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Bay 65-1942 hydrochloride

Catalog No. T14508   CAS 600734-06-3

Bay 65-1942 hydrochloride is an inhibitor of ATP-competitive and selective IKKβ.

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Bay 65-1942 hydrochloride Chemical Structure
Bay 65-1942 hydrochloride, CAS 600734-06-3
Pack Size Availability Price/USD Quantity
2 mg 5 days $ 119.00
5 mg 5 days $ 197.00
25 mg 6-8 weeks $ 652.00
50 mg 6-8 weeks $ 847.00
100 mg 6-8 weeks $ 1,320.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Bay 65-1942 hydrochloride is an inhibitor of ATP-competitive and selective IKKβ.
In vitro Delivery of Bay 65-1942 prior to ischemia significantly decreases left ventricular infarct size compared with animals receiving vehicle. This ratio is significantly reduced by treatment with Bay 65-1942 at each time point (prior to ischemia 42.7±4.1%, at reperfusion 42.7±7.5%, 2 h of reperfusion 29.4±5.2%; each group P<0.05 vs. vehicle). Compared with sham animals, animals receiving vehicle have a significant increase in the infarct-to-area at risk (AAR) ratio (70.7±3.4 vs. 5.8±3.4%, P<0.05). Animals pretreated with Bay 65-1942 (n=3) have significantly attenuated CK-MB levels compared with those animals without treatment prior to IR (14,170 ±3,219 units, P<0.05 vs. vehicle)[1].
In vivo AZD6244 and BAY 65-1942 demonstrate synergistic inhibition of cell viability at the dose combination (5 μM AZD6244+10 μM BAY 65-1942), which correlates with IC75 (CI?=?0.48±0.01). AZD6244 and BAY 65-1942 treatment induces 2- and 1.3-fold caspase 3/7 activation, respectively, compared to the DMSO-treated cells. Treatment with a combination of AZD6244 plus BAY 65-1942 leads to a 3.2-fold increase in caspase 3/7 activity[2]. Inhibitors of MEK (AZD6244) and IKK (BAY 65-1942) are used at their IC50 concentrations, as determined by a 48 hour MTS assay, which achieve sufficient inhibition of kinase activity. MYL-R cells are treated for 24 hours with AZD6244 (5 μM), BAY 65-1942 (10 μM), or a combination of these inhibitors at the same concentrations. Synergism is also indicated at the IC50 (CI?=?0.56±0.09) and IC90 (CI?=?0.46±0.02) dose combinations reported by the software (CI values are the mean of three independent experiments, ± standard deviation).
Molecular Weight 431.91
Formula C22H26ClN3O4
CAS No. 600734-06-3

Storage

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

Solubility Information

DMSO: 50 mg/mL (115.76 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Inhibition of IκB kinase-β protects dopamine neurons against lipopolysaccharide-induced neurotoxicity By Zhang, Feng; Qian, Li; Flood, Patrick M.; Shi, Jing-Shan; Hong, Jau-Shyong; Gao, Hui-Ming J Pharmacol Exp Ther. 2010 June; 333(3): 822-833. 2. Cooper MJ, et al. Application of multiplexed kinase inhibitor beads to study kinome adaptations in drug-resistant leukemia. PLoS One. 2013 Jun 24;8(6):e66755.

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Keywords

Bay 65-1942 hydrochloride 600734-06-3 NF-Κb IκB/IKK Bay 651942 hydrochloride Bay 65 1942 hydrochloride Bay 65-1942 Hydrochloride inhibitor inhibit

 

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