Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SMI-16a (PIM1/2 Kinase Inhibitor VI) , a cell-permeable thiazolidinedione compound, acts as an effective, ATP-competitive inhibitor against Pim-1/2 kinases (IC50: 150/20 nM) while exhibiting little or no activity against a panel of 57 other kinases (≤18% inhibition at 5 μM).
説明 | SMI-16a (PIM1/2 Kinase Inhibitor VI) , a cell-permeable thiazolidinedione compound, acts as an effective, ATP-competitive inhibitor against Pim-1/2 kinases (IC50: 150/20 nM) while exhibiting little or no activity against a panel of 57 other kinases (≤18% inhibition at 5 μM). |
ターゲット&IC50 | Pim1:150 nM, Pim2:20 nM |
In vitro | PIM1/2 Kinase Inhibitor VI exhibits antitumor activity in PC3 human prostate cancer cultures in vitro (IC50: 48 μM). |
In vivo | PIM1/2 Kinase Inhibitor VI exhibits antitumor activity in JC adenocarcinoma-transplanted Balb/C mice in vivo (~46% tumor mass reduction on day 20; 50 mg/kg/day, i.p.). |
キナーゼ試験 | Competition binding reactions used 25 μg human M1 CHO membrane protein, BQCA or vehicle, and 0.15 nM [3H]NMS in 96-well deep-well plates. Binding reactions (30 °C for 2-3 h) are terminated by rapid filtration. Nonspecific binding is determined by adding 10 μM atropine. Filter plates are ished 4×with ice-cold 20 mM HEPES, 100 mM NaCl, and 5 mM MgCl2, pH 7.4 using a 96-well harvester. Plates are dried and radioactivity counted with a microplate scintillation counter[1]. |
別名 | PIM1/2 Kinase Inhibitor VI |
分子量 | 263.31 |
分子式 | C13H13NO3S |
CAS No. | 587852-28-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/mL (569.67 mM)
You can also refer to dose conversion for different animals. 詳細
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SMI-16a 587852-28-6 Chromatin/Epigenetic JAK/STAT signaling Pim SMI 16a inhibit SMI16a PIM1/2 Kinase Inhibitor VI Inhibitor Pim kinases inhibitor