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You are here:Home-Inhibitors & Agonists-Apoptosis-MDM2-p53

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The p53 tumor suppressor is a principal mediator of growth arrest, senescence, and apoptosis in response to a broad array of cellular damage. p53 is a short-lived protein that is maintained at low, often undetectable, levels in normal cells. Under stress conditions, the p53 protein accumulates in the cell, binds in its tetrameric form to p53-response elements and induces the transcription of various genes.


MDM-2 is transcriptionally activated by p53 and MDM-2, in turn, inhibits p53 activity in several ways. MDM-2 binds to the p53 transactivation domain and thereby inhibits p53-mediated transactivation. MDM-2 also contains a signal sequence that is similar to the nuclear export signal of various viral proteins and, after binding to p53, it induces its nuclear export. As p53 is a transcription factor, it needs to be in the nucleus to be able to access the DNA; its transport to the cytoplasm by MDM-2 prevents this. Finally, MDM-2 is a ubiquitin ligase, so is able to target p53 for degradation by the proteasome.


In many tumors p53 is inactivated by the overexpression of the negative regulators MDM2 and MDM4 or by the loss of activity of the MDM2 inhibitor ARF. The pathway can be reactivated in these tumors by small molecules that inhibit the interaction of MDM2 and/or MDM4 with p53. Such molecules are now in clinical trials.



References:


1. Chène P, et al. Inhibiting the p53-MDM2 interaction: an important target for cancer therapy. Nat Rev Cancer. 2003 Feb;3(2):102-9.

2. Brown CJ, et al. Awakening guardian angels: drugging the p53 pathway. Nat Rev Cancer. 2009 Dec;9(12):862-73. 

3. Polager S, et al. p53 and E2f: partners in life and death. Nat Rev Cancer. 2009 Oct;9(10):738-48. doi: 10.1038/nrc2718

Cat. No. Product Name CAS No. Information
H9040

MI 147 hydrochloride

 		1201143-82-9

MI 147 hydrochloride is a potent,an oral MDM2 inhibitor with Ki values of 0.6 nM ,effectively inhibits tumor growth in the SJSA-​1 xenograft model.
H9039

MI 147

 		908027-40-7

MI 147 is a potent,an oral MDM2 inhibitor with Ki values of 0.6 nM ,effectively inhibits tumor growth in the SJSA-​1 xenograft model.
H9015

MI-888

 		1303607-59-1

MI-888 is a highly potent ,an oral MDM2 inhibitor with IC50 of 6.8±0.9 nM; MI-888 was capable of achieving complete and long-lasting tumor regression in animal models of human cancer upon oral administration.
H8885

Sulanemadlin

 		1451199-98-6

Sulanemadlin is a potent p53-​based peptidomimetic macrocycles as inhibitors of the p53-​MDM2, p53-​MDMX, or both p53 and MDM2 and MDMX protein-​protein interactions useful in treatment of cancers.
H8733

MEL23

 		642072-49-9

MEL23 is an inhibitor of the MDM2–MDMX heterocomplex's E3 ligase activity,MEL23 effectively inhibited cell death caused by protein protein.
H1722

YH239-EE

 		1364488-67-4

YH239-EE is the ethyl ester of YH239, which is a highly potent, selective MDM2-p53 antagonist with Ki of 300 nM, shows no affinity for MDM4; induces apoptosis in AML cells and patient samples, induces p53 and activates the apoptotic caspase 3/7 in MOLM-13 (wt-p53) cells.
H1721

WK-298

 		1067654-70-9

A potent small molecule inhibitor that binds and disrupts the MDM2/MDMX-p53 interaction with IC50 of 0.19 uM and 19.7 uM, respectively.
H1720

UNC-2170 maleate

 		2173992-60-2

A small molecule ligand for the methyl-lysine binding protein 53BP1 (p53-binding protein 1) with Kd of 22 uM against the 53BP1 tandem tudor domain; highly cell permeant with no significant measureable cellular efflux; shows modestly potent, demonstrates at least 17-fold selectivity for 53BP1 as compared to nine other Kme reader proteins.
H1719

UNC-2170

 		1648707-58-7

UNC-2170 is a small molecule ligand for the methyl-lysine binding protein 53BP1 (p53-binding protein 1) with Kd of 22 uM against the 53BP1 tandem tudor domain; is highly cell permeant with no significant measureable cellular efflux; shows modestly potent, demonstrates at least 17-fold selectivity for 53BP1 as compared to nine other Kme reader proteins.
H1718

Tenovin-3

 		1011301-27-1

A sirtuin inhibitor that increases p53 levels in MCF-7 cells.

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