ChemicalBook--->CAS DataBase List--->2687970-96-1

2687970-96-1

2687970-96-1 Structure

2687970-96-1 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[density ]

1.41±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[form ]

Solid
[pka]

12.30±0.40(Predicted)
[color ]

White to off-white
[InChI]

InChI=1S/C19H16N4O2S/c24-11-14-12-26-19(23(14)10-13-5-2-1-3-6-13)22-18(25)16-9-21-17-15(16)7-4-8-20-17/h1-9,12,24H,10-11H2,(H,20,21)/b22-19-
[InChIKey]

LJNPGPUDPDQGLE-QOCHGBHMSA-N
[SMILES]

C(C1C=CC=CC=1)N1C(=CS/C/1=N\C(C1=CNC2=NC=CC=C12)=O)CO
Hazard InformationBack 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
Spectrum DetailBack Directory
[Spectrum Detail]

1H-Pyrrolo[2,3-b]pyridine-3-carboxamide, N-[4-(hydroxymethyl)-3-(phenylmethyl)-2(3H)-thiazolylidene]-, [N(Z)]-(2687970-96-1)1HNMR
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