- Signaling Pathways
- Apoptosis
- MDM-2/p53
MDM-2/p53
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.
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MDM-2/p53 Related Products (639)
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Antibodies (17)
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MDM-2/p53 Signaling Pathway
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SEN205A
0 ImagesCat. No.: HY-W237439CAS No.: 958712-85-1SEN205A is a fragment compound that binds to the hydrophobic pocket of human S100B (Kd=0.5-1.0 mM), which is the key region for the interaction of S100B with TRTK-12 and p53, and SEN205A can be displaced from this site by TRTK-12. SEN205A exhibits excellent in vitro ADME properties, including high metabolic stability, chemical stability, and good solubility under physiological pH conditions. SEN205A can serve as a starting fragment for structure-based optimization to develop inhibitors targeting the S100B-p53 protein-protein interaction and investigate the pathogenesis of malignant melanoma. -
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RETRA hydrobromide
0 ImagesCat. No.: HY-113843CAS No.: 1035875-01-4RETRA (hydrobromide) is a mutant p53-dependent activator of p73 that can inhibit cancer cells carrying mutant p53. RETRA (hydrobromide) increases the expression level of p73, induces transcriptional activation of several common to transcriptional targets p53 and p73, which leads to mutant p53- and p73-dependent inhibition of tumor growth, reduction of colony formation and induction of effector caspases. -
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Neuroprotective agent 11
0 ImagesCat. No.: HY-174260CAS No.: 3081915-81-0Neuroprotective agent 11 (Compound 1a) is an orally active polyphenol compound with significant protective effects against cerebral ischemia. The main activities of Neuroprotective agent 11 include inhibiting neuronal inflammation and apoptosis, reducing cerebral infarction volume, and improving behavioral symptoms of cerebral ischemic mice. Neuroprotective agent 11 exerts its regulatory mechanism by downregulating the expression of inflammatory factors (iNOS、COX-2) and apoptotic proteins (cleaved-Caspase3, p53). Neuroprotective agent 11 can be used in the study of cerebral ischemia-related diseases (such as ischemic stroke). -
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BI-0252
0 ImagesCat. No.: HY-100765CAS No.: 1818291-27-8 -
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MC3817 free base
0 ImagesCat. No.: HY-179409AMC3817 free base is a selective DNMT1 inhibitor. MC3817 free base inhibits DNMT1 and DNMT3A/3L with IC50s of 0.044 μM and > 10μM, respectively. MC3817 free base inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage. MC3817 free base elevates cleaved Caspase 3, P53, and γH2AX. MC3817 free base can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research. -
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Antitumor agent-60
0 ImagesCat. No.: HY-146432CAS No.: 865784-65-2Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model. -
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WMJ-J-09
0 ImagesWMJ-J-09 is an HDAC inhibitor with IC50 values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research[1][2]. -
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- FOXO4-DRI acetate
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MI 63
0 ImagesCat. No.: HY-18330CAS No.: 908027-21-4 -
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MAPK-IN-3
0 ImagesCat. No.: HY-169412CAS No.: 2848599-79-9MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK. -
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Lobetyol
0 ImagesCat. No.: HY-117652CAS No.: 136171-87-4Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity. Lobetyol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. -
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FMP
0 ImagesCat. No.: HY-168877FMP is a Platinum(IV) complexe. FMP significantly upregulates the expression of γ-H2AX and p53. FMP increases the production of ROS. FMP markedly upregulates the expressions of Apoptosis-related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP shows antiproliferative activity against breast cancer. -
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SPDI-48-T1
0 ImagesCat. No.: HY-P11255SPDI-48-T1 is a lysine-stapled peptide. SPDI-48-T1 exhibits discernible binding affinities for MDM2 and MDMX, with Kd values of 396 nM and 456 nM, respectively. SPDI-48-T1 exhibits anticancer activity against breast cancer, colorectal cancer, non-small cell lung cancer, cervical cancer, and malignant melanoma. -
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Hdm2 E3 ligase inhibitor 1
0 ImagesCat. No.: HY-131667CAS No.: 414905-09-2Hdm2 E3 ligase inhibitor 1 (Compound 1) is a reversible inhibitor for Hdm2 (an E3 ubiquitin ligase)-mediated ubiquitination of the p53 protein with an IC50 of 12.7 μM. Hdm2 E3 ligase inhibitor 1 binds Hdm2, blocks Hdm2-catalyzed ubiquitin transfer from preligated Ub-Ubc4 to p53, inhibits p53 ubiquitination, stabilizes p53 protein in tumor cell and exhibits antitumor efficacy. -
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Minocycline-d6 hydrochloride
0 ImagesCat. No.: HY-17412SCAS No.: 1035979-33-9Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect. -
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UCI-14
0 ImagesUCI-14 is a gltA1/lprQ modulator with in vitro anti-tuberculosis activity against drug-sensitive and multidrug-resistant mycobacteria. UCI-14 upregulates the expression of genes encoding citrate synthase I, downregulates the expression of genes encoding conserved mycobacterial lipoprotein, and alters the carbon metabolism of mycobacteria. UCI-14 reactivates the expression of wild-type p53 target genes in p53-mutated cells. UCI-14 can be used in the research of tuberculosis and cancer. -
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PROTAC MAGL degrader-1
0 ImagesCat. No.: HY-173369PROTAC MAGL degrader-1 is an orally active, moderately blood-brain barrier permeable bifunctional PROTAC (DC50: 60.28 nM) that possesses MAGL degradation activity alongside MDM2 inhibitory activity. PROTAC MAGL degrader-1 recruits E3 ubiquitin ligase MDM2 to mediate ubiquitination of MAGL and subsequent proteasomal degradation. PROTAC MAGL degrader-1 blocks the interaction between MDM2 and P53 and upregulates the expression of tumor suppressor protein P53. PROTAC MAGL degrader-1 is applicable for research on glioblastoma stem cells, melanoma and breast cancer. -
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Topoisomerase I-IN-18
0 ImagesCat. No.: HY-178373Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, γH2AX phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer. -
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AM-7209
0 ImagesCat. No.: HY-12941CAS No.: 1623432-51-8AM-7209 is a potent and selective MDM2-p53 interaction inhibitor with a Kd of 38 pM. AM-7209 inhibits the MDM2 amplified SJSA-1 osteosarcoma cell line with an IC50 of 1.6 nM. AM-7209 shows antitumor activities. -
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TCF4/β-catenin-IN-1
0 ImagesCat. No.: HY-172393TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin, and induces apoptosis. TCF4/β-catenin-IN-1 up-regulates p53, caspase-3, caspase-8, caspase-9 levels and Bax protein expression as well as down-regulates Bcl-2 protein expression. TCF4/β-catenin-IN-1 can inhibit CYP3A4, CYP1A2, CYP2C19, and shows promising cytotoxic activity in cancer cells. -
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p53 is at the centre of biological interactions that translates stress signals into cell cycle arrest or apoptosis. Upstream signaling to p53 increases its level and activates its function as a transcription factor in response to a wide variety of stresses, whereas downstream components execute the appropriate cellular response.
Cell Stress: p53 induction by acute DNA damage begins when DNA double-strand breaks trigger activation of ATM, a kinase that phosphorylates the CHK2 kinase, or when stalled or collapsed DNA replication forks recruit ATR, which phosphorylates CHK1. p53 is a substrate for both the ATM and ATR kinases, as well as for CHK1 and CHK2, which coordinately phosphorylate p53 to promote its stabilization. These phosphorylation events are important for p53 stabilization, as some of the modifications disrupt the interaction between p53 and its negative regulators MDM2 and MDM4. MDM2 and MDM4 bind to the transcriptional activation domains of p53, thereby inhibiting p53 transactivation function, and MDM2 has additional activity as an E3 ubiquitin ligase that causes proteasome-mediated degradation of p53. Phosphorylation also allows the interaction of p53 with transcriptional cofactors, which is ultimately important for activation of target genes and for responses such as cell cycle arrest, DNA repair, apoptosis and senescence. Non-receptor tyrosine kinase c-Abl can also be activated by DNA damage. Then the JNK/p38 is activated and leads to p53 activation[1][2].
Oncogenic signaling: The response to oncogene activation depends on the binding of ARF to MDM2. ARF is normally expressed at low levels in cells. Inappropriately increased E2F or Myc signals, stemming from oncogene activation, leads to the increased expression of ARF, which inhibits MDM2 by blocking its E3 ubiquitin ligase activity, uncoupling the p53-MDM2 interaction, thereby segregating it from nucleoplasmic p53[3].
The PI3K-Akt pathway activates MDM2 and increases the ubiquitination of p53.
Reference:
[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.