagonist with IC50 values of 33 nM for MDM2 and 41 nM for MDMX in cell-free binding assays[2].
RO-2443 binds the MDMX p53-interaction domain with KD 78 nM and induces its dimerization[3].
RO-2443 is a dual MDM2/MDMX-p53 binding inhibitor with IC50 values of 33 nM for MDM2 and 41 nM for MDMX in a cell-free TR-FRET assay[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1416663-79-0
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Molecular Weight 401.80
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Formula C20H14ClF2N3O2
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SMILES
C(C=1C=2C(=C(C)C(Cl)=CC2)NC1)=C3C(=O)N(CC4=CC(F)=C(F)C=C4)C(=O)N3
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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.
Purity & Documentation
References
[2]. Graves B, et al. Activation of the p53 pathway by small-molecule-induced MDM2 and MDMX dimerization. Proceedings of the National Academy of Sciences of the United States of America. 2012 Jul 17;109(29):11788-93. [Content Brief]
[4]. Zhang Q, et al. Targeting p53-MDM2-MDMX loop for cancer therapy. Sub-cellular biochemistry. 2014;85:281-319. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RO-2443 Related Classifications
HY-123866 Related Classifications
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