LY-364947 is a selective, ATP-competitive inhibitor of Transforming Growth Factor-β Type I receptor kinase. LY364947 inhibits TGF-β-dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3) (IC50 values are 47 and 89 nM respectively). LY364947 is much less potent at related kinases, with IC50 of 400 nM for TGF-β RII and IC50 of 1400 nM for mixed lineage kinase-7 (MLK-7), a kinase in the MAP kinase signal pathway and closely related to TGF-β RII. LY364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. LY364947 (25 mg/kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice.
Front Immunol. 2022 Mar 8;13:849493.
Reduced NK Cell Cytotoxicity by Papillomatosis-Derived TGF-β Contributing to Low-Risk HPV Persistence in JORRP Patients
LY364947 purchased from AbMole
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Source | Cancer Res (2012). Figure 1. LY364947 |
| Method | clonogenic assay | |
| Cell Lines | radiosensitizes glioma cells | |
| Concentrations | 400 nM | |
| Incubation Time | 24 h | |
| Results | Regardless of TGFβ-mediated growth modulation, addition of the TGFβ inhibitor LY364947 significantly increased the radiosensitivity of all three cell lines as measured in clonogenic assay |
| Molecular Weight | 272.31 |
| Formula | C17H12N4 |
| CAS Number | 396129-53-6 |
| Solubility (25°C) | DMSO 10 mg/mL (ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related TGF-β Receptor Products |
|---|
| LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. |
| LSKL, Inhibitor of Thrombospondin (TSP-1)
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. |
| KRFK
KRFK, a peptide derived from TSP-1, can activate TGF-β. |
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Maohuoside A potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways |
| Vicatertide
Vicatertide is a TGF beta-1 inhibitor. |
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