1424635-83-5
中文名稱
1H-Pyrrolo[2,3-b]pyridine-3-carboxamide, N-[3-(phenylmethyl)-2(3H)-thiazolylidene]-
英文名稱
1H-Pyrrolo[2,3-b]pyridine-3-carboxamide, N-[3-(phenylmethyl)-2(3H)-thiazolylidene]-
CAS
1424635-83-5
分子式
C18H14N4OS
分子量
334.39
MOL 文件
1424635-83-5.mol
更新日期
2024/12/26 17:36:49
1424635-83-5 結(jié)構(gòu)式
基本信息
中文別名
N-(3-芐基噻唑-2(3H)-亞基)-1H-吡咯并[2,3-B]吡啶-3-甲酰胺 英文別名
TRULILats-IN-1
Lats-IN-1(TRULI )
1H-Pyrrolo[2,3-b]pyridine-3-carboxamide, N-[3-(phenylmethyl)-2(3H)-thiazolylidene]-
物理化學(xué)性質(zhì)
密度1.36±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 83.33 mg/mL (249.20 mM)
酸度系數(shù)(pKa)12.30±0.40(Predicted)
形態(tài)固體
顏色White to light yellow
常見(jiàn)問(wèn)題列表
生物活性
Lats-IN-1 是一種高效的，ATP 競(jìng)爭(zhēng)性的 Lats1 和 Lats2 激酶抑制劑。Lats-IN-1 能促進(jìn)有絲分裂后哺乳動(dòng)物組織的 Yap 依賴性增殖。體外研究
The IC
50
for Lats-IN-1 increases with the ATP concentration.
Lats-IN-1 (10 μM; 24 hours) interferes with the ability of Lats kinases to phosphorylate Yap, with an EC
50
of 510 nM.
Lats-IN-1 causes Yap-dependent proliferation of murine supporting cells in the inner ear, murine cardiomyocytes, and human Müller glia in retinal organoids.
Lats-IN-1 fosters both the G1-S and G2-M checkpoint transitions and yields supporting cells capable of transdifferentiation.
Cell Proliferation Assay
| Cell Line: | MCF 10A cells |
| Concentration: | 10 μM |
| Incubation Time: | 24 hours |
| Result: | Decreased the phosphorylation of Yap at residue S127. |