MKC8866

SKU: orb1218915

Description

MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibit prostate cancer (PCa) tumor growth.

Key Properties

• CAS Number: 1338934-59-0
• MW: 361.35
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₉NO₇
• SMILES: O=CC1=C(O)C(OC)=CC2=C1OC(C(CC(N3CCOCC3)=O)=C2C)=O
• Target: IRE1 RNase
• Solubility: DMSO:16.67 mg/mL (46.13 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  MKC8866 (oral; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal. Animal model: Female athymic nude mice with MDA-MB-231 tumor. Dosage: 300 mg/kg. Administration: Oral; for 28 days. Result: Reduced tumor regrowth post-NSC 125973 withdrawal.
  Read more...
• In Vitro:
  MKC8866 (20 μM; 6 days) decreases proliferation of all breast cancer cell lines. MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase. MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells. MKC8866 (20 μM; 72 hours) is sufficient to completely block NSC 125973-induced expression of XBP1s. Cell Proliferation Assay. Cell line: MCF7, SKBR3, MDA-MB-231 and MCF10A cells. Concentration: 20 μM. Incubation time: For 6 days. Result: Decreased proliferation of all breast cancer cell lines. Cell Cycle Analysis Cell line: MDA-MB-231, MCF7 and SKBR3 cells. Concentration: 20 μM. Incubation time: 48 hours. Result: Reduced the number of cells entering S phase. Cell Cycle Analysis Cell line: LNCaP, VCaP, 22Rv1 and C4-2B cells. Concentration: 0.2, 0.5, 1, 5, 10 μM Incubation time: 3 days. Result: Suppressed the viability of all four cell lines in a dose-dependent manner. Cell Cycle Analysis Cell line: MDA-MB-231 cells. Concentration: 20 μM. Incubation time: 72 hours. Result: Completely blocked NSC 125973-induced expression of XBP1s.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

IRE1 RNase