2036044-77-4
中文名稱
Porcupine-IN-1
英文名稱
Porcupine-IN-1
CAS
2036044-77-4
分子式
C25H19FN4O
分子量
410.44
MOL 文件
2036044-77-4.mol
更新日期
2024/12/24 22:28:01
2036044-77-4 結(jié)構(gòu)式
基本信息
中文別名
化合物PORCUPINE-IN-1N-((3-氟-2'-甲基-[2,4'-聯(lián)吡啶]-5-基)甲基)-9H-咔唑-2-甲酰胺
英文別名
CS-2802PORCN-IN-1
Porcupine-IN-1
Porcn inhibitor 1
9H-Carbazole-2-carboxamide, N-[(3-fluoro-2'-methyl[2,4'-bipyridin]-5-yl)methyl]-
物理化學(xué)性質(zhì)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: slightly soluble
形態(tài)結(jié)晶固體
顏色White to off-white
常見問題列表
生物活性
Porcn-IN-1 是有效的 porcupine 抑制劑，IC50 值為 0.5±0.2 nM。靶點(diǎn)
IC50: 0.5±0.2 nM (Porcupine inhibitor)
體外研究
Porcupine is an enzyme that catalyses the addition of palmitoleate to a serine residue in Wnt proteins, a process which is required for the secretion of Wnt proteins. Porcupine-IN-1 is as potent as the clinical compound LGK974 in a cell based STF reporter gene assay. Porcn-IN-1 potently inhibits the secretion of Wnt3A, therefore is confirmed to be a porcupine inhibitor.
體內(nèi)研究
Porcn-IN-1 demonstrates moderate clearance under the treatment of human liver microsomes (57 mL/min/kg) and rat liver microsomes (24 mL/min/kg). It exhibits high clearance when treated with mouse microsomes (109 mL/min/kg).