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Chemical Structure| 396129-53-6 Chemical Structure| 396129-53-6

Structure of LY364947
CAS No.: 396129-53-6

Chemical Structure| 396129-53-6

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LY-364947 (HTS466284) displays potent ATP-competitive inhibition of TGFβR-I with an IC50 of 59 nM and exhibits 7-fold selectivity over TGFβR-II.

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Product Citations

Product Citations

Lou, Peng ; Liu, Shuyun ; Wang, Yizhuo ; Pan, Cheng ; Xu, Xuewen ; Zhao, Meng , et al.

Abstract: Chronic wounds remain a worldwide clinical challenge, and bioactive materials that can promote skin regeneration are required. Self-assembling peptide (SAP) hydrogels have shown great potential in tissue repair, but their regenerative efficacy and possible mechanism in chronic wound healing are unclear. Here, we report an SAP (KGH) that enhances extracellular matrix (ECM) remodeling and angiogenesis, thereby promoting chronic wound healing in diabetic mice. In vivo, the KGH hydrogel was retained in wounds up to 7 days after injection, and it was effective in speeding up wound closure by ∼20% compared to the control groups and enhancing angiogenesis (e.g., VEGFA, CD31+ capillaries), cell proliferation (e.g., PCNA+ cells), formation of granulation tissue (e.g., α-SMA), and ECM deposition/remodeling (e.g., collagen I, fibronectin). In vitro, the KGH hydrogel created a 3D microenvironment for skin cells, maintained the sustained growth of cell spheroids, and increased the secretion of ECM proteins (e.g., laminin) and growth factors (e.g., PDGFB, VEGFA, and TGF-β) in skin keratinocytes compared to the conventional 2D culture. Mechanistically, the KGH hydrogel might promote wound tissue regeneration by activating the Rho/ROCK and TGF-β/MEK/MAPK pathways. As a type of designed material, SAP can be further re-engineered with biological motifs, therapeutic reagents, or stem cells to enhance skin regeneration. This study highlights that SAP hydrogels are a promising material platform for advanced chronic wound healing and might have translational potential in future clinical applications.

Keywords: Chronic wound ; Self-assembling peptide ; 3D culture ; Extracellular matrix ; Angiogenesis

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Product Details of LY364947

CAS No. :396129-53-6
Formula : C17H12N4
M.W : 272.30
SMILES Code : C1(C2=CNN=C2C3=NC=CC=C3)=CC=NC4=CC=CC=C14
MDL No. :MFCD00800758
InChI Key :IBCXZJCWDGCXQT-UHFFFAOYSA-N
Pubchem ID :447966

Safety of LY364947

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • CK1

    CK1δ, IC50:0.22 μM

  • TGFβRII

    TGFβRII, IC50:0.4 μM

  • TGFβRI/ALK5

    TGFβRI, IC50:59 nM

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.67mL

0.73mL

0.37mL

18.36mL

3.67mL

1.84mL

36.72mL

7.34mL

3.67mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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