MKC8866

SKU: orb1308186

Description

MKC8866 is a potent and selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human cell-based assays. It suppresses the production of pro-tumorigenic factors in breast cancer cells and has demonstrated in vivo efficacy by inhibiting tumor growth in prostate cancer models.

Research Area

Cell Biology

Key Properties

• CAS Number: 1338934-59-0
• MW: 361.35
• Purity: 99.85% (May vary between batches)
• Formula: C₁₈H₁₉NO₇
• SMILES: COc1cc2c(C)c(CC(=O)N3CCOCC3)c(=O)oc2c(C=O)c1O
• Target: IRE1
• Solubility: DMSO:3.62 mg/mL (10.02 mM)

Bioactivity

• Target IC50:
  IRE1 Rnase:0.29 μM
• In Vivo:
  MKC8866 (oral; 300 mg/kg; for 28 days) reduces tumor regrowth following NSC 125973 withdrawal .
• In Vitro:
  MKC8866 strongly suppresses DTT-induced X-box-binding protein 1-spliced (XBP1s) expression (EC50: 0.52 μM) and unstressed RPMI 8226 cells (IC50: 0.14 μM). MKC8866 (0.2-10 μM; 3 days) inhibits the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells, and MKC8866 (20 μM; 72 hours) is sufficient to completely block NSC 125973-induced expression of XBP1s . MKC8866 (20 μM; 6 days) reduces the proliferation of all breast cancer cell lines and MKC8866 (20 μM; 48 hours) decreases the number of cells entering the S phase .
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Storage & Handling

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

Alternative Names

Inositol requiring enzyme 1, Inhibitor, MKC 8866, MKC8866, MKC-8866, IRE1 RNase, IRE1, inhibit

Compound Identifiers

PubChem CID

89542346