XMD8-87

SKU: orb1303864

Description

XMD8-87 (ACK1-B19) is a potent and selective small molecule inhibitor of TNK2 (ACK1) kinase activity, effectively blocking its autophosphorylation. This compound, along with the analog XMD16-5, suppresses oncogenic TNK2 truncation mutants and is a valuable chemical probe for studying ACK1 signaling in cancer cell lines and in vivo tumor models.

Research Area

Metabolism Research, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 1234480-46-6
• MW: 445.52
• Purity: 98.05%
• Formula: C₂₄H₂₇N₇O₂
• SMILES: COc1cc(ccc1Nc1ncc2NC(=O)c3ccccc3N(C)c2n1)N1CCN(C)CC1
• Target: PPAR,Tyrosinase
• Solubility: Ethanol:5 mg/mL (11.22 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:5.33 mg/mL (11.96 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.24 mM)

Bioactivity

• Target IC50:
  D163E mutations:16nM|R806Q mutations:77 nM
• In Vitro:
  XMD8-87 is found to be potent in the inhibition of TNK2 phosphorylation. XMD8-87 and XMD16-5 potently inhibit phosphorylation of TNK2 truncation mutations found in solid tumor types.
• Cell Research:
  293T cells expressing TNK2 are plated in 6-well format at a density of 250,000 cells per well 48 hours prior to treatment. Cells are then treated with a 100 μL of XMD8-87 or XMD16-5 at 5 μmol/L and with 9 1:1 serial dilutions down to ≈10 nmol/L. Two additional samples are treated with DMSO only. Cells are then incubated for 6 hours at 37°C. Protein extraction is accomplished by adding 300 μL of lysis buffer to cells after removing media. Plates are gently shaken for 5 minutes at room temperature. Lysates are collected and cleared of incompletely solubilized material by spinning for 10 minutes at maximum speed in a microcentrifuge. Samples are prepared for SDS-PAGE using the EPage loading buffer.(Only for Reference)

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

ACK1-B19, Inhibitor, inhibit, XMD887, XMD-8-87, XMD8-87, XMD8 87, TNK2, Tyrosinase

Compound Identifiers

PubChem CID

53322923