标签归档：mdm

373227-10MG   MDM2 E3 Ligase Inhibitor III, MEL23   品牌 Merck

发表于由

MDM2 E3 Ligase Inhibitor III, MEL23

货号： 373227-10MG      产品名称： MDM2 E3 Ligase Inhibitor III, MEL23   品牌： Merck 规格： *** 3周到货 生化实验

MDM2 Inhibitor VII, MEL23
A cell-permeable tetrahydro-β-carbolinylbarbiturate compound that selectively inhibits the E3 ligase activity of Mdm2-MdmX hetero-complex over that of Mdm2-Mdm2 homo-complex (70.6% vs. 17.6% inhibition, respectively, at 100 µM), without affecting Mdm2-MdmX complex formation or the activity of two other UbcH5C-utilizing ligase complexes Roc1-Cul1 and BRCA1-BARD1. Effectively inhibits ubiquitination and proteasomal degradation of cellular Mdm2 and p53 (effective conc. = 14 µM in U2OS, RKO, and HCT116 cultures) and induce RKO and MEF cell death in a p53- and Mdm2-dependent manner. Unlike Nutlin-3 (Cat. Nos. 444143 & 444151), MEL23 does not interfere with Mdm2-p53 interaction.
产品信息
Form  Yellow solid
Molar mass  354.4
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥95% by HPLC
Solubility  DMSO
Chemical formula  C19H22N4O3
商店和运输信息
Storage  +2°C to +8°C
Ship  Ambient Temperature Only
Standard Handling

2°C – 8°C

444152-5MG   MDM2 Antagonist IV, Nutlin-3a   品牌 Merck

发表于由

MDM2 Antagonist IV, Nutlin-3a

货号： 444152-5MG      产品名称： MDM2 Antagonist IV, Nutlin-3a   品牌： Merck 规格： *** 3周到货 生化实验

MDM2 Antagonist IV, Nutlin-3a
(-)-4-(4,5-bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl)piperazine-2-one
A cell-permeable and highly potent active enantiomer of Nutlin-3 (Cat. No. 444143) that binds to the p53-binding pocket and blocks the interaction of p53 and MDM2 (IC50 = 90 nM). Exhibits over 150-fold greater affinity for MDM2 than its less active enantiomer, Nutlin-3b. Induces p53 mediated apoptosis by both transcription-dependent and independent mechanisms. Shown to greatly potentiate the cytotoxic effects of chemotherapeutic agents and reduce tumor burden in vivo. Also shown to overcome ATM-mediated resistance to fludarabine in chronic lymphocyte leukemia. Cells treated with Nutlin-3a permanently lose their ability to proliferate and enter into a pattern of permanent senescence. Mouse embryonic fibroblasts with p53+/+MEFs show significantly reduced reprogramming capabilities following Nutlin-3a treatment.
产品信息
Form  White powder
Molar mass  581.5
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥98% by HPLC
Solubility  DMSO
Chemical formula  C30H30Cl2N4O
CAS number  675576-98-4
商店和运输信息
Storage  -20°C
Ship  Shipped with Blue Ice or with Dry Ice
Standard Handling

-20°C