TCS PIM-1 1

Modify Date: 2024-01-02 19:01:12

TCS PIM-1 1 Structure
TCS PIM-1 1 structure
Common Name TCS PIM-1 1
CAS Number 491871-58-0 Molecular Weight 367.196
Density 1.6±0.1 g/cm3 Boiling Point 592.6±50.0 °C at 760 mmHg
Molecular Formula C18H11BrN2O2 Melting Point N/A
MSDS N/A Flash Point 312.2±30.1 °C

 Use of TCS PIM-1 1


TCS PIM-1 1(sc-204330) is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).IC50 value: 50 nM [1]Target: Pim-1TCS PIM-1 1 bound convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggested that 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2 (IC50 > 20 lM). Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors.

 Names

Name 6-(5-Bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydro-3-pyridine carbonitrile
Synonym More Synonyms

 TCS PIM-1 1 Biological Activity

Description TCS PIM-1 1(sc-204330) is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).IC50 value: 50 nM [1]Target: Pim-1TCS PIM-1 1 bound convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggested that 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2 (IC50 > 20 lM). Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors.
Related Catalog
References

[1]. Cheney IW, et al. Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83.

[2]. Shen Y, et al. Pim-1 inhibitor attenuates trinitrobenzene sulphonic acid induced colitis in the mice. Clin Res Hepatol Gastroenterol. 2018 Sep;42(4):382-386.

 Chemical & Physical Properties

Density 1.6±0.1 g/cm3
Boiling Point 592.6±50.0 °C at 760 mmHg
Molecular Formula C18H11BrN2O2
Molecular Weight 367.196
Flash Point 312.2±30.1 °C
Exact Mass 366.000397
PSA 77.14000
LogP 4.60
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.728
Storage condition 2-8℃

 Precursor & DownStream

Precursor  2

DownStream  0

 Synonyms

2-oxo-4-phenyl-5H-furan-3-carbonitrile
6-(5-Bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydropyridine-3-carbonitrile
TCS PIM-1 1
3-cyano-4-phenyl-2(5H)-furanone
3-Cyano-4-phenyl-2(5H)-furanon
3-Cyan-4-phenyl-2(5H)-furanon
2-oxo-4-phenyl-2,5-dihydro-furan-3-carbonitrile
2-oxo-4-phenyl-2,5-dihydro-3-furancarbonitrile
3-Pyridinecarbonitrile, 6-(5-bromo-2-hydroxyphenyl)-1,2-dihydro-2-oxo-4-phenyl-
3-cyano-4-phenyl-6-(3-bromo-6-hydroxyphenyl)-2-pyridone
3-cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone
6-(5-Bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydro-3-pyridinecarbonitrile