| Identification | Back Directory | [Name]
1H-Pyrrolo[2,3-b]pyridine-3-carboxamide, N-[4-(hydroxymethyl)-3-(phenylmethyl)-2(3H)-thiazolylidene]-, [N(Z)]- | [CAS]
2687970-96-1 | [Synonyms]
TDI-011536
1H-Pyrrolo[2,3-b]pyridine-3-carboxamide, N-[4-(hydroxymethyl)-3-(phenylmethyl)-2(3H)-thiazolylidene]-, [N(Z)]- | [Molecular Formula]
C19H16N4O2S | [MOL File]
2687970-96-1.mol | [Molecular Weight]
364.42 |
| Hazard Information | Back Directory | [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]
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]. | Animal Model: | Living mice (immunoblot analysis of the heart, liver, and skin immediately after injection)[1]. | | Dosage: | 200 mg/kg | | Administration: | Intraperitoneal injections; once. | | Result: | Reduced the amount of pYap for at least 4 h after injection in all three organs and the levels returned to control values within a day. |
| Animal Model: | Male 8-week-old mice (cryolesion model)[1]. | | Dosage: | 100 mg/kg | | Administration: | Intraperitoneal injections; once daily for 2 or 3 days. | | Result: | Promoted cardiomyocytes proliferation. |
| [storage]
Store at -20°C | [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 |
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