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LY-364947

Catalog No. T2048 CAS 396129-53-6

Synonyms: LY 364947, HTS466284

LY364947 is a potent ATP-competitive inhibitor of TGFβR-I.

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LY-364947, CAS 396129-53-6

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	LY364947 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, MLK-7K:1.4 μM
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 2 years

Solubility Information

DMSO: 27.2 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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. 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 2. 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. 3. 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 4. 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

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

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 MLK RIP kinase TGF-beta/Smad Casein Kinase LY364947 LY 364947 Transforming growth factor beta receptors Inhibitor inhibit HTS-466284 HTS 466284 HTS466284 TGF-β Receptor inhibitor

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