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SMI-16a

Catalog No. T3989 CAS 587852-28-6

Synonyms: PIM1/2 Kinase Inhibitor VI

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).

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SMI-16a, CAS 587852-28-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 40.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 163.00
50 mg	In stock	$ 247.00
100 mg	In stock	$ 372.00
1 mL * 10 mM (in DMSO)	In stock	$ 84.00

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Purity: 99.78%

Biological Description

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Description	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).
Targets&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.).
Kinase Assay	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].

Synonyms	PIM1/2 Kinase Inhibitor VI
Molecular Weight	263.31
Formula	C13H13NO3S
CAS No.	587852-28-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL (569.67 mM)

References and Literature

1. Xia Z., et al. Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases. J Med Chem. 2009 Jan 8;52(1):74-86. 2. Hiasa M., et al. Pim-2 kinase is an important target of treatment for tumor progression and bone loss in myeloma. Leukemia. 2015 Jan;29(1):207-17.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Immunology/Inflammation Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Bioactive Compound Library Kinase Inhibitor Library JAK-STAT Compound Library Apoptosis Compound Library NO PAINS Compound Library Anti-Prostate Cancer Compound Library

Related Products

Related compounds with same targets

GDC-0339 TP-3654 TCS PIM-1 1 (Z)-SMI-4a SGI-1776 CX-6258 hydrochloride Hispidulin Neoprzewaquinone A

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SMI-16a 587852-28-6 Chromatin/Epigenetic JAK/STAT signaling Pim SMI 16a inhibit SMI16a PIM1/2 Kinase Inhibitor VI Inhibitor Pim kinases inhibitor

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