BIP-135

BIP-135 是一个高效、选择性的,ATP 竞争性的 GSK-3 抑制剂,对 GSK-3α 和 GSK-3β 作用的 IC50 值分别为 16 nM 和 21 nM。BIP 135 具有神经保护作用。

CAS号

941575-71-9

分子式

C21H13BrN2O3

主要靶点

GSK-3

仅限科研使用

Cat No : CM11602

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Synonyms



产品信息

BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor. With IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect[1].

CAS号 941575-71-9
分子式 C21H13BrN2O3
主要靶点 GSK-3
主要通路 PI3K/Akt/mTOR信号通路|干细胞
分子量 421.24
纯度 99.77%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

GSK-3α:16 nM|GSK-3β:21 nM

体内活性

BIP-135 (75 mg/kg; i.p.; daily; from postnatal day 0 to 21) prolongs the median survival time of Δ7 SMA KO mouse model of spinal muscular atrophy. And it does not appear to be toxic and was well-tolerated by the animals (no decrease in body weight)[1].

体外活性

BIP-135 (20 μM; 48 hours) is a superior neuroprotective agent in the model of oxidative stress[1]. BIP-135 (20-30 μM; 72 hours) increases the survival motor neuron (SMN) protein levels at a dose of 25 μM in human SMA fibroblasts. And the typical bell-shaped dose-response curve is observed due to some toxicity at higher concentrations[1].

溶解度

DMSO:56.7mg/mL (134.6mM),ultrasonic and warming and heat to 60°C

参考文献

1.Chen PC, et al. Identification of a Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitor, BIP-135, that Prolongs the Median Survival Time of Δ7 SMA KO Mouse Model of Spinal Muscular Atrophy. ACS Chem Neurosci. 2012 Jan 18;3(1):5-11.

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