| Identification | Back Directory | [Name]
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride | [CAS]
600734-06-3 | [Synonyms]
Bay 65-1942 HCl
KINK-1 hydrochloride
Bay 65-1942 (HCl salt)
Bay 65-1942 (hydrochloride)
KINK-1 hydrochloride >=98% (HPLC)
(S)-7-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-5-(piperidin-3-yl)-1H-pyrido[2,3-d][1,3]oxazin-2(4H)-one hydrochloride
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride
2H-Pyrido[2,3-d][1,3]oxazin-2-one,7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-,Hydrochloride(1:1) | [Molecular Formula]
C22H25N3O4.ClH | [MOL File]
600734-06-3.mol | [Molecular Weight]
431.917 |
| Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
DMSO : 50 mg/mL (115.76 mM; Need ultrasonic) | [form ]
powder | [color ]
white to beige | [optical activity]
[α]/D -19 to -24°, c = 0.2 in DMF |
| Hazard Information | Back Directory | [Uses]
Bay 65-1942 hydrochloride is an ATP-competitive and selective IKKβ inhibitor. | [Biochem/physiol Actions]
KINK-1 (Kinase Inhibitor of NF-ΚB-1; Bay 65-1942; CmpdA; Compound A) is an ATP-competitive, IKKβ-selective IΚB kinase (IKK) inhibitor (Ki against ATP = 2 nM/IKKβ and 135 nM/IKKα) that potently inhibits IKKβ-catalyzed GST-IΚBα(1–54) phosphorylation (IC50 = 4 nM, 200 nM ATP) without affecting (IC50 >10μM) IKK3 or 27 other kinases, lipases, phosphatases, caspases, and MMPs. KINK-1 effectively inhibits NF-ΚB activation and cytokines production in various human and murine cultures (IC50 from 18 to 502 nM) and is efficacious against LPS-induced plasma TNF-α production in mice and rats in vivo (EC50 = 9.1 and 6.6 mg/kg p.o., repectively) with good pharmacokinetic profile and oral availability. KINK-1 is also shown to effectively inhibit OVA-induced lung inflammation in a rat model of asthma (ED50 <0.3 mg/kg p.o.) without adverse effects to the animals. | [in vivo]
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. 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). 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). 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]. | [IC 50]
IKKβ | [storage]
Store at -20°C | [References]
[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. DOI:10.1152/ajpheart.00776.2007
[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. DOI:10.1371/journal.pone.0066755 |
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