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ApoptosisMdm2
Mouse double minute 2 homolog (MDM2) also known as E3 ubiquitin-protein ligase Mdm2 is a protein that in humans is encoded by the MDM2 gene. Mdm2 is an important negative regulator of the p53 tumor suppressor. Mdm2 protein functions both as an E3 ubiquitin ligase that recognizes the N-terminal trans-activation domain (TAD) of the p53 tumor suppressor and as an inhibitor of p53 transcriptional activation.
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.
- $178
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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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Triptolide
Cited
T217938748-32-2
Triptolide (PG490) belongs to the tricyclic diterpenoid group of natural products and is an inhibitor of NF-κB activation. Triptolide exhibits immunosuppressive, anti-rheumatic, anti-inflammatory, anti-proliferative and anti-tumor activities.
- $37
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Cited
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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Navtemadlin
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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MD-224
T119802136247-12-4
MD-224 is a highly potent and efficacious MDM2 degrader based on the proteolysistargeting chimera (PROTAC) concept,and as a new class of anticancer agent.
- $64
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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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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.
- $263
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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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RG7112
T6965939981-39-2
RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
- $41
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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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Kevetrin 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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CitedMX69
T36531005264-47-0
MX69 is the MDM2 XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
- $31
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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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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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Serdemetan Cited
T2243881202-45-5
Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
- $39
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CitedRO-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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SJ-172550
T16888431979-47-4
SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).
- $37
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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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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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SP-141
T217731253491-42-7
SP 141 is a MDM2 inhibitor.SP-141 promotes MDM2 auto-ubiquitination and degradation, with anticancer activity.
- $38
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NVP-CGM097
TQ02311313363-54-0
NVP-CGM097 (CGM097) is an effective and specific MDM2 inhibitor (IC50: 1.7 nM for hMDM2).
- $79
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NSC 66811
T215786964-62-1
NSC 66811is a novel inhibitor of the murine double minute 2 (MDM2)-p53 interaction. It binds to MDM2 with a Ki of 120 nM and activates p53 in cancer cells with a mechanism of action consistent with targeting the MDM2-p53 interaction.
- $38
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RO8994
T35171309684-94-3
RO8994 is a highly effective and specific inhibitor of spiroindolinone small-molecule MDM2, with IC50 of 20 nM (MTT proliferation assays) and 5 nM (HTRF binding assays).
- $34
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MB710
T96612230044-57-0In house
MB710 is an amino benzothiazole derivative that binds tightly to the Y220C pocket and stabilizes p53-Y220C in vitro. It exhibits anticancer activity and can be used in cancer research.
- $197
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CP-31398 dihydrochloride
T216481217195-61-3
CP-31398 dihydrochloride is a p53 stabilizer which stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53.
- $42
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Nutlin-3b
T6614675576-97-3
Nutlin-3b ((+)-Nutlin-3) is a p53 MDM2 antagonist or inhibitor (IC50: 13.6 μM), 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.
- $35
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MI-1061
T120311410737-34-6
MI-1061 is a orally bioavailable inhibitor of MDM2 (MDM2-p53 interaction) (IC50=4.4 nM).
- $3,598
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MA242
T119311049704-18-8
MA242 is a nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy and dual inhibitor of murine double minute 2 (MDM2).
- $1,930
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IVHD-valtrate
TN434128325-56-6
VHD-valtrate has anticancer effects against human ovarian cancer cells in vitro and in vivo, it is a potential therapeutic agent for ovarian cancer, providing a basis for development of the compound as a novel chemotherapeutic agent.
- $2,998
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Ganoderic acid X
TN410786377-53-9
Ganoderic acid X is a potential Mdm2 inhibitor(K(i) = 16nM). It is a potential anticancer drug, inhibits topoisomerases and induces apoptosis of cancer cells.
- $290
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MG-277
T12027
MG-277 is a molecular glue compound transformed from PROTAC degradation agent, MG-277 potently inhibits tumor cell growth in a p53-independent manner.
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