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Apoptosisp53
Tumor protein p53, also known as p53, cellular tumor antigen p53 (UniProt name), the Guardian of the Genome, phosphoprotein p53, tumor suppressor p53, antigen NY-CO-13, or transformation-related protein 53 (TRP53), is any isoform of a protein encoded by homologous genes in various organisms, such as TP53 (humans) and Trp53 (mice). This homolog (originally thought to be, and often spoken of as, a single protein) is crucial in multicellular organisms, where it prevents cancer formation, and thus functions as a tumor suppressor. As such, p53 has been described as "the guardian of the genome" because of its role in conserving stability by preventing genome mutation.
C16 Ceramide
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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Rotenone
Cited
T297083-79-4
Rotenone (Rotocide) is a natural product and a botanical insecticide. Rotenone is a mitochondrial electron transport complex I inhibitor that promotes the production of reactive oxygen species in mitochondria and induces apoptosis.
- $42
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CitedUSP7-IN-4
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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Isoliquiritin
T5S03315041-81-6
1. Isoliquiritin (Neoisoliquritin) has antitussive effects. 2. Isoliquiritin has antidepressant-like effects. 3. Isoliquiritin, liquiritin and isoliquirigenin inhibits the p53-dependent pathway and shows crosstalk between Akt activities.
- $39
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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.
- $270
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Pifithrin-α hydrobromide Cited
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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CitedRezatapopt
T812892636846-41-6
Rezatapopt (PC14586) is a small molecule p53 reactivator with anti-tumor activity that selectively binds to the cleft present in the TP53 Y220C mutant protein and restores the p53 wild-type (normal) conformation and transcriptional activity, and can be used to study locally advanced or metastatic solid tumors.
- $81
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Verbascoside Cited
T337561276-17-3
Verbascoside (Kusaginin) is a protein kinase C inhibitor with antimicrobial, anti-inflammatory activities.
- $58
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CitedEprenetapopt
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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CBL0137 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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Magnolol Cited
T3000528-43-8
Magnolol (5,5'-Diallyl-2,2'-biphenyldiol) is a dual agonist of RXRα( EC50=10.4 μM) and PPARγ(EC50=17.7 μM). It blocks TNF-α-induced NF-KB activation.
- $39
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CitedCT-1
T270931983924-33-9In house
CT-1 is a DNA minor groove ligand and causes p53-dependent breast cancer cell apoptosis.
- $117
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Pifithrin-μ
T621064984-31-2
Pifithrin-μ (NSC-303580) is an inhibitor of p53 and HSP70, with neuroprotective and antitumor activity.
- $39
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DPBQ
T110927029-89-2In house
DPBQ (ZINC1620467) is a p53 activator. DPBQ could activate p53 and trigger apoptosis in a polyploid-specific manner, without inhibition of topoisomerase or bind DNA.
- $107
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CBL0137
T41261197996-80-7
CBL0137 (Curaxin 137), a metabolically stable curaxin, activates p53 (EC50: 0.37 μM) and inhibits NF-κB (EC50: 0.47 μM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer.
- $44
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UC2288
T96981394011-91-6
UC2288 is a relatively selective p21 attenuator which is synthesized based Sorafenib. UC2288 attenuates p21 protein levels with minimal effect on p21 protein stability.
- $41
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Moringin
TN458373255-40-0
Moringin is an isothiocyanate obtained from myrosinase-mediated hydrolysis of the glucosinolate precursor glucoMoringin present in Moringa oleifera seeds. Moringin has anti-inflammatory and antioxidative properties.
- $138
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Pifithrin-α, p-Nitro, Cyclic Cited
T1247260477-38-5
Pifithrin-α, p-Nitro, Cyclic (PFN-α) is a cell-permeable, active-form inhibitor of p53.
- $34
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CitedNSC348884 Cited
T690981624-55-7
NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.
- $35
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CitedPinoresinol
TN2080487-36-5
Pinoresinol ((+)-Pinoresinol) has antiinflammatory, hepatoprotective, and fungicidal activities, it can protect pial microcirculation from I-reperfusion injury, to increase nitric oxide release and to reduce oxidative stress preserving pial blood flow distribution; it may exert pharmacologically interesting effects via modulation of the insulin-like signalling pathway in C.elegans. Pinoresinol causes an upregulation of the CDK inhibitor p21(WAF1 Cip1) both at mRNA and protein levels, inhibits NF-kappaB and activating protein 1 (AP-1).
- $52
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HBX 41108
T21527924296-39-9
HBX 41108 (HBX-41108) is a non-competitive, reversible inhibitor of USP7 with an IC50 of 424nM. HBX 41108 inhibited deubiquitination of p53 mediated by USP7 in a dose-dependent manner with an IC50 of 0.8μM.
- $47
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Phenoxodiol
T1652281267-65-4
Phenoxodiol (Idronoxil) activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis(XIAP), disrupts FLICE inhibitory protein(FLIP) expression, and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol induces cell cycle arrest in the G1 S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner. Phenoxodiol also inhibits DNA topoisomerase II.
- $60
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δ-Tocotrienol
TMA247425612-59-3
δ-Tocotrienol (Delta-Tocotrienol) is a potential angiogenic inhibitor. δ-Tocotrienol is also a nontoxic activator of mir-34a which can inhibit nonsmall cell lung cancer cells (NSC-LC) cell proliferation, induce apoptosis and inhibit invasion, and thus offering a potential starting point for the design of novel anticancer agents.
- $40
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XI-006
T661058131-57-0
XI-006 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization activation and DNA damage, and also regulates MDM2, an E3 ligase.
- $51
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SCH529074
T37042922150-11-6
SCH529074 is a selective activator of p53 (Ki = 1 μM) and can be used in studies about non-small-cell lung carcinoma. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53.
- $30
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COTI-2
T43251039455-84-9
COTI-2, an orally available thiosemicarbazone, is an activator of mutant forms of the p53 protein with potential antineoplastic activity.
- $38
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Pifithrin-β hydrobromide Cited
T3637511296-88-1
Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).
- $34
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CitedKevetrin hydrochloride Cited
T318466592-89-0
Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
- $38
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CitedBenzonitrile, 3,3'-[(2-oxo-1,3-cyclohexanediylidene)dimethylidyne]bis-
T912963476-70-0
Benzonitrile, 3,3'-[(2-oxo-1,3-cyclohexanediylidene)dimethylidyne]bis- is an inhibitor of p53 with an IC50 value of 0.35 μM
- $44
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1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one
TN5263569-83-5
1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.
- $36
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Sarmustine
T2866381965-43-7In house
Sarmustine (SarCNU) is an alkylating agent with anticancer activity that inhibits the growth of prostate cancer cells via p53-dependent and p53-independent pathways.Sarmustine mediates the selection of P140K methylguanine-DNA-methyltransferase-transduced human CD34(+) cells in vitro.
- $195
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p53-MDM2-IN-1
T72026381717-91-5
p53-MDM2-IN-1 (Example 30), an inhibitor of the p53-MDM2 X protein interaction, exhibits a K i value of 23.35 µM and holds potential for applications in anti-tumor research.
- $117
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BAY 1892005
T777682036352-13-1
BAY 1892005 is a p53 protein modulator that targets the p53 condenser for the study of diseases associated with misfolded p53 protein
- $93
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PhiKan 083
T16523L880813-36-5
PhiKan 083, a carbazole derivative, exhibits potential as an eco-friendly dye with applications in the development of organic photovoltaic cells (OPVs).
- $30
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SLMP53-1
T608391643469-17-3
SLMP53-1 is a p53 activator with anti-tumor activity, inhibits wt and mutp53, activates reprogramming of glucose metabolism in xenografted human tumor tissues, and interferes with angiogenesis and migration. SLMP53-1 inhibits tumor cell growth and can be used to study human rectal cancer.
- $128
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Indole-3-carbinol
T2947700-06-1
Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.
- $29
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Serdemetan Cited
T2243881202-45-5
Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
- $39
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CitedNSC59984
T6910803647-40-7
NSC59984, a p53 pathway activator, induces mutant p53 protein degradation and p73 activation.
- $64
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RO-5963
T167711416663-77-8In house
RO-5963 is a dual inhibitor of p53-MDM2 and p53-MDMX (IC50s: ~17 nM and ~24 nM, respectively).
- $64
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Tenovin-6 Hydrochloride
T84801011301-29-3
Tenovin-6 Hydrochloride is an SIRT1, SIRT2 and HDAC8 inhibitor(IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively), and is also a potent p53 activator .
- $33
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RITA Cited
T1798213261-59-7
RITA (NSC-652287)(NSC-652287) induced cross-links of both DNA-DNA and DNA-protein with no detectable DNA single-strand breaks. RITA, like nutlin-3, can disrupt the p53 Mdm2 interaction.
- $30
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CitedMMRi64
T28078430458-66-5
MMRi64 is a specific inhibitor of Mdm2-MdmX E3 ligase activity.MMRi64 potently induces p53 accumulation and apoptosis in the p53 pathway in leukemia lymphoma cells, disrupts Mdm2-MdmX interactions, and downregulates Mdm2 and MdmX in leukemia cells.MMRi64 MMRi64 can be used in cancer research.
- $51
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ZMC1
T246471555-25-4
NSC-319726 (ZMC1), a mutant p53R175 reactivator, suppresses growth of fibroblasts that expresses the p53R175 mutation (IC50 = 8 nM).
- $32
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Amifostine thiol
T3753831098-42-7
Amifostine thiol (WR-1065) is a radioprotectant that protects DNA from fast neutron-induced strand breaks.Amifostine thiol ameliorates (P<0.001) 6-OHDA-induced stiffness in a dose-dependent manner and activates p53 through a JNK-dependent signaling pathway.
- $30
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Tenovin-1
T1919380315-80-0
Tenovin-1 inhibits protein-deacetylating activities of SirT1 and SirT2 and protects against MDM2-mediated p53 degradation, which involves ubiquitination.
- $50
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p53-Mdm2 inhibitor 4
T67698350678-63-6
p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.
- $30
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MIRA-1
T2298072835-26-8
MIRA-1 (WRN Helicase Inhibitor) is a restorer of wild-type p53 conformation cellular function and selectively inhibits Werner syndrome WRN helicase activity with an IC50 of 20 µM.
- $34
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