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Mutantp53 modulator-1 is a mutantp53 modulator. Mutantp53 modulator-1 reduces the progression of cancers that contain a p53 mutation (extracted from patent WO2021231474A1, compound 231B) .
STIMA-1 can stimulate mutantp53 DNA binding in vitro and induce expression of p53 target proteins and trigger apoptosis in mutantp53-expressing human tumor cells .
RETRA is a mutantp53-dependent activator of p73 that suppresses mutantp53-bearing cancer cells. RETRA increases the expression level of p73, and a release of p73 from the blocking complex with mutantp53, which produces tumor-suppressor effects .
p53 Activator 5 (compound 134A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 5 can bind to mutantp53 and restore the ability of the p53mutant to bind DNA. p53 Activator 5 shows anti-tumor activity . p53 Activator 5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
p53 Activator 10 (Example C-2) is a compound that targets the y220c mutant of p53. p53 Activator 10 activation is involved in the downstream effects of tumor suppression .
Colletofragarone A2 can be be isolated from the fungus Colletotrichum sp. (13S020). Colletofragarone A2 inhibits mutantp53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutantp53 and suppressing tumor growth in vivo .
p53 Activator 12 (compound 510B) is a potent p53 activator. p53 Activator 12 binds to mutantp53 and restores the ability of the p53mutant to bind DNA .
p53 Activator 3 (compound 87A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 3 can bind to mutantp53 and restore the ability of the p53mutant to bind DNA. p53 Activator 3 shows anti-tumor activity . p53 Activator 3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
NSC59984 induces mutantp53 protein degradation via MDM2 and the ubiquitin-proteasome pathway . NSC59984 acts by targeting GOF-mutantp53 and stimulates p73 to restore the p53 pathway signaling .
RETRA (hydrobromide) is a mutantp53-dependent activator of p73 that can inhibit cancer cells carrying mutantp53. RETRA (hydrobromide) increases the expression level of p73, induces transcriptional activation of several common to transcriptional targets p53 and p73, which leads to mutantp53- and p73-dependent inhibition of tumor growth, reduction of colony formation and induction of effector caspases .
BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC50=23 nM), exhibits selective toxicity against p53mutant cancer cells .
p53 Activator 7 is a p53 mutation Y220C (MDM-2/p53) activator with an EC50 of 104 nM. p53 Activator 7 can bind to p53mutant and restore its ability to bind DNA (WO2022213975A1; Example B-1) . p53 Activator 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
COTI-2, an anti-cancer agent with low toxicity, is an orally available third generation activator of p53mutant forms. COTI-2 acts both by reactivating mutantp53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutantp53 to wild-type conformation .
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 .
PK7242 is an inducer of reactivation of mutantp53 in cancer cells. In cancer cells carrying the Y220C mutant, PK7242 binds to the p53-Y220C core domain and induces growth inhibition, cell-cycle arrest, and apoptosis.
ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutantp53 DBD. ADH-6 targets and dissociates mutantp53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases[1].
Antitumor agent-202 is a stabilizer of the p53 Y220C mutant. It exhibits a selective inhibitory effect on the proliferation of tumor cells carrying the p53 Y220C mutation and can be applied to the research of cancers associated with the p53 Y220C mutation .
ADH-6 TFA is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutantp53 DBD. ADH-6 TFA targets and dissociates mutantp53 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 .
MIRA-1 is a maleimide analogue. MIRA-1 can induce apoptosis in mutantp53 cells via restoration of p53-dependent transcriptional transactivation. MIRA-1 has anticancer activity .
TRAP-1 (XJZ-06-462) is a selective p53Y220C transcriptional activator. TRAP-1 can engage p53Y220C and BRD4 in a ternary complex, which potently activates mutantp53 and triggers robust p53 target gene transcription. TRAP-1 rapidly upregulates p21 and other p53 target genes in pancreatic cell lines with p53Y220C. TRAP-1 exhibits higher antiproliferative activity in BxPC-3 (p53Y220C) cells than in A549 cells (p53WT), with IC50 values of 0.531 μM and 3.94 μM, respectively. TRAP-1 can be used for the study of p53Y220C-bearing cancer.
CP-31398 can stabilize the active conformation of p53 and promote p53 activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth .
SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutantp53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC) .
Peptide 234CM is a peptide containing isoleucine at position 3, corresponding to the sequence of a point mutation in p53 codon 234. Peptide 234CM induces potent cytotoxic T cell (CTL) and antitumor immune responses against mutantp53 .
DS-5272 is an orally acitve inhibitor for p53-MDM2 with an IC50 of 20 nM. DS-5272 inhibits the proliferation of SJSA-1 (wildtype p53, IC50=0.17 μM) and DLD-1 (mutantp53). DS-5272 arrest the cell cycle, and induces apoptosis in SJSA-1. DS-5272 exhibits antitumor efficacy in mice .
PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutantp53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .
NSC319726 (ZMC1) is a mutantp53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity .
PRIMA-1 (NSC-281668) is a mutantp53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.
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 mutantp53 cancer cell death by increasing reactive oxygen species (ROS) levels .
MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutantp53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53mutant), with a Kd of 167 μM. PhiKan 083 can be used for cancer research .
Kevetrin 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 .
PK7088 is a pyrazole and a specific peptide. PK7088 supports the reactivation of mutantp53 by converting it to a form exhibiting wild-type properties. PK7088 exhibit anticancer activity in cancer research .
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity .
PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53mutant), with a Kd of 167 μM , and a relative binding affinity (Kd) of 150 μM in Ln229 cells .
Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53mutant peptide aggregation in vitro .
SLMP53-2 is a mutantp53 reactivator. SLMP53-2 restores wild-type-like conformation and DNA-binding ability of mutp53-Y220C by enhancing its interaction with the Hsp70, leading to the reestablishment of p53 transcriptional activity. SLMP53-2 can induce cell cycle arrest, apoptosis and endoplasmic reticulum (ER) stress. SLMP53-2 exhibits antitumor activity .
Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
YX-02-030M is a PROTAC MDM2 degrader. YX-02-030M inhibits MDM2-p53 binding and VHL-HIF1α binding with IC50s of 63 nM and 1.35 μM respectively. YX-02-030M binds MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, and effectively kills p53mutant or deleted Triple-negative breast cancers (TNBC) cells. (Blue: VHL ligand; Black: linker; Pink: MDM2 inhibitor) .
Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53mutant peptide aggregation in vitro .
Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53mutant peptide aggregation in vitro .
MS78 is an acetylation targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein. MS78 recruits histone acetyltransferase p300/CBP to acetylate the p53Y220C mutant. MS78 upregulates TRAIL apoptotic genes and downregulates DNA damage response pathways. MS78 contains a CBP/p300 binder, a p53Y220C binder and a linker .
Acetylcholine (chloride) (Standard) is the analytical standard of Acetylcholine (chloride). This product is intended for research and analytical applications. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53mutant peptide aggregation in vitro .
SLMP53-1 is a wild-type and mutantp53 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 .
Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells .
Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
Peptide 234CM is a peptide containing isoleucine at position 3, corresponding to the sequence of a point mutation in p53 codon 234. Peptide 234CM induces potent cytotoxic T cell (CTL) and antitumor immune responses against mutantp53 .
Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53mutant peptide aggregation in vitro .
Acetylcholine (chloride) (Standard) is the analytical standard of Acetylcholine (chloride). This product is intended for research and analytical applications. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53mutant peptide aggregation in vitro .
Colletofragarone A2 can be be isolated from the fungus Colletotrichum sp. (13S020). Colletofragarone A2 inhibits mutantp53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutantp53 and suppressing tumor growth in vivo .
Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53mutant peptide aggregation in vitro .
Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53mutant peptide aggregation in vitro .
Antigen NY-CO-13; BCC7; Cellular tumor antigen p53; FLJ92943; LFS1; mutant tumor protein 53; p53; p53 tumor suppressor; p53_HUMAN; Phosphoprotein p53; Tp53; Transformation related protein 53; TRp53; tumor antigen p55; Tumor protein 53; Tumor protein p53; Tumor suppressor p53
WB, IHC-P, ICC/IF, IP, ELISA
Human
p53 Antibody (YA5861) is a rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to p53. It can be applicated for WB, IHC-P, ICC/IF, IP, ELISA assays, in the background of human.
BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC50=23 nM), exhibits selective toxicity against p53mutant cancer cells .
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