For research use only. Not for therapeutic Use.
LY2109761(CAT: I004628) is a novel selective inhibitor that targets both type I and type II receptors of the transforming growth factor-beta (TGF-β) pathway. It acts as a dual inhibitor of TGF-β receptor type I (TβRI) and type II (TβRII) with Ki values of 38 nM and 300 nM, respectively. By inhibiting these receptors, LY2109761 negatively affects the phosphorylation of Smad2, a downstream effector of the TGF-β signaling pathway. This inhibition of TGF-β signaling can have therapeutic implications, as dysregulation of the TGF-β pathway is implicated in various diseases, including cancer, fibrosis, and immune disorders. LY2109761 has been studied for its potential as an anti-cancer agent and for its ability to modulate TGF-β signaling in other pathological conditions.
| Catalog Number | I004628 |
| CAS Number | 700874-71-1 |
| Synonyms | 4-[2-[4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl]oxyethyl]morpholine |
| Molecular Formula | C26H27N5O2 |
| Purity | ≥95% |
| Target | TGF-βR1(ALK5) |
| Solubility | 10 mM in DMSO |
| Storage | 3 years -20C powder |
| IC50 | 38 nM/300 nM(Ki, TβRI/II) [1] |
| IUPAC Name | 4-[2-[4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl]oxyethyl]morpholine |
| InChI | InChI=1S/C26H27N5O2/c1-2-9-27-22(4-1)26-25(24-5-3-11-31(24)29-26)21-8-10-28-23-18-19(6-7-20(21)23)33-17-14-30-12-15-32-16-13-30/h1-2,4,6-10,18H,3,5,11-17H2 |
| InChIKey | IHLVSLOZUHKNMQ-UHFFFAOYSA-N |
| SMILES | C1CC2=C(C(=NN2C1)C3=CC=CC=N3)C4=C5C=CC(=CC5=NC=C4)OCCN6CCOCC6 |
| Reference | <br /> |
