MDM-2/p53 MDM2 Inhibitor

AM-7209 is a potent and selective MDM2-p53 interaction inhibitor with a K_d of 38 pM. AM-7209 inhibits the MDM2 amplified SJSA-1 osteosarcoma cell line with an IC₅₀ of 1.6 nM. AM-7209 shows antitumor activities.

MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.

Navtemadlin-d₇ is the deuterium labeled Navtemadlin. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC₅₀ of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM.

RDR03871 (compound 2) is a potent dual MDM2/MDM4 inhibitor with IC₅₀ values of 35.4 nM and 10.4 nM for MDM2-p53 and MDM4-p53, respectively.

HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.

PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology.

MDM2/4-p53-IN-1 is a potent MDM2-p53 and MDM4-p53 inhibitor with IC₅₀ values of 35.9, 57.4 nM, respectively. MDM2/4-p53-IN-1 shows antiproliferative activity.

USP7-IN-2 (compound 4) is a non-competitive USP7 inhibitor with an IC₅₀ of 6 nM. USP7-IN-2 causes degradation of MDM2, stabilization of p53 and induction of p21 in multiple cell lines, and can be utilized in cancer research.

D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC₅₀=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models.

RG7112D is a potent MDM2 inhibitor with IC₅₀s of 11 nM and >10000 nM and for MDM2-p53 and VHL-HIF1α by binding HTRF assay, respectively. RG7112D is coupled by an amide bond to VHL-Amine, resulting in a bi-functional molecule, YX-02-030. YX-02-03, a MDM2-PROTAC, potently inhibits MDM2-p53 binding (HTRF IC₅₀=63nM). RG7112D can stabilize MDM2 protein and increase p53 protein levels.

AM-6761 is a potent MDM2 inhibitor with an IC₅₀ of 0.1 nM.

AM-8735 is a potent and selective MDM2 inhibitor with an IC₅₀ of 25 nM.

MI-219 is an antagonist for MDM2 with a K_i of 13.3 μM. MI-219 inhibits the MDM2-p53 interaction, inhibits thus the proliferation of FSCCL cells, with an IC₅₀ of 2.5 μM.

MI-1063 is an inhibitor for MDM-2, that blocks the MDM2-p53 interaction, and activates the tumor suppressor function of p53. MI-1063 inhibits the growth of cancer cell RS4-11 and MV4-11 with IC₅₀ of 179 nM and 93 nM. MI-1063 can be used as target protein ligand in synthesis of PROTAC degrader MD-265 (HY-169327).

Milademetan (tosylate hydrate) (Standard) is the analytical standard of Milademetan (tosylate hydrate) (HY-101266B). This product is intended for research and analytical applications. Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.

Milademetan (Standard) is the analytical standard of Milademetan (HY-101266). This product is intended for research and analytical applications. Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.

SP-141 (Standard) is the analytical standard of SP-141 (HY-110182). This product is intended for research and analytical applications. SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells.

Alrizomadlin (Standard) is the analytical standard of Alrizomadlin (HY-101518). This product is intended for research and analytical applications. Alrizomadlin (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.

RG7112 (Standard) is the analytical standard of RG7112 (HY-10959). This product is intended for research and analytical applications. RG7112 is a potent, selective, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC₅₀ of 18 nM and a K_d of 11 nM for binding to MDM2.

Nutlin-3 (Standard) is the analytical standard of Nutlin-3. This product is intended for research and analytical applications. Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.