ZM 449829

Names

[ Name ]:
ZM 449829

[Synonym ]:
1-(2-naphthyl)prop-2-en-1-one
1-b-Naphthylpiperazine
2-Propen-1-one, 1-(2-naphthalenyl)-
3-naphthyl piperazine
vinyl phenyl ketone
1-(2-Naphthyl)-2-propen-1-one

Biological Activity

[Description]:

ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3[1].

[Related Catalog]:

Signaling Pathways >> JAK/STAT Signaling >> JAK

Signaling Pathways >> Epigenetics >> JAK

Signaling Pathways >> Stem Cell/Wnt >> JAK

Research Areas >> Inflammation/Immunology

[Target]

JAK3:6.8 (pIC50)

[In Vitro]

ZM 449829 (compound 22) is a very weak inhibitors of EGF-R (pIC50=5.0) , Jak1 (pIC50=4.7), and tyrosine kinases Lck and CDK4 (pIC50 <5.0)[1]. ZM449829 (1 μM; 30 minutes) blocks IL-2-induced STAT5 phosphorylation[2]. Western Blot Analysis[2] Cell Line: YTS, NK92, and ex vivo NK cells Concentration: 1 μM Incubation Time: 30 minutes pretreatment Result: Inhibits the phosphorylation of STAT5.

[References]

[1]. Brown GR, et, al. Naphthyl ketones: a new class of Janus kinase 3 inhibitors. Bioorg Med Chem Lett. 2000 Mar 2010(6)575-9.

[2]. Orange JS, et, al. IL-2 induces a WAVE2-dependent pathway for actin reorganization that enables WASp-independent human NK cell function. J Clin Invest. 2011 Apr; 121(4): 1535-48.

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
319.3±15.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₃H₁₀O

[ Molecular Weight ]:
182.218

[ Flash Point ]:
137.5±15.3 °C

[ Exact Mass ]:
182.073166

[ PSA ]:
17.07000

[ LogP ]:
3.11

[ Vapour Pressure ]:
0.0±0.7 mmHg at 25°C

[ Index of Refraction ]:
1.619

Safety Information

[ HS Code ]:
2914399090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2914399090

[ Summary ]:
2914399090. other aromatic ketones without other oxygen function. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:5.5%. General tariff:30.0%