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产品介绍
产品介绍
产品信息
抗原名称
TACC3,
商品描述
KHS101 is a novel inhibitor of transforming acidic coiled-coil protein 3 (TACC3). It is a selective inducer of neuronal differentiation.
分子量
339.46
纯度
≥98%
可溶性
DMSO: 60 mg/mL (176.75 mM)
In vitro(体外研究)
KHS101 increased neuronal differentiation of adherently cultured rat NPCs in a dose-dependent fashion (EC50 ∼ 1 μM). KHS101-induced neuron formation (40–60% TuJ1+ cells at 1.5–5 μM KHS101) was also observed under neurosphere-forming conditions in secondary neurospheres derived from both the hippocampus and the subventricular zone (SVZ) of adult rats . SMMC-7721 and SK-Hep-1 cells were cultured with different KHS101 concentrations (40 μM and 20 μM, respectively) to determine the IC50 values. The number and size of spheres were significantly decreased after treatment with KHS101 compared with the control (DMSO) treatment. Sphere formation was dependent on the KHS101 concentration. Bmi1, c-Myc, and Nanog were all decreased in the presence of KHS101. Compared with the control (DMSO), KHS101 decreases the expression of p-AKT, p-GSK3β and β-catenin, as well as the expression of the downstream markers c-Myc and cyclin D1 .
In vivo(体内研究)
The doses of 6 mg/kg KHS101 (i.v. and s.c.) resulted in reasonable plasma concentrations (>1.5 μM) with a plasma half-life of 1.1–1.4 h, and relative bioavailability of 69% following s.c. dosing. Most importantly, the distribution of KHS101 to the brain was extensive as demonstrated by a brain-to-plasma AUC(0–3h) ratio of ∼8 (dosing: 3 mg/kg KHS101, i.v.) .
背景
别名
KHS-101；KHS101
分子式
C18H21N5S
CAS号
1262770-73-9
制备和贮存
保存方式
Store at -20℃ for three years（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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