NCGC-6782 | LATS1/2 inhibitor | Probechem Biochemicals

Chemical Structure : NCGC-6782

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NCGC-6782 (NCGC6782)

货号: PC-28690Not For Human Use, Lab Use Only.

NCGC-6782 is a potent and selective LATS1/2 inhibitor with IC50 of 1.3 and 2.0 nM against LATS1 and LATS2 in vitro kinase assays, inhibits Hippo signaling pathway for regenerative application.

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100 mg		Get quote

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生物&药学活性

NCGC-6782 is a potent and selective LATS1/2 inhibitor with IC50 of 1.3 and 2.0 nM against LATS1 and LATS2 in vitro kinase assays, inhibits Hippo signaling pathway for regenerative application.
NCGC-6782 exhibits EC50 of 21 nM in cell-based NanoBRET readouts.
NCGC-6782 induced rapid (4 h), dose-dependent YAP1 nuclear translocation and robust transactivation of three bona-fide YAP1 target genes AMOTL2, CTGF, and CYR61 and of YAP1/TEAD-dependent transcriptional reporters.
NCGC-6782 shows>200-fold selectivity against AKT1, and about a 15-fold to 30-fold selectivity against ROCK1/2.
NCGC-6782 induces dose-dependent acceleration of wound closure in Hippo-pathway proficient NCI-H28 cells.
NCGC-6782 exhibits favorable pharmacokinetic (PK) profiles following intraperitoneal (IP), intravenous (IV), or oral (PO) dosing, leading to rapid inhibition of YAP-phosphorylation in murine liver samples.
NCGC-6782 accelerates proliferative regeneration in both cell-based and in vivo wound healing models of full-thickness excisional skin injury, significantly shortening wound-closure time without evidence of systemic toxicity.

物理化学性质&存储条件

分子量	493.58
分子式	C27H32FN5O3
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-(4-((3S,4R,5R)-1-(dimethyl-L-seryl)-4-hydroxy-3,5-dimethylpiperidin-4-yl)-3-fluoro-5-methylphenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile

参考文献

1. Tosto FA, et al. Proc Natl Acad Sci U S A. 2026 Nov 10;123(45):e2602240123.

NCGC-6782 (NCGC6782)

生物&药学活性

物理化学性质&存储条件

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NCGC-6782 (NCGC6782)

生物&药学活性

物理化学性质&存储条件

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