K-252A

K-252A化学性质

熔点 :262-273℃ (decomposition) (methanol )
沸点 :685.3±55.0 °C(Predicted)
密度 :1.68
闪点 :87℃
储存条件 :-20°C
溶解度 :DMF: 1 mg/mL
酸度系数(pKa) :11.95±0.40(Predicted)
形态 :Lyophilized solid.
颜色 :White or off-white
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

安全信息

K-252A性质、用途与生产工艺

简介 K-252a 可从土壤真菌Nocardiopsis sp.中分离得到的一种十字孢碱的类似物，是蛋白激酶的抑制剂，对 PKC、PKA、II型钙调素依赖性激酶和磷酸化酶激酶的 IC50 值分别为470 nM、140 nM、270 nM和1.7 nM。K-252a 是一种有效抑制 NGF 受体 gp140trk 的酪氨酸蛋白激酶 (TRK) 活性，IC50 为 3 nM。
生物活性 K-252a 可从土壤真菌Nocardiopsis sp.中分离得到的一种十字孢碱的类似物，是蛋白激酶的抑制剂，对 PKC、PKA、II型钙调素依赖性激酶和磷酸化酶激酶的 IC50 值分别为470 nM、140 nM、270 nM和1.7 nM。K-252a 是一种有效抑制 NGF 受体 gp140trk 的酪氨酸蛋白激酶 (TRK) 活性，IC50 为 3 nM。
靶点

IC50: 470 nM (PKC), 140 nM (PKA), 270 nM (Ca ²⁺ /calmodulin-dependent kinase type II), 1.7 nM (phosphorylase kinase).

体外研究

K-252a (3-100 nM, 8d) inhibits NGF-promoted neurite outgrowth.

Western Blot Analysis.

Cell Line:	LINC00641-overexpressed cell line.
Concentration:	1.7 nM (NGF (50 ng/mL)).
Incubation Time:	6 h.
Result:	Decreased p-Akt and p-TrkB levels.

Cell Viability Assay.

Cell Line:	PC12 subclone h cells.
Concentration:	3 to 100 nM.
Incubation Time:	8 d.
Result:	Inhibited NGF-promoted neurite outgrowth.

体内研究

K252a (20 mg/kg/day) inhibiting TrkB pathway dampens the neuroprotective effects induced by TH.

Animal Model:	Mice.
Dosage:	20 mg/kg/day.
Administration:	Intraperitoneally, daily, for consecutive 5 days.
Result:	Dampened the neuroprotective effects induced by TH.