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ApoptosisMDM-2/p53
p53 is a key tumor suppressor protein and transcription factor, which plays a crucial role in cell cycle regulation, DNA repair, apoptosis and stress response. MDM2 is the most important negative regulator of p53, which directly binds to the N-terminal end of the p53 transcription activation domain to inhibit the transactivation of p53, with the functions of inhibiting cell growth, inducing apoptosis and regulating the cell cycle. Blocking the interaction between MDM2 and p53 protein can restore the oncogenic function of p53 wild type.
D-(-)-3-Phosphoglyceric acid disodium
3-Phospho-D-glyceric acid disodium
T3718580731-10-8
D-(-)-3-Phosphoglyceric acid disodium (3-Phospho-D-glyceric acid disodium) is an intermediate in glycolysis/gluconeogenesis and the biosynthesis of serine, glycine, and threonine, competitively inhibiting yeast enolase. It also functions as an intermediate in biosynthetic pathways in plants, eukaryotes, and prokaryotes.
- $30
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QTY
Darizmetinib
HRX215, HRX-0215
T729562369583-33-3
Darizmetinib (HRX215, HRX-0215) is an MKK4 inhibitor. Inhibition of MKK4 leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration.
- $70
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Milademetan
RAIN-32, DS3032b, DS-3032
T120401398568-47-2In house
Milademetan (DS-3032) is an orally active and potent MDM2 inhibitor with antitumor activity that induces G1 cell cycle arrest, senescence, and apoptosis.Milademetan is used in the study of acute myeloid leukemia and solid tumors.
- $89
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Nutlin-3a
Nutlin-3a chiral, (−)-Nutlin-3, (-)-Nutlin-3
T6023675576-98-4
Nutlin-3a is the active enantiomer of Nutlin-3, an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3a binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3a has antitumor activity.
- $45
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USP7-IN-4
USP7-IN-2, USP7 inhibitor ALM4, AD-04
T698202196243-57-7
USP7-IN-4(USP7 inhibitor ALM4) is a non-competitive, potent and selective inhibitor of USP7 (ubiquitin-specific protease 7) with an IC50 = 6 nM, up-regulates p53 and p21, down-regulates MDM2, increases the level of ubiquitination of MDM2, and exhibits anti-proliferative activity in a variety of cancer cell lines, with an EC50 = 2.0 nM in RS4;11 (acute lymphoblastic leukemia cell line) .
- $333
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QTY
SAR405838
MI-77301, MI-773, MI773, MI 773
T65851303607-60-4In house
MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
- $45
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C16 Ceramide
Palmitoyl Ceramide, N-Palmitoylsphingosine, N-acylsphingosine, C16 Ceramide (d18:1/16:0)
T3756224696-26-2
C16 Ceramide (Palmitoyl Ceramide) is a naturally occurring small molecule that activates p53 by directly and selectively binding to it.
- $39
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CBL0137 hydrochloride
Curaxin-137 hydrochloride, Curaxin 137 hydrochloride, CBL-C137 hydrochloride, CBLC137 hydrochloride
T43611197397-89-9
CBL0137 hydrochloride (Curaxin-137 hydrochloride) is an inhibitor of the histone chaperone FACT, which also activates p53 and inhibits NF-κB with EC50 values of 0.37 and 0.47 μM, respectively. CBL0137 hydrochloride functionally inactivates the complex that promotes chromatin transcription (FACT), thereby driving effects on p53 and NF-κB and promoting cancer cell death, and when used in combination with cisplatin, CBL0137 hydrochloride has potent anticancer activity against SCLC.
- $43
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Amifostine
WR2721, Gammaphos, Ethyol
T328920537-88-6
Amifostine (Ethyol) anhydrous is a cytoprotective agent, acts as a free radical scavenging activity.
- $30
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Pifithrin-α hydrobromide
Cited
Pifithrin-α (PFTα) HBr, Pifithrin-α, Pifithrin hydrobromide, PFTα hydrobromide, PFTα
T270763208-82-2
Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes.
- $33
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CitedNavtemadlin
CS-1300, AMG232
TQ01271352066-68-2
Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.
- $67
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BI-907828, BI907828, BI 907828
T699232095116-40-6
Brigimadlin (BI 907828) is an orally active and highly potent E3 ubiquitin-protein ligase
MDM2-p53 antagonist with antitumor activity.Brigimadlin can be used to study metastatic BTC, PDAC, lung adenocarcinoma, or bladder cancer.
- $162
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Minocycline hydrochloride Cited
Minocycline HCl
T110113614-98-7
Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.
- $38
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CitedAstegolimab
RG 6149, MSTT 1041A
T769102173054-79-8
Astegolimab (RG 6149) is a humanised IgG2 monoclonal antibody that targets the IL-33 receptor and inhibits IL-33 signalling. Astegolimab is used in the study of chronic obstructive pulmonary disease (COPD) and severe asthma in adults.
- $237
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Alrizomadlin
AA-115
T143031818393-16-6
Alrizomadlin is an orally active MDM2 inhibitor. APG-115 shows significant dose-dependent inhibitory effects on TP53wt AML cell lines. The IC50 values are 26.8 nM for MOLM-13 cells and 165.9 nM for MV-4-11 cells. , OCI-AML-3 cells 315.6 nM. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell cycle arrest and apoptosis in a p53-dependent manner.
- $48
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Eprenetapopt
PRIMA-1Met, APR-246
T44145291-32-7
Eprenetapopt (PRIMA-1Met) restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1MET also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.
- $67
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Flubendazole
NSC 313680, Fluvermal, Flumoxane, Flumoxanal
T000931430-15-6
Flubendazole (Flumoxane) is available OTC in Europe that is an anthelmintic using to treat worm infection in humans.
- $33
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Solanidine
T1297180-78-4
Solanidine, a cholestane alkaloid isolated from potato species [Solanum spp.], exhibits antitumor effects by inhibiting cell proliferation.
- $89
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Nutlin-3 Cited
Nutlin3
T2158548472-68-0
Nutlin-3 is an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3 binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3 has antitumor activity.
- $31
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Cited7α-Hydroxycholesterol
T19161566-26-7
7α-Hydroxycholesterol, a cholesterol oxide formed through both enzymatic and non-enzymatic oxidation, can serve as a biomarker for lipid peroxidation.
- $42
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RG7112
RO5045337, RG-7112, RG 7112
T6965939981-39-2
RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
- $41
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Theaflavin-3-gallate Cited
Theaflavine-3-Gallate
T305130462-34-1
Theaflavin-3-gallate (Theaflavine-3-Gallate) can play a role in decreased intestinal cholesterol absorption via inhibition of micelle formation. Theaflavin-3-gallate has anticancer and apoptotic effects in non-small cell lung carcinoma, it acts as prooxidants and induce oxidative stress, with carcinoma cells more sensitive than normal fibroblasts.
- $130
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CitedIdasanutlin Cited
Ro 5503781, RG7388
T62541229705-06-9
Idasanutlin (Ro 5503781) (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
- $34
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CitedGSK3326595
EPZ015938
T57451616392-22-3In house
GSK3326595 (EPZ015938) is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
- $39
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