Cat.No. | Name | Information |
---|---|---|
M3628 | RG7112 | RG7112 (RO5045337) is the first-in-class small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. |
M2185 | Nutlin-3 | Nutlin-3 is a selective MDM2 (mouse double minute 2) antagonist with IC50 of 90 nM. |
M21506 | MD-222 | MD-222 is a first-in-class, highly effective ProTAC-based MDM2 depressant. MD-222 has anti-cancer properties. |
M13439 | Milademetan | Milademetan (DS-3032) is a specific, orally active MDM2 inhibitor for the study of acute myeloid leukemia and solid tumors. |
M13393 | NVP-CGM097 | NVP-CGM097 is a highly effective and selective MDM2 inhibitor with a Ki value of 1.3 nM. |
M11331 | UC2288 | UC2288 is a novel p21 attenuator with cellular permeability and oral activity (relatively selective activity for P21), based on the structural synthesis of sorafenib. UC2288 down-regulated the expression of P21 mRNA and reduced the level of P21 protein independently of p53, and had little effect on the stability of P21 protein. UC2288 did not inhibit VEGFR2 and Raf kinases, even at 10 μM. |
M10781 | Alrizomadlin | Alrizomadlin (APG-115) is an oral active small molecule MDM2 protein inhibitor that binds to MDM2 protein.IC50 value and Ki The values are 3.8 nM and 1 nM, respectively. Alrizomadlin blocks MDM2 interaction with p53 and induces cell cycle arrest and apoptosis in a p53-dependent manner. |
M10374 | AMG 232 | AMG 232 is an extremely potent MDM2 inhibitor (SPR KD = 0.045 nM, SJSA-1 EdU IC50 = 9.1 nM), with remarkable pharmacokinetic properties and in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft model (ED50 = 9.1 mg/kg). *The compound is unstable in solutions, freshly prepared is recommended |
M9184 | RO8994 | RO8994 is a potent and selective spiroindolinone MDM2 inhibitor, with IC50 of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). |
M8895 | MX69 | MX69 is a dual inhibitor of MDM2 and XIAP that binds to MDM2 RING protein with binding Kd values of 2.34 μM. |
M7535 | HDM201 | HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4. |
M6301 | SAR405838 | MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. |
M5700 | Idasanutlin (RG-7388) | Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity. |
M5225 | MI-773 | MI-773 is an orally available MDM2 antagonist with Ki of 0.88 nM. |
M4265 | Peimisine | Peimisine (Ebeiensine) noncompetitively antagonizes M receptors in tracheal smooth muscle and thus inhibits Ach induced smooth muscle contraction. Peimisine also stimulates beta receptors and antagonizes the release of calcium, promoting the release of NO and thus relaxing the smooth muscles of the trachea to achieve antiasthmatic effects. |
M3224 | NSC 207895 | NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase. |
M3014 | SL-01 | SL-01 is a p53-Mdm2 interaction inhibitor with IC50 of 3.18 μM. |
M2895 | Nutlin-3b | Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite enantiomer Nutlin-3a. |
M2894 | Nutlin-3a | Nutlin-3a, the active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits the p53/MDM2 interaction with IC50 of 90 nM. |
M2207 | NSC 66811 | NSC 66811 is a potent MDM2 inhibitor with Ki value of 120 nM, which disrupts MDM2-p53 interaction and activates p53 function. |
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