Kinase Inhibitor of NF-ΚB-1

产品名称：

600734-06-3
KINK-1 hydrochloride
Compound A
7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido[2,3-d][1,3]oxazin-2-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
CmpdA
Bay 65-1942
Kinase Inhibitor of NF-ΚB-1

产品介绍：

产品说明

生化/生理作用

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.

基本信息

经验(实验)分子式	C₂₂H₂₅N₃O₄ · HCl
分子量	431.91
MDL编号	MFCD11040976
NACRES	NA.77

产品性质

测定	≥98% (HPLC)
形式	powder
旋光性	[α]/D -19 to -24°, c = 0.2 in DMF
储存条件	desiccated
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear
储存温度	−20℃
SMILES string	OC1=CC=CC(OCC2CC2)=C1C3=NC(NC(OC4)=O)=C4C([C@@H]5CCCNC5)=C3.Cl

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable