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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.
Milademetan
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
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
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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SAR405838
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
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
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
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
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
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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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
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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CitedAlrizomadlin
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
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
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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Nutlin-3 Cited
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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CitedRG7112
T6965939981-39-2
RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
- $41
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Idasanutlin Cited
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
T57451616392-22-3In house
GSK3326595 (EPZ015938) is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
- $39
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Cyclopiazonic acid
T1502718172-33-3
Cyclopiazonic acid (CPA) is a neurotoxic secondary metabolite (SM) made by A. flavus. Cyclopiazonic acid (CPA) is an endoplasmic reticulum calcium ATPase (Ca2+ATPase; SERCA)nanomolar inhibitor and a potent inducer of cell death in plants.
- $54
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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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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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