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Lats-IN-1

Names

[ CAS No. ]:
1424635-83-5

[ Name ]:
Lats-IN-1

[Synonym ]:
MFCD33402276
1H-Pyrrolo[2,3-b]pyridine-3-carboxamide, N-[3-(phenylmethyl)-2(3H)-thiazolylidene]-

Biological Activity

[Description]:

Lats-IN-1 is a potent and ATP-competitive inhibitor of Lats1 and Lats2 kinases. Lats-IN-1 promotes Yap-dependent proliferation in postmitotic mammalian tissues[1].

[Related Catalog]:

Research Areas >> Others
Signaling Pathways >> Others >> Others

[In Vitro]

The IC50 for Lats-IN-1 increases with the ATP concentration[1]. Lats-IN-1 (10 μM; 24 hours) interferes with the ability of Lats kinases to phosphorylate Yap, with an EC50 of 510 nM[1]. Lats-IN-1 causes Yap-dependent proliferation of murine supporting cells in the inner ear, murine cardiomyocytes, and human Müller glia in retinal organoids[1]. Lats-IN-1 fosters both the G1-S and G2-M checkpoint transitions and yields supporting cells capable of transdifferentiation[1]. Cell Proliferation Assay[1] Cell Line: MCF 10A cells Concentration: 10 μM Incubation Time: 24 hours Result: Decreased the phosphorylation of Yap at residue S127.

[References]

[1]. Nathaniel Kastan, et al. Small-molecule inhibition of Lats kinases promotes Yap-dependent proliferation in postmitotic mammalian tissues. bioRxiv 2020.02.11.944157.

Chemical & Physical Properties

[ Density]:
1.36±0.1 g/cm3

[ Molecular Formula ]:
C18H14N4OS

[ Molecular Weight ]:
334.39

Safety Information

[ Hazard Codes ]:
Xi


Related Compounds

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