An important mediator of growth arrest, senescence, and apoptosis in response to a wide range of cellular damage is the tumor suppressor protein p53. In healthy cells, the short-lived protein p53 is kept at very low levels that are frequently undetectable. When under stress, the p53 protein builds up in the cell, binds to p53-response elements in its tetrameric form, and triggers the transcription of a number of genes.
P53 causes MDM-2 to become transcriptionally active, and MDM-2 then inhibits p53 activity in a number of ways. MDM-2 inhibits p53-mediated transactivation by attaching to the p53 transactivation domain. After binding to p53, MDM-2 induces nuclear export because it has a signal sequence that is similar to the nuclear export signal of several viral proteins. Because p53 is a transcription factor, MDM-2's transport of it to the cytoplasm prevents it from accessing the DNA, which is necessary for its function. Finally, because MDM-2 is an ubiquitin ligase, it can direct the proteasome to target p53 for destruction.
The overexpression of the negative regulators MDM2 and MDM4 or the diminished activity of the MDM2 inhibitor ARF both inactivate p53 in many tumors. In these tumors, small molecules that block the interaction of MDM2 and/or MDM4 with p53 can cause the pathway to be reactivated. Trials on such molecules are currently being conducted.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
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![2-Ammo-3-memyl-imidazo-[4,5-f]-quinoIine](http://www.invivochem.com/upload/0201/V107016.png)
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V107016 | 2-Ammo-3-memyl-imidazo-[4,5-f]-quinoIine | 76180-96-6 | 2-Amino-3-methyl-imidazo[4,5-f]-quinoline is a mutagenic compound. |
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V2657 | A-1155463 | 1235034-55-5 | A-1155463 (A1155463) is a novel highly potent and selective BCL-XL inhibitor with antitumor activity. |
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V2656 | A-1331852 | 1430844-80-6 | A-1331852 (A1331852) is a potent and selective BCL-XL inhibitor with anticancer and immunomodulatory effects. |
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V115267 | AKT-100 | 3076960-67-0 | AKT-100 is a p53 activator. |
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V109037 | ATSP-7342 | 1451198-97-2 | ATSP-7342 is a negative control analog of ATSP-7041. |
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V2655 | BDA-366 | 1821496-27-8 | BDA-366 (BDA366) is a potent andselective small-molecule antagonist of the Bcl2-BH4 domain with potential anticancer activity. |
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V109113 | BW-AQ-113 | 1537900-10-9 | BW-AQ-113 is an anthraquinone derivative. |
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V110530 | Dimethyl bisphenolate | Dimethyl bisphenol ester (compound DMB) is a natural neolignan derivative with oral antitumor activity. | |
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V109137 | DPMI-ω | DPMI-ω is a bispecific D-peptide antagonist that can antagonize the oncogenic proteins MDM2 and MDMX. | |
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V118718 | dsP53-285 saRNA | dsP53-285 saRNA is a small activating RNA (saRNA) that can easily activate the expression of wild-type p53 by targeting its promoter. | |
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V2651 | Eprenetapopt (APR246; PRIMA-1MET) | 5291-32-7 | Eprenetapopt (APR-246; PRIMA-1MET), a methylated derivative of PRIMA-1 and a mutant p53 reactivator, is a novel and potent small molecule compoundthat is able to restore wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. |
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V3166 | HDM201 (Siremadlin) HCl | 1448867-42-2 | HDM201 HCl (also called Siremadlin;NVP-HDM201, HDM stands for human double minute 2 homolog) is an orally bioavailable, highly potent and selective inhibitor of the p53-Mdm2 protein-protein interaction. |
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V115851 | ISA 27 | 1254366-73-8 | ISA 27 is a small molecule inhibitor of MDM2-p53 protein-protein interactions. |
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V85381 | JN122 | JN122 is a spiroindoline-containing molecule and is a MDM2 inhibitor. | |
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V115521 | LQFM030 | 2180931-49-9 | LQFM030 is an MDM2 inhibitor. |
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V83557 | MDM2-IN-24 | ||
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V83552 | MDM2-IN-26 | 1818393-11-1 | |
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V86068 | MDM2-p53-IN-18 | 1818291-95-0 | |
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V85877 | MDM2-p53-IN-20 | 2095120-09-3 | |
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V51571 | MDM2/XIAP-IN-2 | 2761969-85-9 | dual inhibitor of MDM2/XIAP |
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