MKI-1

SKU: orb1689339

Description

MKI-1 is a small molecule inhibitor of MASTL kinase (IC50 = 9.9 µM). It acts as a radiosensitizer and exhibits antitumor effects in breast cancer models by reactivating the tumor suppressor PP2A. Its activity has been demonstrated in both cellular and in vivo research studies.

Key Properties

• CAS Number: 1190277-80-5
• MW: 302.33
• Purity: 99.81% (May vary between batches)
• Formula: C₁₈H₁₄N₄O
• SMILES: O=C(Nc1nc2ccccc2[nH]1)c1cccc(c1)-n1cccc1
• Target: Others
• Solubility: DMSO:225 mg/mL (744.22 mM)

Bioactivity

• Target IC50:
  MASTL:9.9 μM
• In Vivo:
  MKI-1 (50 mg/kg, ip, twice a week) enhances the radiosensitivity of the BT549 xenograft model to 6 Gy irradiation, reducing tumor growth without significant changes in body weight .
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• In Vitro:
  MKI-1 (20 μM, 16 h) reduces c-Myc stability through PP2A activation in MCF7 cells. MKI-1 (5-20 μM) inhibits the activity of MASTL in breast cancer cells. MKI-1 (100 μM, 72 h) inhibits various oncogenic properties of breast cancer cells but showed much weaker effects on the viability of normal breast cells. MKI-1 clearly reduces both total c-Myc and serine 62-phosphorylation of c-Myc, with a decrease in ENSA phosphorylation.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

microtubule-associated serine/threonine kinase-like, MKI 1, MKI1, MKI-1, MASTL Kinase Inhibitor-1

Compound Identifiers

PubChem CID

27649598