ARN-3236

Names

[ Name ]:
ARN-3236

[Synonym ]:
3-(2,4-DIMETHOXYPHENYL)-4-(THIOPHEN-3-YL)-1H-PYRROLO[2,3-B]PYRIDINE

Biological Activity

[Description]:

ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2) (IC50 <1 nM), with activity in inhibiting growth and enhancing paclitaxel sensitivity in cultures and xenografts of ovarian cancer cell lines[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> Salt-inducible Kinase (SIK)

[Target]

SIK2:<1 nM (IC50)

SIK1:21.63 nM (IC50)

SIK3:6.63 nM (IC50)

[References]

[1]. Lombardi MS, et al. SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J Leukoc Biol. 2016 May;99(5):711-21.

[2]. Zhou J, et al. A Novel Compound ARN-3236 Inhibits Salt-Inducible Kinase 2 and Sensitizes Ovarian Cancer Cell Lines and Xenografts to Paclitaxel. Clin Cancer Res. 2017 Apr 15;23(8):1945-1954.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₆N₂O₂S

[ Molecular Weight ]:
336.41

[ Storage condition ]:
2-8℃

Related Compounds

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