p53
The p53 tumor suppressor is a 53 kDa nuclear phosphoprotein of 393 amino acids that is encoded by the TP53 gene (20 kb with 11 exons and 10 introns) and characterized by the presence of several structural and functional domains, including a N-terminus, a central core domain, a C-terminal region, a strongly basic carboxyl-terminal regulatory domain, a nuclear localization signal sequence and three nuclear export signal sequence. The p53 is considered as a major “guardian of genome” for its activities in a wide range of cellular events, including cell-cycle regulation, induction of apoptosis, gene amplification, DNA recombination, chromosomal segregation and cellular senescence.
Products for p53
- Cat.No. Product Name Information
- GC42586 6α-hydroxy Paclitaxel 6α-hydroxy Paclitaxel is a primary metabolite of the anticancer compound paclitaxel, produced by the action of the cytochrome P450 isoform CYP2C8.
- GC41643 9(Z),11(E),13(E)-Octadecatrienoic Acid 9(Z),11(E),13(E)-Octadecatrienoic Acid (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil.
- GC40785 9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester 9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil.
- GC40710 9(Z),11(E),13(E)-Octadecatrienoic Acid methyl ester 9Z,11E,13E-octadecatrienoic acid (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil.
- GC65880 ADH-6 TFA ADH-6 TFA is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 TFA targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 TFA has the potential for the research of cancer diseases.
- GC33356 AM-8735 AM-8735 is a potent and selective MDM2 inhibitor with an IC50 of 25 nM.
- GC15828 AMG232 AMG232 (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. AMG232 binds to MDM2 with a Kd of 0.045 nM.
- GC42785 Amifostine (hydrate) Amifostine (hydrate) (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine (hydrate) selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine (hydrate) is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine (hydrate) protects cells from damage by scavenging oxygen-derived free radicals. Amifostine (hydrate) reduces renal toxicity and has antiangiogenic action.
- GC61804 Amifostine thiol Amifostine thiol (WR-1065) is an active metabolite of the cytoprotector Amifostine. Amifostine thiol is a cytoprotective agent with radioprotective abilities. Amifostine thiol activates p53 through a JNK-dependent signaling pathway.
- GC35367 APG-115 APG-115 (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively. APG-115 blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.
- GC18136 BH3I-1 Bcl-2 or Bcl-XL inhibitor
- GC35511 BI-0252 BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.
- GC43189 CAY10681 Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer.
- GC43190 CAY10682 (±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo.
- GC14634 CBL0137 curaxin that activates p53 and inhibits NF-κB
-
GC15394
CBL0137 (hydrochloride)
curaxin that activates p53 and inhibits NF-κB
- GC43239 Chk2 Inhibitor Chk2 Inhibitor (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2 Inhibitor can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect.
- GC64649 Cjoc42 Cjoc42 is a compound capable of binding to gankyrin. Cjoc42 inhibits gankyrin activity in a dose-dependent manner. Cjoc42 prevents the decrease in p53 protein levels normally associated with high amounts of gankyrin. Cjoc42 restores p53-dependent transcription and sensitivity to DNA damage.
- GC43297 Coenzyme Q2 Coenzyme Q10 is a component of the electron transport chain and participates in aerobic cellular respiration, generating energy in the form of ATP.
- GC15225 COTI-2 activates mutant forms of p53
- GC15840 CP 31398 dihydrochloride A p53 stabilizing agent
- GC32911 CTX1 CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system.
- GC43408 Deoxycholic Acid (sodium salt hydrate) Deoxycholic acid (cholanoic acid) sodium hydrate,a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5.
- GC47187 Deoxycholic Acid-d4 A quantitative analytical standard guaranteed to meet MaxSpec® identity, purity, stability, and concentration specifications
- GC33384 DPBQ DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells.
- GC15258 GN25 p53-Snail binding Inhibitor
- GC61608 HLI373 dihydrochloride HLI373 dihydrochloride is an efficacious Hdm2 inhibitor.
- GC14755 Inauhzin SIRT1 inhibitor
- GC12117 JNJ-26854165 (Serdemetan) An antagonist of MDM2 action
- GC32919 Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells.
- GC62629 MB710 MB710, an aminobenzothiazole derivative, is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds tightly to the Y220C pocket and stabilizes p53-Y220C, with a Kd of 4.1?μM. MB710 shows anticancer activity in p53-Y220C cell lines.
- GC62716 MD-222 MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects.
- GC38812 MD-224 MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
- GC62557 MDM2-IN-1 MDM2-IN-1 (Compound 30) is a synthetic MDM2-p53 interaction (MDM2) inhibitor and contains the trans (D-)configuration.
- GC36605 MI-1061 MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
- GC62598 MI-1061 TFA MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
- GC16296 MI-773 MDM2 inhibitor
- GC11547 MI-773 (SAR405838) MI-773 (SAR405838) (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. MI-773 (SAR405838) binds to MDM2 with a Ki of 0.88 nM. MI-773 (SAR405838) induces apoptosis and has potent antitumor activity.
- GC32881 Milademetan (DS-3032) Milademetan (DS-3032) (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.
- GC62621 Milademetan tosylate hydrate Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.
- GC12893 MIRA-1 A mutant p53 reactivator
- GC62322 MS7972 MS7972 is a small molecule that blocks human p53 and CREB binding protein association. MS7972 can almost completely block this BRD interaction at 50 μM.
- GC68371 Mutant p53 modulator-1
- GC19257 MX69 MX69 is an inhibitor of MDM2/XIAP, used for cancer treatment.
- GC15621 NSC 146109 hydrochloride An activator of p53
- GC15404 NSC 319726 A p53 reactivator
- GC16151 NSC348884 nucleophosmin inhibitor
-
GC16179
NSC59984
Restores the p53 signaling pathway
- GC16051 Nutlin-3 A racemic mixture of (?)-nutlin-3 and (+)-nutlin-3
- GC10470 Nutlin-3a chiral An inhibitor of the p53-Mdm2 interaction
- GC12508 Nutlin-3b MDM2/p53 inhibitor
- GC12647 NVP-CGM097 potent and selective MDM2 inhibitor
- GC36785 NVP-CGM097 sulfate NVP-CGM097 sulfate is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
- GC19268 NVP-HDM201 NVP-HDM201 (NVP-HDM201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
- GC48652 Olomoucine II A CDK inhibitor
- GC11711 ONC201 ONC201 (ONC-201) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. ONC201 can cross the blood-brain barrier.
- GC15613 p-nitro-Cyclic Pifithrin-α p-nitro-Cyclic Pifithrin-α (PFN-α) is cell-permeable and active-form p53 inhibitor.
- GC15812 p-nitro-Pifithrin-α p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor.
- GC67765 p53 Activator 5
-
GC69648
p53 Activator 7
p53 Activator 7 is a p53 mutant Y220C (MDM-2/p53) activator with an EC50 of 104 nM. It can bind to p53 mutants and restore their ability to bind DNA (WO2022213975A1; Example B-1).
- GC36835 p53 and MDM2 proteins-interaction-inhibitor chiral p53 and MDM2 proteins-interaction-inhibitor chiral (Compound 32) is an inhibitor of the interaction between p53 and MDM2 proteins.
- GC36836 p53 and MDM2 proteins-interaction-inhibitor dihydrochloride p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is an inhibitor of the interaction between p53 and MDM2 proteins.
- GC36837 p53 and MDM2 proteins-interaction-inhibitor racemic p53 and MDM2 proteins-interaction-inhibitor racemic (Compound 2j) is an inhibitor of the interaction between p53 and MDM2 proteins.
-
GP10036
p53 tumor suppressor fragment
Regulates cell cycle
- GC65961 P53R3 P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53R175H, p53R248W and p53R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research.
- GC45758 Paclitaxel octadecanedioate A prodrug form of paclitaxel
- GC47853 Paclitaxel-d5 An internal standard for the quantification of paclitaxel
- GC12658 PhiKan 083
- GC36896 PhiKan 083 hydrochloride PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM, and a relative binding affinity (Kd) of 150 μM in Ln229 cells.
- GC10538 Pifithrin-α (PFTα) Pifithrin-α(PFT-α) is a p53 inhibitor. Pifithrin-αwidely used in neuroscience to block neuronal apoptotic cell death. Pifithrin-αis also a potent stimulant of aryl hydrocarbon receptor (AhR)..
- GC17262 Pifithrin-β potent p53 inhibitor
- GC10282 Piperlongumine An alkaloid with anticancer and antioxidant activities
- GC32946 PK11007 PK11007 is a mild thiol alkylator with anticancer activity. PK11007 stabilizes p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. PK11007 induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels.
- GC44652 PK7242 (maleate) The protein p53, often called the 'guardian of the genome,' is a transcription factor that is activated in response to cellular stress (low oxygen levels, heat shock, DNA damage, etc.) and acts to prevent further proliferation of the stressed cell by promoting cell cycle arrest or apoptosis.
- GC64768 PK9327 PK9327 is a small-molecule stabilizer targeting cavity-creating p53 cancer mutations.
- GC10315 Plumbagin A natural naphthoquinone
- GC12086 PRIMA-1 A re-activator of the apoptotic function of mutant p53 proteins
- GC37010 PROTAC MDM2 Degrader-1 PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC37011 PROTAC MDM2 Degrader-2 PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC37012 PROTAC MDM2 Degrader-3 PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC37013 PROTAC MDM2 Degrader-4 PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC15946 ReACp53 inhibit p53 amyloid formation
- GC13019 RG7112 An inhibitor of the MDM2-p53 interaction
- GC11594 RG7388 An inhibitor of the MDM2-p53 interaction
- GC12793 RITA (NSC 652287) An inhibitor of the p53-HDM-2 interaction
- GC37549 RO-5963 RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively.
- GC19312 RO8994 RO8994 is a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitor, with IC50 of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays).
- GC18624 Roslin-2 Roslin-2 (Benzylhexamethylenetetramine bromide) is a p53 reactivator with anticancer effects. Roslin-2 binds FAK, disrupts the binding of FAK and p53.
- GC13590 SJ 172550 A small molecule inhibitor of MDMX
- GC65284 SLMP53-1 SLMP53-1 is a wild-type and mutant p53 reactivator with promising antitumor activity. SLMP53-1 mediates the reprograming of glucose metabolism in cancer cells. SLMP53-1 depletes angiogenesis, decreasing endothelial cell tube formation and vascular endothelial growth factor (VEGF) expression levels.
- GC16371 Solasodine An alkaloid with diverse biological activities
-
GC69968
Sulanemadlin
Sulanemadlin (ALRN-6924) is a potent p53-based peptide macrocycle. Sulanemadlin is an inhibitor of protein-protein interactions between p53-MDM2, p53-MDMX, or p53 and MDM2 and MDMX. Sulanemadlin can be used for cancer research.
- GC14165 Tenovin-1 A small molecule activator of p53
- GC12337 Tenovin-3 p53 activator
- GC16436 Tenovin-6 SIRT inhibitor and p53 activator
- GC37761 Tenovin-6 Hydrochloride Tenovin-6 Hydrochloride, an analog of Tenovin-1, is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH).
- GC61352 Triglycidyl isocyanurate Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities.
-
GP10028
tumor protein p53 binding protein fragment [Homo sapiens]/[Mus musculus]
P53 binding protein fragment
- GC11557 WR 1065 A radioprotective agent
- GC19545 WR-1065 dihydrochloride WR-1065 dihydrochloride can protect normal tissues from the toxic effects of certain cancer drugs and activate p53 through a JNK-dependent signaling pathway.