LY-364947
Based on 24 publication(s) in Google Scholar
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.23%
- CAS No.: 396129-53-6
- Formule: C17H12N4
- Masse moléculaire:272.30
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) LY-364947
More- Theranostics. 2024 Jan 1;14(3):1049-1064. [Abstract]
- Cell Discov. 2022 Sep 20;8(1):94. [Abstract]
- Genome Med. 2025 Aug 15;17(1):90. [Abstract]
- Pharmacol Res. 2021 Oct:172:105797. [Abstract]
- ACS Appl Mater Interfaces. 2025 Apr 2;17(13):19286-19303. [Abstract]
- Haematologica. 2020 Mar;105(3):674-686. [Abstract]
- Oncogene. 2019 Jun;38(23):4637-4654. [Abstract]
- Neural Regen Res. 2025 Jun 19. [Abstract]
- Cell Biosci. 2019 Jun 14:9:48. [Abstract]
- World J Gastroenterol. 2017 Apr 7;23(13):2330-2336. [Abstract]
- Mol Oncol. 2024 May 21. [Abstract]
- World Allergy Organ J. 2025 Oct 10;18(10):101126. [Abstract]
- FASEB J. 2022 Dec;36(12):e22625. [Abstract]
- iScience. 2024 Mar 29;27(6):109625. [Abstract]
- J Cell Physiol. 2019 May;234(5):6263-6273. [Abstract]
- BMC Complement Med Ther. 2023 Feb 21;23(1):62. [Abstract]
- Cell Transplant. 2023 Jan-Dec:32:9636897231177356. [Abstract]
- Environ Toxicol. 2022 Jun;37(6):1321-1331. [Abstract]
- Curr Res Toxicol. 2024 Oct 24:7:100199. [Abstract]
- J Cosmet Dermatol. 2021 Jul;20(7):2287-2295. [Abstract]
- Biochem Biophys Res Commun. 2020 Jan 29;522(1):270-277. [Abstract]
- Int J Clin Exp Pathol. 2018 Dec 1;11(12):5592-5601. [Abstract]
- Research Square Preprint. 2021 Nov.
- Eur Rev Med Pharmacol Sci. 2017 Apr;21(7):1551-1558. [Abstract]
Customer Validation & Images
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WB
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RT-PCR
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Cell Migration/Invasion Assay
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WB
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WB
Activité biologique
IC50: 59 nM (TGFβR-I)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
60 nM
Compound: HTS-466284
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Inhibition of TGF-beta-induced expression of PAI-luciferase reporter in HepG2 cells
Inhibition of TGF-beta-induced expression of PAI-luciferase reporter in HepG2 cells
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[PMID: 14643325] |
| NIH3T3 | IC50 |
0.081 μM
Compound: LY-364947
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Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
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[PMID: 18314943] |
| NIH3T3 | IC50 |
0.081 μM
Compound: LY-364947
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Inhibitory activity against TGF-beta-stimulated proliferation in NIH3T3 cells
Inhibitory activity against TGF-beta-stimulated proliferation in NIH3T3 cells
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[PMID: 16539403] |
| Sf9 | IC50 |
0.051 μM
Compound: 1
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Inhibition of human Transforming growth factor (TGF) beta-1 receptor (T204D mutation) autophosphorylation in Sf9 cells
Inhibition of human Transforming growth factor (TGF) beta-1 receptor (T204D mutation) autophosphorylation in Sf9 cells
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[PMID: 12954047] |
| Sf9 | IC50 |
0.059 μM
Compound: LY-364947
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Inhibition of recombinant human TGFbeta R1 expressed in Sf9 cells
Inhibition of recombinant human TGFbeta R1 expressed in Sf9 cells
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[PMID: 16539403] |
| Sf9 | IC50 |
0.059 μM
Compound: LY-364947
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Inhibition of TGFbeta type receptor 1 ALK5 (T204D) expressed in Sf9 cells
Inhibition of TGFbeta type receptor 1 ALK5 (T204D) expressed in Sf9 cells
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[PMID: 18314943] |
LY-364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I Kinase with Ki of 28 nM. LY-364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY-364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY-364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY-364947 (2 μM) prevents TGF-β-induced epithelial mesenchymal transition in NMuMg cells[1]. LY-364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours[2]. LY-364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY-364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 396129-53-6
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Appearance Solid
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Masse moléculaire 272.30
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Formule C17H12N4
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Color Off-white to yellow
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SMILES
C1(C2=CNN=C2C3=NC=CC=C3)=CC=NC4=CC=CC=C14
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Synonyms
HTS466284
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (24)
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Journal Impact Factor
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Most Recent
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Theranostics
Keratinocyte-to-macrophage communication exacerbate psoriasiform dermatitis via LRG1-enriched extracellular vesicles. [Abstract]2024 Jan 1;14(3):1049-1064. PMID: 38250043 -
Cell Discov
Single-cell transcriptome reveals cellular hierarchies and guides p-EMT-targeted trial in skull base chordoma. [Abstract]2022 Sep 20;8(1):94. PMID: 36127333
LY-364947 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94. [Abstract]
Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h repressed the p-EMT-like program, as evidenced by decreased ZEB2 and TGFBI protein levels in the UM‑Chor1 cell line.
LY-364947 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94. [Abstract]
Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h repressed the p-EMT-like program, as evidenced by decreased ZEB2 and TGFBI mRNA levels in the UM‑Chor1 cell line.
LY-364947 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94. [Abstract]
Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h attenuated the invasiveness of UM‑Chor1 cells.
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Genome Med
Aging increases susceptibility to liver fibrosis through enhanced NAT10-mediated ac4C modification of TGFβ1 mRNA. [Abstract]2025 Aug 15;17(1):90. PMID: 40817062 -
Pharmacol Res
A phosphoproteomics study reveals a defined genetic program for neural lineage commitment of neural stem cells induced by olfactory ensheathing cell-conditioned medium. [Abstract]2021 Oct:172:105797. PMID: 34352399 -
ACS Appl Mater Interfaces
Facile Nanocomposite Hydrogel Scaffold with Sustained Drug Release and Osteo-Immunomodulatory Effects to Enhance Bone Regeneration. [Abstract]2025 Apr 2;17(13):19286-19303. PMID: 40116446 -
Haematologica
2020 Mar;105(3):674-686. PMID: 31289206 -
Oncogene
MSC-regulated lncRNA MACC1-AS1 promotes stemness and chemoresistance through fatty acid oxidation in gastric cancer. [Abstract]2019 Jun;38(23):4637-4654. PMID: 30742067 -
Neural Regen Res
Exacerbation of neuronal senescence after spinal cord injury: Role of the macrophage-derived transforming growth factor-β1-SMAD2 signaling axis. [Abstract]2025 Jun 19. PMID: 40537008 -
Cell Biosci
Label-free quantitative proteomics identifies transforming growth factor β1 (TGF-β1) as an inhibitor of adipogenic transformation in OP9-DL1 cells and primary thymic stromal cells. [Abstract]2019 Jun 14:9:48. PMID: 31249661 -
World J Gastroenterol
Notch signaling mediated by TGF-β/Smad pathway in concanavalin A-induced liver fibrosis in rats. [Abstract]2017 Apr 7;23(13):2330-2336. PMID: 28428712 -
Mol Oncol
Targeting chondroitin sulfate suppresses macropinocytosis of breast cancer cells by modulating syndecan-1 expression. [Abstract]2024 May 21. PMID: 38770553 -
World Allergy Organ J
Increased LOXL2 facilitates tissue remodeling in eosinophilic chronic rhinosinusitis with nasal polyps. [Abstract]2025 Oct 10;18(10):101126. PMID: 41143091 -
FASEB J
Renal tubular epithelial cell necroptosis promotes tubulointerstitial fibrosis in patients with chronic kidney disease. [Abstract]2022 Dec;36(12):e22625. PMID: 36331546 -
iScience
Organic phosphate but not inorganic phosphate regulates Fgf23 expression through MAPK and TGF-ꞵ signaling. [Abstract]2024 Mar 29;27(6):109625. PMID: 38883842 -
J Cell Physiol
TGF-β1-PML SUMOylation-peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) form a positive feedback loop to regulate cardiac fibrosis. [Abstract]2019 May;234(5):6263-6273. PMID: 30246389
LY-364947 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2019 May;234(5):6263-6273. [Abstract]
NMCFs are treated with TGF-β1 (5 ng/mL) and LY364947 (LY, 3 μM) for 6 hr. The protein levels are analyzed by western blot analysis.
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BMC Complement Med Ther
Baicalein alleviates fibrosis and inflammation in systemic sclerosis by regulating B-cell abnormalities. [Abstract]2023 Feb 21;23(1):62. PMID: 36810081 -
Cell Transplant
Dexamethasone Induces Senescence-Associated Changes in Trabecular Meshwork Cells by Increasing ROS Levels Via the TGFβ/Smad3-NOX4 Axis. [Abstract]2023 Jan-Dec:32:9636897231177356. PMID: 37265069 -
Environ Toxicol
Inorganic arsenic promotes apoptosis of human immortal keratinocytes through the TGF-β1/ERK signaling pathway. [Abstract]2022 Jun;37(6):1321-1331. PMID: 35142421 -
Curr Res Toxicol
Hydrogen sulfide donor NaHS inhibits formaldehyde-induced epithelial-mesenchymal transition in human lung epithelial cells via activating TGF-β1/Smad2/3 and MAPKs signaling pathways. [Abstract]2024 Oct 24:7:100199. PMID: 39524036 -
J Cosmet Dermatol
Inhibitory effect of glutathione S-transferase A3 in the progression of cutaneous squamous cell carcinoma. [Abstract]2021 Jul;20(7):2287-2295. PMID: 33089654 -
Biochem Biophys Res Commun
TOPK promotes epithelial-mesenchymal transition and invasion of breast cancer cells through upregulation of TBX3 in TGF-β1/Smad signaling. [Abstract]2020 Jan 29;522(1):270-277. PMID: 31757421
LY-364947 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Jan 29;522(1):270-277. [Abstract]
MDA-MB-231 cells are pretreated with DMSO or LY364947 (1 μM) for 1 h, and then treated with or without TGF-β1 for 6 h. Immunoblotting is done using indicated antibody.
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Int J Clin Exp Pathol
TGF-β1/Smad3 signaling promotes collagen synthesis in pulmonary artery smooth muscle by down-regulating miR-29b. [Abstract]2018 Dec 1;11(12):5592-5601. PMID: 31949646 -
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Eur Rev Med Pharmacol Sci
TGFβ1 protects myocardium from apoptosis and oxidative damage after ischemia reperfusion. [Abstract]2017 Apr;21(7):1551-1558. PMID: 28429351
Solvant et solubilité
DMSO : 15.62 mg/mL (57.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (4.59 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
BALB/c nude mice 5 to 6 weeks of age are used in the assay. Parental, or VEGF-C- or TGF-β1-expressing tumor cells (5×106) in 100 μL PBS are implanted subcutaneously into male nude mice and allowed to grow for 2 to 3 weeks to reach proliferative phase, before initiation of TβR-I inhibitor administration. TβR-I inhibitor LY-364947, dissolved in 5 mg/mL in DMSO and diluted with 100 μL PBS, or the vehicle control, is injected intraperitoneally at 1 mg/kg, 3 times a week for 3 weeks. Excised samples are directly frozen in dry-iced acetone for immunohistochemistry. Frozen samples are further sectioned at 10-μm thickness in a cryostat and subsequently incubated with primary and secondary antibodies. Samples are observed using a confocal microscope.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (624 KB)
- English - EN (624 KB)
- Français - FR (624 KB)
- Deutsch - DE (624 KB)
- Norwegian - NO (624 KB)
- Español - ES (624 KB)
- Swedish - SV (624 KB)
- Italian - IT (624 KB)
- Portuguese - PT (624 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Peng SB, et al. Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition. Biochemistry, 2005, 44(7), 2293-2304. [Content Brief]
[2]. Oka M, et al. Inhibition of endogenous TGF-beta signaling enhances lymphangiogenesis. Blood, 2008, 111(9), 4571-4579. [Content Brief]
[3]. Naka K, et al. TGF-beta-FOXO signalling maintains leukaemia-initiating cells in chronic myeloid leukaemia. Nature, 2010, 463(7281), 676-680. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6724 mL | 18.3621 mL | 36.7242 mL | 91.8105 mL |
| 5 mM | 0.7345 mL | 3.6724 mL | 7.3448 mL | 18.3621 mL | |
| 10 mM | 0.3672 mL | 1.8362 mL | 3.6724 mL | 9.1811 mL | |
| 15 mM | 0.2448 mL | 1.2241 mL | 2.4483 mL | 6.1207 mL | |
| 20 mM | 0.1836 mL | 0.9181 mL | 1.8362 mL | 4.5905 mL | |
| 25 mM | 0.1469 mL | 0.7345 mL | 1.4690 mL | 3.6724 mL | |
| 30 mM | 0.1224 mL | 0.6121 mL | 1.2241 mL | 3.0604 mL | |
| 40 mM | 0.0918 mL | 0.4591 mL | 0.9181 mL | 2.2953 mL | |
| 50 mM | 0.0734 mL | 0.3672 mL | 0.7345 mL | 1.8362 mL |
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