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LY-364947

Catalog No. T2048 CAS 396129-53-6

Synonyms: LY 364947, HTS466284

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.

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LY-364947, CAS 396129-53-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 59.00
10 mg	In stock	$ 75.00
25 mg	In stock	$ 146.00
50 mg	In stock	$ 268.00
100 mg	In stock	$ 393.00
200 mg	In stock	$ 589.00
500 mg	In stock	$ 923.00
1 mL * 10 mM (in DMSO)	In stock	$ 66.00

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Purity: 99.96%

Purity: 99.65%

Purity: 99.41%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.
Targets&IC50	TGFβRII:0.4 μM, RIPK2:0.11 μM, CK1δ:0.22 μM, TGFβRI:59 nM, MLK7K:1.4 μM
In vitro	Administering 1 mg/kg i.p. of LY364947 significantly enhances the LYVE-1-positive regions within the tumor tissues in a BxPC3 pancreatic cancer xenograft model. Similarly, 25 mg/kg i.p. of LY364947 markedly increases LYVE-1-positive areas in a chronic peritonitis mouse model, indicating accelerated lymphangiogenesis. Additionally, LY364947 (25 mg/kg) increases p-Akt levels and decreases nuclear Foxo3a in leukemia-initiating cells in mice infected with CML.
In vivo	At a concentration as low as 0.25 μM, LY364947 enhances the xVent2-lux BMP4 response in NMuMG cells by 30%. At 2 μM, it prevents TGF-β-induced epithelial-mesenchymal transition (EMT) in NMuMG cells. A 3 μM dose of LY364947, after 24 hours of treatment, induces the expression of Prox1 and LYVE-1 in nearly all HDLECs. LY364947 promotes the nuclear export of Foxo3a and is characterized by low Smad2/3 and high Akt phosphorylation levels in leukemia-positive cells. When co-cultured with OP-9 stromal cells, LY364947 (at concentrations <20 μM) inhibits the colony-forming ability of leukemia-initiating cells. Acting as an ATP-competitive, tight-binding inhibitor, LY364947 inhibits P-Smad3 phosphorylation through TGFβR-I kinase with a Ki of 28 nM and inhibits Smad2 phosphorylation in NMuMG cells in vivo with an IC50 of 135 nM.
Kinase Assay	The IC50 of LY-364947 at different enzyme concentrations are determined by the filter-binding assay. Typically, 40 μL reactions in 50 mM HEPES at pH 7.5, 1 mM NaF, 200 μM pKSmad3(-3), and 50 mM ATP containing a titration of each inhibitor with concentrations of 1600, 800, 400, 200, 100, 50, 25, and 0 nM are incubated at 30°C for 30 min. The IC50 is calculated using a nonlinear regression method with GraphPad Prism software. The binding type is determined by plotting the correlation between enzyme concentrations and IC50 values.

Synonyms	LY 364947, HTS466284
Molecular Weight	272.3
Formula	C17H12N4
CAS No.	396129-53-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27.2 mg/mL (100 mM)

References and Literature

1. Li HY, et al. J Med Chem, 2006, 49(6), 2138-2142. 2. Vogt J, et al. Cell Signal, 2011, 23(11), 1831-1842. 3. Peng SB, et al. Biochemistry, 2005, 44(7), 2293-2304. 4. Oka M, et al. Blood, 2008, 111(9), 4571-4579. 5. Naka K, et al. Nature, 2010, 463(7281), 676-680. 6. Deng Y, Li L, Zhu J H, et al. COX-2 promotes the osteogenic potential of BMP9 through TGF-β1/p38 signaling in mesenchymal stem cells[J]. Aging (Albany NY) . 2021, 13(8): 11336. 7. Chen Q Z, Li Y, Shao Y, et al. TGF-β1/PTEN/PI3K signaling plays a critical role in the anti-proliferation effect of tetrandrine in human colon cancer cells [J]. International journal of oncology. 2017, 50(3): 1011-1021. 8. Li Q, Ma Y, Liu X L, et al. Anti‑proliferative effect of honokiol on SW620 cells through upregulating BMP7 expression via the TGF‑β1/p53 signaling pathway[J]. Oncology Reports. 2020

Citations

1. Han L, Song B, Zhang P, et al.PC3T: a signature-driven predictor of chemical compounds for cellular transition.Communications Biology.2023, 6(1): 989. 2. Liu S, Yan X, Guo J, et al.Periodontal ligament‐associated protein‐1 knockout mice regulate the differentiation of osteoclasts and osteoblasts through TGF‐β1/Smad signaling pathway.Journal of Cellular Physiology.2023 3. Liu S, Yu X, Guo Q, et al.Periodontal ligament‐associated protein‐1 promotes osteoclastogenesis in mice by modulating TGF‐β1/Smad1 pathway.Journal of Periodontology.2023 4. Liu F, Zhao H, Kong R, et al. Derlin-1 and TER94/VCP/p97 are required for intestinal homeostasis. Journal of Genetics and Genomics. 2021 5. Li Q, Ma Y, Liu X L, et al. Anti-proliferative effect of honokiol on SW620 cells through upregulating BMP7 expression via the TGF-β1/p53 signaling pathway. Oncology Reports. 2020, 44(5): 2093-2107 6. Deng Y, Li L, Zhu J H, et al. COX-2 promotes the osteogenic potential of BMP9 through TGF-β1/p38 signaling in mesenchymal stem cells. Aging (Albany NY). 2021, 13(8): 11336. 7. Li Q, Ma Y, Liu X L, et al. Anti‑proliferative effect of honokiol on SW620 cells through upregulating BMP7 expression via the TGF‑β1/p53 signaling pathway. Oncology Reports. 2020 Nov;44(5):2093-2107

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library TGF-beta/Smad Compound Library Tyrosine Kinase Inhibitor Library Anti-Colorectal Cancer Compound Library Target-Focused Phenotypic Screening Library Cancer Cell Differentiation Compound Library Anti-Fibrosis Compound Library Anti-Liver Cancer Compound Library Bioactive Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

LY-364947 396129-53-6 Apoptosis MAPK Metabolism NF-Κb Stem Cells RIP kinase TGF-beta/Smad Casein Kinase MLK LY 364947 HTS-466284 Transforming growth factor beta receptors Inhibitor inhibit HTS 466284 TGF-β Receptor LY364947 HTS466284 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.