SM1-71

SKU: orb2901012

Description

SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.

Key Properties

• CAS Number: 2088179-99-9
• MW: 463.96
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₆ClN₇O
• SMILES: CN1CCN(CC1)c1ccc(Nc2ncc(Cl)c(Nc3ccccc3NC(=O)C=C)n2)cc1
• Target: p38 MAPK
• Solubility: In Vitro: DMSO : 125 mg/mL (269.42 mM; Ultrasonic )

Bioactivity

• In Vitro:
  SM1-71 (0.001-100 μM; 72 h) potently inhibits the proliferation of H23 and Calu-6 non-small cell lung cancer cell lines with a concentration-dependent manner. SM1-71 (72 h) induces potent cytotoxicity with nanomolar values for GR50 and negative GRmax values in eight of 11 cancer cell lines. Cell Viability Assay Cell line: H23-KRASG12C and Calu-6-KRASQ61K cells. Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM Incubation time: 72 hours. Result: Inhibited proliferation of H23-KRASG12C and Calu-6-KRASQ61K cells with IC50s of 0.4 and 0.3 μM, respectively.

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

p38 MAPK