MDM-2/p53 Inhibitor

MDM-2/p53 Inhibitors (98):

Cat. No.	Product Name	Effect	Purity

HY-112780

UC2288	Inhibitor	99.82%
UC2288 is a potent and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 potently inhibits cancer cell growth by inducing apoptosis. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM.

HY-P99444

Astegolimab	Inhibitor	99.00%
Astegolimab (MSTT 1041A; RG 6149) is a human IgG2 monoclonal antibody. Astegolimab blocks IL-33 signaling by targeting the IL-33 receptor ST2. Astegolimab reduces p53 expression, mitigates IL33-upregulated SASP factors such as IL1α, IL6 and MCP1. Astegolimab mitigates IL33-increased p-p65/p65 ratio. Astegolimab blocks CM-induced neutrophil extracellular trap (NET) formation. Astegolimab is used in chronic obstructive pulmonary disease (COPD) and myocardial research.

HY-152860

Darizmetinib	Inhibitor	99.94%
Darizmetinib (HRX-0215) is an orally active, potent and selective inhibitor of mitogen-activated protein kinase kinase 4 (MKK4). Darizmetinib leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration. Darizmetinib is promising for research of preventing liver failure after extensive oncological liver resections or transplantation of small liver grafts.

HY-P4210

Sulanemadlin	Inhibitor	99.49%
Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research.

HY-P4157

FOXO4-DRI	Inhibitor	99.96%
FOXO4-DRI is a cell-permeable peptide antagonist that blocks the interaction of FOXO4 and p53. FOXO4-DRI is a senolytic peptide that induces apoptosis of senescent cells.

HY-124284

Hexamethylene bisacetamide	Inhibitor	99.56%
Hexamethylene bisacetamide (HMBA) is a differentiation inducer and selective bromine domain inhibitor that can differentiate across the blood-brain barrier. Hexamethylene bisacetamide can induce tumor cell differentiation and inhibit cell proliferation, showing antitumor activity. Hexamethylene bisacetamide induces apoptosis by Notch1, Bcl-2 and p53 signaling pathways. In addition, Hexamethylene bisacetamide improves the obesity phenotype of mice.

HY-W592871

10-Hydroxy-2-decenoic acid	Inhibitor	99.93%
10-Hydroxy-2-decenoic acid (10-HDA) is an orally active unsaturated medium-chain fatty acid with various physiological activities. 10-Hydroxy-2-decenoic acid induces ROS-mediated apoptosis in A549 cells. 10-Hydroxy-2-decenoic acid inhibits VEGF-induced angiogenesis in human venous endothelial cells. 10-Hydroxy-2-decenoic acid alleviates non-alcoholic fatty liver disease (NAFLD) by activating the AMPK-α signaling pathway. 10-Hydroxy-2-decenoic acid protects against bone loss by inhibiting NF-κB signaling downstream of FFAR4. 10-Hydroxy-2-decenoic acid is an antibiotic against many bacteria and fungi, such as Neurospora sitophila, molds and Staphylococcus aureus. 10-Hydroxy-2-decenoic acid has longevity-promoting effects in C. elegans. 10-Hydroxy-2-decenoic acid prevents osteoarthritis by targeting aspartyl β hydroxylase and inhibiting chondrocyte senescence.

HY-P5831

Biotin-H10	Inhibitor	98.94%
Biotin-H10 is a specific anterior gradient homolog 2 (AGR2) inhibitor with a K_D of 6.4 nM. Biotin-H10 inhibits cancer cells viability.

HY-148409

MMRi62	Inhibitor	99.59%
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 mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12.

HY-B0774

Seratrodast	Inhibitor	99.59%
Seratrodast (AA 2414), an orally active antiasthmatic agent, is a thromboxane A2 receptor (TP) antagonist and ferroptosis inhibitor. Seratrodast reduces lipid ROS production, modulates the systemic xc-/GSH/GPX4 axis, and inhibits JNK phosphorylation and p53 expression. Seratrodast exhibits anti-asthmatic and anti-epileptic activity.

HY-112440

HZX-02-059	Inhibitor	99.40%
HZX-02-059 is a potent methuosis inducer and dual-target PIKfyve/tubulin inhibitor with anticancer activity. Methuosis mainly disrupts the balance of endocytosis and exocytosis, forming a large number of vesicles and inducing cell death. HZX-02-059 also induces cell vacuolization, promotes apoptosis, downregulates the p53 pathway, inhibits PI3K/AKT phosphorylation, and inhibits c-Myc and NF-κB transcription.

HY-N0392

Polygalasaponin F	Inhibitor	99.85%
Polygalasaponin F is an orally active triterpenoid saponin monomer. Polygalasaponin F downregulates the expression of Bax, p53, caspase-3, NF-κB p65 and MEK1; restores and upregulates the expression of Bcl-2; activates the PI3K/Akt signaling pathway; inhibits the phosphorylation of p38 MAPK, nuclear translocation of NF-κB, TLR4-mediated signaling pathway, mitophagy (Mitophagy) and ROS production; enhances cell viability and suppresses apoptosis (Apoptosis). Polygalasaponin F maintains mitochondrial function, alleviates Ca²⁺ overload, upregulates pCREB and BDNF, preserves cell viability and inhibits the release of inflammatory cytokines. Polygalasaponin F alleviates lung injury induced by influenza A H1N1 and cerebral ischemia-reperfusion injury. Polygalasaponin F is applicable to researches related to Parkinson's disease, cerebral ischemia, pneumonia induced by influenza A H1N1, stroke and Alzheimer's disease.

HY-106263B

Tyroserleutide hydrochloride	Inhibitor	99.92%
Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis.

HY-17493

MI-773	Inhibitor
MI-773 is an orally active, selective MDM2-p53 interaction inhibitor with a K_i of 0.88 nM for MDM2. MI-773 blocks the MDM2-TP53 interaction. MI-773 potently activates p53. MI-773 induces Apoptosis. MI-773 causes tumor regression in xenograft models of adenoid cystic carcinoma. MI-773 exhibits anticancer effects in neuroblastoma. MI-773 TFA can be used for the research of adenoid cystic carcinoma.

HY-N2445

Flavokawain C	Inhibitor	99.79%
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway. Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer.

HY-P2096

Hexapeptide-11	Inhibitor	99.77%
Hexapeptide-11 is an anti-aging peptide that can protect fibroblasts from premature cell senescence mediated by oxidative stress. Hexapeptide-11 is also a potential stimulator of hyaluronic acid in keratinocytes, and can enhance skin barrier function by upregulating the expression of HAS2 and EGR3, and downregulating the expression of HYAL2. Hexapeptide-11 can also improve skin elasticity.

HY-156906

UNC3474	Inhibitor	98.56%
UNC3474 is a small molecule ligand, binding with 53BP1. UNC3474 binds the aromatic methyl-lysine binding cage of 53BP1^TT, with a dissociation constant (K_d) of 1.0 ± 0.3 μM. UNC3474 inhibits the recruitment of 53BP1 to DSBs by stabilizing a pre-existing autoinhibited state of 53BP1 in cells.

HY-107566

Conessine	Inhibitor	99.87%
Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pK_i values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy.

HY-148833

MDM2-p53-IN-16	Inhibitor	99.08%
MDM2-p53-IN-16 is a MDM2-p53 complex inhibitor with an IC₅₀ value of 4.3 nM to dissociate human p53/MDM2 complex. MDM2-p53-IN-16 reactivates p53, and induces Glioblastoma Multiforme (GBM) cell apoptosis and cell-cycle arrest. MDM2-p53-IN-16 can be used for the cancer research.

HY-W340313

p53-MDM2-IN-4	Inhibitor	99.79%
p53-MDM2-IN-4 (Example 4) is an inhibitor of p53-MDM2/X protein interaction, with a K_i value of 3.079 μM. p53-MDM2-IN-4 can be used in anti-tumor research.

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