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MAPK MLK LY364947

LY364947

Catalog No. T2048   CAS 396129-53-6
Synonyms: LY 364947, LY-364947, HTS466284

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

LY364947, CAS 396129-53-6
Pack Size Availability Price/USD Quantity
5 mg In stock 78.00
10 mg In stock 105.00
25 mg In stock 220.00
50 mg In stock 330.00
100 mg In stock 510.00
200 mg In stock 765.00
1 mL * 10 mM (in DMSO) In stock 84.00
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Purity 99.65%
Purity 99.96%
Biological Description
Chemical Properties
Storage & Solubility Information
Description LY364947 is a potent ATP-competitive inhibitor of TGFβR-I.
Targets&IC50 CK1δ : ic50 0.22μM ,   MLK-7K : ic50 1.4μM ,   RIPK2 : ic50 0.11μM ,   TGFβRI : ic50 59nM ,   TGFβRII : ic50 0.4μM
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.
Animal Research
Animal Model: Tumor xenograft models with BxPC3 pancreatic adenocarcinoma cells.
Synonyms LY 364947 , LY-364947 , HTS466284
Purity 99.65%
Molecular Weight 272.3
Formula C17H12N4
CAS No. 396129-53-6

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 27.2 mg/mL (100 mM)

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

Citations

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

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-cancer Compound Library

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