LY2157299 (Galunisertib) could inhibit TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells. Furthermore, administration of LY2157299 ameliorated anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure in vivo. LY2157299 also shows dose dependent potentiation of VEGF or bFGF induced cell proliferation in HUVEC. LY2157299 blocked the phsophorylation of Smad2 but had no effect on fibroblast growth factor (FGF) or platelet-derived growth factor (PDGF) signaling. In the in vitro VEGF-stimulated cord formation assay, LY2157299 potentiates angiogenesis. LY2157299 induces angiogenesis and enhances VEGF and basic-fibroblast-growth-factor-induced angiogenesis in a Matrigel-plug assay, whereas adding an alpha5-integrin-neutralizing antibody to the Matrigel selectively inhibits this enhanced response.
Composites Part B. 2023 Feb 15;110487.
Construction of tissue-engineered vascular grafts with high patency by mimicking immune stealth and blocking TGF-β mediated endothelial-to-mesenchymal transition
LY2157299 (Galunisertib) purchased from AbMole
EMBO Mol Med. 2019 Aug;11(8):e9830.
An autocrine ActivinB mechanism drives TGFβ/Activin signaling in Group 3 medulloblastoma.
LY2157299 (Galunisertib) purchased from AbMole
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Source | Universite Paris-Sud (2014). Figure 6. LY2157299 (Abmole Bioscience) |
| Method | Flow cytometry | |
| Cell Lines | IGR-CaP1 and IGR-CaP1-R cells | |
| Concentrations | 25 μM | |
| Incubation Time | 72 h | |
| Results | "Our results show that the targeting of the TGFβ signaling pathway with LY2157299 in combination with Docetaxel induces cell death of the Docetaxel-resistant cells." |
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Source | Universite Paris-Sud (2014). Figure 5. LY2157299 (Abmole Bioscience) |
| Method | Clonogenicity assay | |
| Cell Lines | IGR-CaP1 and IGR-CaP1-R cells | |
| Concentrations | 25 μM | |
| Incubation Time | 72 h | |
| Results | Figure 5A shows that treatment of cells with 25μM of LY2157299 alone did not affect the survival of parental and resistant cells. |
| Cell Experiment | |
|---|---|
| Cell lines | HCC cell |
| Preparation method | HCC cells were incubated in serum-free medium overnight and treated with 5 ng/mL of TGF-β for 1 hour followed by the addition of 1 or 10 μM galunisertib for 5 and 24 hours. Concentrations were selected to be in the range of observed plasma exposure |
| Concentrations | 1 or 10 µM |
| Incubation time | 5 and 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Sprague-Dawley male rats |
| Formulation | 0.9% NaCl water |
| Dosages | 75 mg/kg/day |
| Administration | intragastrically |
| Molecular Weight | 369.42 |
| Formula | C22H19N5O |
| CAS Number | 700874-72-2 |
| Solubility (25°C) | DMSO 80 mg/mL |
| 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.
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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. |
| Maohuoside A
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| Vicatertide
Vicatertide is a TGF beta-1 inhibitor. |
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