MDM-2/p53 Inhibitor

p53-MDM2-IN-7 (compound 6d) (hydrochloride) is a p53-MDM2 inhibitor. p53-MDM2-IN-7 has an IC₅₀ value of 8.13 μM against A549 cells. p53-MDM2-IN-7 can be used in anti-cancer research.

Polygalasaponin F (Standard) is the analytical standard of Polygalasaponin F. This product is intended for research and analytical applications. 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.

p53-HDM2-IN-1 is a potent inhibitor of p53-HDM2 protein-protein interaction, with an IC₅₀ of 0.103 μM. p53-HDM2-IN-1 can be used for the research of cancer.

MI-888 is an orally active MDM2 inhibitor with a K_i of 0.44 nM. MI-888 can inhibit the MDM2-p53 interaction. MI-888 has favorable pharmacokinetic properties and anti-tumor activity.

TH-407a is an orally active and selective USP15 inhibitor with an IC₅₀ of 0.76 μM. As an allosteric modulator, TH-407a binds to a non-catalytic site to block deubiquitinating activity. TH-407a inhibits cell growth, proliferation, clonogenicity and migration, regulates the p53 signaling pathway, and reduces the stability of PARP1. TH-407a exhibits anti-tumor activity in breast cancer xenograft mouse models. TH-407a can be used for the research of breast cancer.

PROTAC LZK degrader 1 is an LZK (MAP3K13) PROTAC degrader. PROTAC LZK degrader 1 binds LZK with a K_d of 35 nM and recruits VHL E3 ubiquitin ligase to induce ubiquitin-proteasome dependent degradation of LZK in MAP3K13-amplified HNSCC cells. PROTAC LZK degrader 1 eliminates both kinase-dependent c-MYC stabilization and kinase-independent GOF p53 accumulation downstream of LZK, suppresses colony formation of LZK-amplified head and neck squamous cell carcinoma (HNSCC) cells. PROTAC LZK degrader 1 can be used for research on LZK-driven HNSCC.

XRF-1021 is an orally active HIPK2 inhibitor (IC₅₀ = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease.

SP-141 (hydrochloride) is a specific inhibitor of MDM2. SP-141 (hydrochloride) promotes MDM2 auto-ubiquitination and degradation. SP-141 (hydrochloride) might be used for the research of pancreatic cancer and breast cancer cells.

YL93 is a dual inhibitors of MDM2/4 with K_i values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. YL93 induces cell-cycle arrest and apoptosis. YL93 shows p53-dependent cell growth inhibition.

CK2-TN03 is an ATP-competitive casein kinase 2 (CK2) inhibitor, with an IC₅₀ of 165 nM and a K_i of 20 nM. CK2-TN03 inhibits CK2-mediated survivin activation and reduces CK2-dependent phosphorylation levels of BRD4/MYCN and AKT1. CK2-TN03 exerts anti-neuroblastoma effects by inhibiting survivin, leading to mitotic catastrophe and apoptosis of cancer cells. CK2-TN03 can be used in studies related to neuroblastoma.

MDM2/XIAP-IN-2 is a dual inhibitor of murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP). MDM2/XIAP-IN-2 degrades MDM2, and inhibits XIAP mRNA translation to inhibits cancer cells. Particularly, MDM2/XIAP-IN-2 inhibits acute lymphoblastic leukemia cell line EU-1 with an IC₅₀ value of 0.3 μM.

MDM2-p53-IN-19 (Compound A-8d) is a chemical intermediate that can be used to synthesize inhibitors of the MDM2-p53 interaction with anticancer activity.

p53-hDM2 cyclic peptide inhibitor 16e is a p53-hDM2 cell-permeable peptide inhibitor with an IC₅₀ of 9.24 nM for hDM2. p53-hDM2 cyclic peptide inhibitor 16e can be used for cancers like breast, colorectal and cervical cancers research.

MDM2/XIAP-IN-1 (compound 14) is an orally active inhibitor of dual MDM2/XIAP. MDM2/XIAP-IN-1 has anti-cancer activity with an IC₅₀ value of 0.3 μM, which can be used in cance rescrch.

YL-1-9 is an inhibitor of the degradation of p53 by MDM2 through strong binding to the key hydrophobic pockets of MDM2. YL-1-9 induces cell cycle arrest and apoptosis in breast cancer cells.

MMRi6 is a Mdm2-MdmX RING domain inhibitor that can disrupt Mdm2-MdmX RING-RING interaction in vitro. MMRi6 inhibits MdmX-stimulated Mdm2 autoubiquitination and Mdm2-MdmX-mediated p53 polyubiquitination in vitro without affecting NEDD4-1 autoubiquitination. MMRi6 induces p53 stabilization and accumulation and induces PARP cleavage in wt-p53 Emu-myc lymphoma cells. MMRi6 inhibits the growth of wt-p53 and p53-null Emu-myc lymphoma cells with IC₅₀s of approximately 0.5 μM and 3 μM, respectively. MMRi6 can be used for the study of leukemia/lymphoma.

HIPK2-IN-2 is an orally active and selective HIPK2 inhibitor with an IC₅₀ of 0.36 μM against HIPK2. HIPK2-IN-2 reduces HIPK2 protein expression levels. HIPK2-IN-2 inhibits the proliferation and migration of renal interstitial fibroblasts, alleviates renal tubular injury and collagen deposition, and suppresses TGF-β/Smad3-mediated profibrotic signaling pathways as well as TNF-α/NF-κB-mediated inflammatory signaling pathways in renal cells. HIPK2-IN-2 is used for the study of chronic kidney disease-associated renal fibrosis.

NMC-001 is a human IgG1 monoclonal antibody (mAb) targeting MDM2. NMC-001 can be used in pancreatic cancer research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).

Caylin-1 is an inhibitor of MDM2 and an analog of Nutlin-3. Caylin-1 can bind to Bcl-XL and is used in multi-target anticancer research.

NU-8231 (Compound 2) is a p53-MDM2 binding inhibitor with an IC₅₀ of 5.3-200 μM for inhibiting the p53-MDM2 interaction. NU-8231 is applicable for cancer research.