1H-Pyrrolo[2,3-b]pyridine-3-carboxamide, N-[4-(hydroxymethyl)-3-(phenylmethyl)-2(3H)-thiazolylidene]-, [N(Z)]-

Description

TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration^[1].

TDI-011536 (3 µM; 24 h) reduces Yap phosphorylation and (3 µM; 5 days) induces proliferation of MÜller glia in human retinal organoids^[1].

Cell Proliferation Assay^[1]

TDI-011536 (200 mg/kg; i.p.; once) provides over 4 h of Lats inhibition in the liver, heart, and skin and reduces the amount of pYap for at least 4 h after injection in all three organs^[1].
TDI-011536 (100 mg/kg; i.p.; once daily for 2 or 3 days) shows proliferative effect on cardiomyocytes^[1].

Uses

TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration[1].

in vivo

References

[1] Kastan NR, et al. Development of an improved inhibitor of Lats kinases to promote regeneration of mammalian organs. Proc Natl Acad Sci U S A. 2022 Jul 12;119(28):e2206113119. DOI:10.1073/pnas.2206113119