LY364947

Catalog No.S2805 Synonyms: HTS 466284

LY364947 Chemical Structure

Molecular Weight(MW): 272.3

LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.

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2 Customer Reviews

  • The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively.

    Chem Biol Interact 2014 217, 1-8. LY364947 purchased from Selleck.

    HCECs were treated with TGF-β1 (10 ng/ml) alone, or in combination with LY364947 (2μM) for 3days. The protein expression of p16 and p21 in HCECs induced by TGF-β1.

    Aging (Albany NY), 2016, 8(10):2337-2354.. LY364947 purchased from Selleck.

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Biological Activity

Description LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.
Targets
TGFβRI [1]
(Cell-free assay)
RIPK2 [2]
(Cell-free assay)
CK1δ [2]
(Cell-free assay)
TGFβRII [1]
(Cell-free assay)
MLK-7K [1]
(Cell-free assay)
59 nM 0.11 μM 0.22 μM 0.4 μM 1.4 μM
In vitro

LY364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I kinase with Ki of 28 nM. LY364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY364947 (2 μM) prevents TGF-β-induced epithelial−mesenchymal transition in NMuMg cells. [3] LY364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. [4] LY364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells. [5]

In vivo LY364947 (1 mg/kg i.p.) accelerates lymphangiogenesis, as evidence by significantly increased the LYVE-1-positive areas, in a mouse model of chronic peritonitis. LY364947 (1 mg/kg i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells. [4] LY364947 (25 mg /kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice. [5]

Protocol

Animal Research:[4]
+ Expand
  • Animal Models: Tumor xenograft models with BxPC3 pancreatic adenocarcinoma cells.
  • Formulation: Dissolved in 5 mg/mL in DMSO and diluted with 100 μL PBS
  • Dosages: 1 mg/kg
  • Administration: Intraperitoneally administrated 3 times a week for 3 weeks.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 1 mg/mL (3.67 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+ddH2O 0.75mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 272.3
Formula

C17H12N4

CAS No. 396129-53-6
Storage powder
in solvent
Synonyms HTS 466284

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID