| Bioactivity | STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM.STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 in the low nanomolar range by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model[1]. |
| CAS | 2591440-71-8 |
| Formula | C36H32F3N7O5 |
| Molar Mass | 699.68 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Peng He, et al. Discovery of a Highly Potent and Orally Bioavailable STAT3 Dual Phosphorylation Inhibitor for Pancreatic Cancer Treatment. J Med Chem. 2022 Nov 24;65(22):15487-15511. |
STAT3-IN-32
CAS: 2591440-71-8 F: C36H32F3N7O5 W: 699.68
STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tet
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