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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Hippo-TDI-011536
TDI-011536

Chemical Structure : TDI-011536

CAS No.: 2687970-96-1

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TDI-011536 (TDI 011536)

货号: PC-49206Not For Human Use, Lab Use Only.

TDI-011536 is a potent, ATP-competitive inhibitor of Lats kinases with IC50 of 0.76 nM (2 mM ATP) in vitro assays, prevents Yap phosphorylation in the cell-based assays with EC50 of 10 nM.

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10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TDI-011536 is a potent, ATP-competitive inhibitor of Lats kinases with IC50 of 0.76 nM (2 mM ATP) in vitro assays, prevents Yap phosphorylation in the cell-based assays with EC50 of 10 nM.
TDI-011536 (3 uM, 24h) reduced Yap phosphorylation by almost 80% on retinal organoids derived from human induced pluripotent stem cells.
TDI-011536 was significantly more potent than TRULI in stimulating Yap signaling and the proliferation of Müller glia in human retinal organoids.
TDI-011536 (200 mg/kg, i.p.) demonstrated a remarkable reduction in pYap relative to total Yap in the heart, liver, and skin in living animals, and this effect was reversible.
TDI-011536 upregulated Yap-target genes and induced proliferative effect on cardiomyocytes in vivo.

物理化学性质&存储条件

分子量 364.423
分子式 C19H16N4O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(Z)-N-(3-benzyl-4-(hydroxymethyl)thiazol-2(3H)-ylidene)-1H-pyrrolo[2,3-b]pyridine-3-carboxamide

参考文献

1. Nathaniel R Kastan, et al. Proc Natl Acad Sci U S A. 2022 Jul 12;119(28):e2206113119.

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