In HEK-293 cells express NUAK1 as well as NUAK2, HTH-01-015 suppresses NUAK1-mediated MYPT1 phosphorylation. HTH-01-015 suppresses cell migration In NUAK1+/+ MEFs, and inhibit U2OS cell invasion. Moreover, HTH-01-015 inhibits cell proliferation in both cell lines. HTH-01-015 inhibitors markedly restricted cells from entering into mitosis in U2OS cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||58 mg/mL warmed in DMSO|
Interplay between Polo kinase, LKB1-activated NUAK1 kinase, PP1βMYPT1 phosphatase complex and the SCFβTrCP E3 ubiquitin ligase.
Banerjee S, et al. Biochem J. 2014 Jul 15;461(2):233-45. PMID: 24785407.
Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.
Banerjee S, et al. Biochem J. 2014 Jan 1;457(1):215-25. PMID: 24171924.
|Related AMPK Products|
Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.
ETC-1002 (ESP-55016) is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule.
AICAR is an activator of AMP-activated protein kinase (AMPK), down-regulates the insulin receptor expression in HepG2 cells.
Ginkgolide C is a flavone isolated from Ginkgo biloba leaves, possessing multiple biological functions, such as decreasing platelet aggregation and ameliorating Alzheimer disease.
BML-275 (Dorsomorphin) is a cell-permeable pyrazolopyrimidine compound shown to be an AMPK inhibitor with Ki of 109 nM in cell-free assays.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.