DMAPT

SKU: orb1309755

Description

DMAPT is an orally bioavailable dimethylamino analog of parthenolide that potently inhibits NF-κB. It demonstrates cytotoxic activity against primary AML cells with an LD₅₀ of 1.7 µM and has been investigated in preclinical studies for its potential anti-tumor and anti-metastatic properties in both cellular and animal models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 870677-05-7
• MW: 293.4
• Purity: >99.99% (May vary between batches)
• Formula: C₁₇H₂₇NO₃
• SMILES: [H][C@@]12CC\C(C)=C/CC[C@@]3(C)O[C@@H]3[C@@]1([H])OC(=O)[C@@H]2CN(C)C
• Target: NF-κB
• Solubility: H2O:insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (13.63 mM);DMSO:100 mg/mL (340.83 mM)

Bioactivity

• Target IC50:
  NF-κB:1.7 μM(LD50)
• In Vivo:
  DMAPT (100 mg/kg, oral gavage daily for 7 days) treatment can increase the sensitivity of PC-3 tumor xenografts to X-rays. DMAPT (100 mg/kg, 42 to 300 days from birth, oral gavage three times a week) treatment can slow the normal tumor development of TRAMP mice and prolong the reachable prostate tumor time by 20%. DMAPT further reduced the lung tissue transfer area of TRAMP mice to below the water vehicle treatment group (0.10%±0.15 SD, 92% reduction, p = 0.0028).
• In Vitro:
  DMAPT treatment reduced the constitutive NF-κB binding activity and inhibited the proliferation and viability of PC-3 and DU145 cells. Treatment of PC-3 and DU145 cells with 5 and 4 μM DMAPT, respectively, increased the population doubling time of PC-3 prostate cancer cells from 23.0±5.0 h to 42.0±3.0 h, while the population doubling time of DU145 cells increased from 20.4±2.2 h By 72.5±24.8 hours.

Storage & Handling

• Storage: 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

Dimethylamino Parthenolide, DMAPT, inhibit, NF-κB, Nuclear factor-kappaB, Nuclear factor-κB, NF-kB, NFkB, NFκB, Inhibitor

Compound Identifiers

PubChem CID

129395999