1. PROTAC
    Apoptosis
    Metabolic Enzyme/Protease
  2. PROTAC
    MDM-2/p53
    E1/E2/E3 Enzyme
  3. MD-224

MD-224 

目录号: HY-114312 纯度: 96.15%
产品使用指南

MD-224 是基于蛋白水解定位嵌合体 (PROTAC) 的高效小分子 (MDM2) 降解物。MD-224 在人白血病细胞中,诱导 MDM2 的快速降解 (<1 nM),抑制 RS4;11 细胞生长的 IC50 值为 1.5 nM。MD-224 有可能成为一类新的抗癌剂。

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MD-224 Chemical Structure

MD-224 Chemical Structure

CAS No. : 2136247-12-4

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Description

MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent[1].

IC50 & Target[1]

MDM2

1 nM (IC50)

In Vitro

MD-224 (1-30 nM; 2 hours) effectively induces depletion of MDM2 protein and concurrently accumulation of p53 protein in a dose-dependent manner in RS4;11 cells[1].
MD-224 (30 nM; 6 hours) is more potent than MI-1061 in induction of transcriptional upregulation of these p53 target genes but have no effect on TP53 itself in RS4;11 cells[1].
MD-224 (0.001-1 μM; 24 hours) induces robust apoptosis at ≤10 nM in a dose-dependent manner upon a 24 hours treatment[1].

Western Blot Analysis[1]

Cell Line: RS4;11 cells
Concentration: 1 nM; 3 nM; 10 nM; 30 nM
Incubation Time: 2 hours
Result: Decreased MDM2 protein and accumulated of p53 protein.

RT-PCR[1]

Cell Line: RS4;11 cells
Concentration: 30 nM
Incubation Time: 6 hours
Result: Upregulated p53 target gene expression.

Apoptosis Analysis[1]

Cell Line: RS4;11 cells
Concentration: 0.001 μM, 0.003 μM, 0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM
Incubation Time: 24 hours
Result: Induces robust apoptosis in RS4;11 cells.
Molecular Weight

889.80

Formula

C₄₈H₄₃Cl₂FN₆O₆

CAS No.

2136247-12-4

SMILES

FC1=C(Cl)C=CC=C1[C@@H]2[C@@]3(C(C=CC(Cl)=C4)=C4NC3=O)C5(CCCCC5)N[C@H]2C(NC6=CC=C(C(NCCCC#CC7=C(CN(C8C(NC(CC8)=O)=O)C9=O)C9=CC=C7)=O)C=C6)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

MD-224MD224MD 224PROTACMDM-2/p53E1/E2/E3 EnzymeProteolysis-targeting chimeraE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseRS4;11leukemiacancerInhibitorinhibitorinhibit

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HY-114312
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