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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Hippo-NCGC-023
NCGC-023

Chemical Structure : NCGC-023

CAS No.: 3024011-79-5

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NCGC-023 (NCGC023, NCGC00846023)

货号: PC-27351Not For Human Use, Lab Use Only.

NCGC-023 (NCGC00846023) is a potent, selective small-molecule inhibitor of LATS1/2 with IC50 of 14.1 nM and 14.7 nM for LATS1 and LATS2, respectively, effectively activates Yap protein in vitro and in vivo.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

NCGC-023 (NCGC00846023) is a potent, selective small-molecule inhibitor of LATS1/2 with IC50 of 14.1 nM and 14.7 nM for LATS1 and LATS2, respectively, effectively activates Yap protein in vitro and in vivo.
NCGC-023 shows robust LATS1/2 inhibition in cell-based NanoBRET target-engagement assays (IC50 = 367 nM and 57 nM for LATS1 and LATS2, respectively.
caused significant induction of transcriptional targets of Yap1, including Amotl2, Ctgf, and Cyr61 in HepG2 human hepatocellular carcinoma cells.
NCGC-023 (acute intraperitoneal (IP)) markedly inhibited Yap Ser397 phosphorylation in mouse livers up to 8 hours after treatment.
NCGC-023 protects human enteroids from radiation in vitro.
NCGC-023 treatment before IR upregulated key signaling pathways controlled by LATS1/2, including Yap-dependent regenerative responses involving Il-33 and Yap-independent cellular responses to heavy metals mediated by metallothioneins.

物理化学性质&存储条件

分子量 485.62
分子式 C26H32FN3O3S
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

4-((3R,4s,5S)-4-(4-(3-fluoro-1H-pyrrolo[2,3-b]pyridin-4-yl)-2-methylphenyl)-4-hydroxy-3,5-dimethylpiperidin-1-yl)tetrahydro-2H-thiopyran 1,1-dioxide

参考文献

1. Driver LM, et al. NPJ Regen Med. 2026 Jul 20. doi: 10.1038/s41536-026-00496-5.

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