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LY2409881 trihydrochloride

Catalog No. T2081 CAS 946518-60-1

Synonyms: LY2409881

LY2409881 trihydrochloride is a novel specific inhibitor of IKK2 (IC50: 30 nM); IC50 for IKK1 and other common kinases is at least one log higher.

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LY2409881 trihydrochloride Chemical Structure

LY2409881 trihydrochloride, CAS 946518-60-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 177.00
25 mg	In stock	$ 353.00
50 mg	In stock	$ 547.00
100 mg	In stock	$ 788.00
1 mL * 10 mM (in DMSO)	In stock	$ 139.00

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Purity: 98%

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Description	LY2409881 trihydrochloride is a novel specific inhibitor of IKK2 (IC50: 30 nM); IC50 for IKK1 and other common kinases is at least one log higher.
Targets&IC50	IKK2:30 nM
Kinase Assay	CYP3A activity is assessed using the probe reactions, midazolam-1′-hydroxylation and testosterone 6β-hydroxylation. For reversible inhibition, incubations (37°C, 10 min) are composed of (final concentrations): potassium phosphate buffer (100 mM, pH 7.4), β-NADPH (1 mM), magnesium chloride (5 mM), microsomal protein (0.025 mg/mL), probe substrate (1 μM midazolam or 25 μM testosterone), LCL161 (0, 0.5, 1, 5, 10, 25, 50, or 100 μM) and organic solvent (0.2% acetonitrile for midazolam, 0.2% methanol for testosterone). After a 3-minute preincubation, the reactions are initiated by addition of β-NADPH and terminated by addition of acetonitrile (two volumes). Reactions are previously shown to be linear with respect to time and protein concentration (results not shown) with midazolam and testosterone turnover of 8.7±1.3% (n=3) and 2.6±0.20%, respectively. Formation of 1′-hydroxymidazolam and 6β-hydroxytestosterone is determined by LC-MS/MS as described below[3].
Cell Research	Cytotoxicity is evaluated using the CellTiter-Glo Reagent according to the manufacturer's manual. Experiments are carried out in 96-well plates, with each treatment in triplicate. Samples are taken at typically 24, 48, and 72 hours after treatment. Cytotoxicity is expressed by the decreasing percentage of live cells in each treatment relative to the untreated control from the same experiment. IC50 for each cell line is calculated using the CalcuSyn Version 2.0 software.(Only for Reference)

Synonyms	LY2409881
Molecular Weight	594.43
Formula	C24H32Cl4N6OS
CAS No.	946518-60-1

Storage

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

Solubility Information

DMSO: 16 mg/mL (26.9 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Deng C, et al. Clin Cancer Res. 2015, 21(1):134-145.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Liver Cancer Compound Library Immunology/Inflammation Compound Library Kinase Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Pyroptosis Compound Library NF-κB Signaling Compound Library Anti-Prostate Cancer Compound Library HIF-1 Signaling Pathway Compound Library

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Keywords

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