Nutlin-3a

SKU: orb1301142

Description

Nutlin-3a is the biologically active enantiomer of Nutlin-3, functioning as a potent and selective MDM2 antagonist that disrupts the MDM2-p53 interaction. This stabilization and activation of p53 underpins its utility in cancer research, demonstrating antitumor activity in both cellular assays and in vivo models.

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 675576-98-4
• MW: 581.49
• Purity: 99.71% (May vary between batches)
• Formula: C₃₀H₃₀Cl₂N₄O₄
• SMILES: COc1ccc(C2=N[C@H]([C@H](N2C(=O)N2CCNC(=O)C2)c2ccc(Cl)cc2)c2ccc(Cl)cc2)c(OC(C)C)c1
• Target: Apoptosis,Autophagy,MDM-2/p53,E1/E2/E3 Enzyme
• Solubility: Ethanol:58.2 mg/mL (100.09 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.44 mM);DMSO:55 mg/mL (94.58 mM)

Bioactivity

• Target IC50:
  OVAS cells:25 μM|U2OS cells:3.35 μM|TOV21G cells:14 μM|Vero cells:> 50 μM|U-937 cells:15.6 μM|SKOV3 cells:38 μM|wild-type TP53 (HOC-7, OVCA429 and A2780 cells):4 - 6 μM|MDM2-p53 interaction:90 nM
• In Vivo:
  METHODS: To investigate the mechanism of demyelination induced in vivo, Ionomycin calcium (2-50 µM, 0.5 µL) was dorsal column injected into SD rats. RESULTS: Rats injected with Ionomycin calcium showed varying degrees of lesions observed from days 1-21, including areas of localized edema, a small number of scattered demyelinated axons, and larger lesions containing up to 200 demyelinated or degenerated axons.
• In Vitro:
  METHODS: N1E-115 cells were treated with Ionomycin calcium (0.2-10 µM) for 3-24 h. Cell viability was determined by trypan blue dye exclusion assay. RESULTS: Ionomycin calcium induced cell death in a concentration and time dependent manner. METHODS: Fura-2-loaded mouse cerebellar astrocytes were treated with Ionomycin calcium (0.1-10 µM) for 35 min, and cell membrane Ca(2+) concentration was monitored by changes in the Fura-2 340/380 ratio. RESULTS: At concentrations ≤1 µM [Ca2+]c slowly declined after the initial peak, reaching significantly lower levels after 35 min. However, at 2 µM of ionomycin the peak level of [Ca2+]c was sustained in the plateau phase, and at concentrations >2 µM ionomycin [Ca2+]c was significantly higher after 35 min than at the initial peak.
• Cell Research:
  SRB(Only for Reference)

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, Autophagy, carcinomas, (-)-Nutlin-3, (−)-Nutlin-3, E1 activating enzyme, E2Enzyme, E3 Enzyme, E2 Enzyme, E2 conjugating enzyme, E1/E2/E3 Enzyme, E1 Enzyme, E1Enzyme, E3 ligating enzyme, E3Enzyme, Inhibitor, MDM-2/p53, inhibit, p53, p53/MDM2, Nutlin 3a, Nutlin-3, Nutlin3a, Nutlin-3a, Nutlin-3a chiral, ovarian, Rebemadlin, Ubiquitin ligase, Ubiquitin conjugating enzyme, Ubiquitin activating enzyme

Compound Identifiers

PubChem CID

11433190