| Bioactivity | JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines[1]. |
| Invitro | JH-XVII-10 (compound 10) (1 µM; CAL27 cells) shows active against JNK1 (IC50=1130 nM), JNK2 (IC50=1100 nM), JNK3 (IC50=>10 000 nM), FAK (IC50=90 nM), RSK1 (IC50=82 nM), RSK2 (IC50=80 nM), RSK3 (IC50=61 nM)[1].JH-XVII-10 (10 µM; 72 h) decreases cell proliferation by ~45%, and ~40% for CAL27 and FaDu cells, respectively[1].JH-XVII-10 (1, 10 µM; 24 h) induces apoptosis in CAL27 cells[1].JH-XVII-10 (0.5, 1, 5, 10 µM; 24 h) shows inhibitory effects on pro-tumor signaling in CAL27 cells[1]. Cell Proliferation Assay[1] Cell Line: |
| Name | JH-XVII-10 |
| Formula | C22H18F4N8O |
| Molar Mass | 486.42 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |