MI-192 是一种选择性HDAC2和HDAC3抑制剂,IC50分别为 30 nM 和 16 nM。MI-192 比其他 HDAC 异构体对 HDAC2/3 具有更高选择性。MI-192 诱导髓系白血病细胞Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)。抗癌和神经保护活性。
产品描述
MI-192 is a selective HDAC2 and HDAC3 inhibitor with IC 50 s of 30 nM and 16 nM, respectively. MI-192 is more selective for HDAC2/3 than other HDAC isomers.MI-192 induces myeloid leukaemic cells apoptosis. MI-192 has potential use in leukaemia and anti-stroke [1] [2].
体外活性
MI-192 (0.15-1 μM; 72 h) induces differentiation and is cytotoxic by promoting apoptosis in acute myeloid leukaemic cell lines U937, HL60 and Kasumi-1 [1]. Apoptosis Analysis [1] Cell Line: HL60 and Kasumi-1 cells Concentration: 150 nM, 300 nM, 500 nM, 1 μM Incubation Time: 72 h Result: Induced a substantial degree of apoptosis in both HL60 and Kasumi-1 cells.
体内活性
MI-192 (40 mg/kg; i.p; once a day; for 3 days) exhibits the neuroprotective activity in the mouse brain subjected to photothrombotic stroke [2]. Animal Model: Adult male outbred mice CD-1 (20-25 g) with photothrombotic stroke (PTS) [2] Dosage: 40 mg/kg Administration: i.p; once a day; for 3 days Result: Reduced the volume of the PTS-induced infarction core in the mouse brain, partly restored the functional symmetry in the forelimb use, decreased the level of PTS-induced apoptosis and acetylation of α-tubulin characteristic for stable microtubules, and increased the expression of GAP-43 in the cerebral cortex of the damaged hemisphere.
Cas No.
1415340-63-4
分子式
C24H21N3O2
分子量
383.44
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years