TA-01 inhibitors inhibit cardiac development when applied at 5 μM. TA-01 shows an almost complete inhibition of cardiogenesis when applied at 5 μM. TA-01 shows reduced expression of all tested mesoderm markers and the pre-cardiac marker Isl-1.
|Cell lines||Human pluripotent stemcell lines HES-3 and H7|
|Preparation method||Human pluripotent stemcell lines HES-3 and H7 were seeded at 2.5 × 106 cells/12-ULA well in BSFS medium with cell line optimized concentrations of CHIR99021 for 24 h (Supplemental Fig. S7). Thereafter the 2,4,5-trisubstituted azoles or IWP-2 or IWR-1 were added at a concentration of 5 μM (2.5 μM for IWR-1) either from 1-8 days or from 4-8 days. Dissociated EBs showed an average of 50–60% NKX2-5+ cells on day 11 when either 2,4,5-trisubstituted azoles, IWP-2 and IWR-1 were applied from 4-8 days i.e. at the post mesoderm stage. In comparison to premesoderm treatment only HES-3 showed high cardiomyocyte expansion fold with SB203580 (days 1-8) (Fig. 3A). To confirm that 2,4,5-trisubstituted azoles had no negative impact on cell viability, we analyzed the cell growth kinetics. EBs treated with IWP-2 and IWR-1 generated significantly fewer cells compared to 2,4,5-trisubstituted azoles in both cell lines (Fig. 3A). Metabolismrates of EBs measured with MTT showed an increase with TA-01 but not with IWR-1 and IWP-2 during the compound induction period.|
|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||DMSO ≥ 30 mg/mL|
EGFR, HER2 target based molecular docking analysis, in vitro screening of 2, 4, 5-trisubstituted imidazole derivatives as potential anti-oxidant and cytotoxic agents.
Guda R, et al. J Photochem Photobiol B. 2017 Nov;176:69-80. PMID: 28964888.
Cardiomyocyte differentiation of pluripotent stem cells with SB203580 analogues correlates with Wnt pathway CK1 inhibition independent of p38 MAPK signaling.
Laco F, et al. J Mol Cell Cardiol. 2015 Mar;80:56-70. PMID: 25528965.
|Related Casein Kinase Products|
LH846 is a selective inhibitor of casein kinase with IC50 values of 290 nM, 1.3 μM and 2.5 μM for CK1δ, ε and α, respectively.
SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively.
Emodin is an inhibitor of NF-κB activation and adhesion molecule expression.
TBB(NSC 231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2)with IC50s of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively).
TTP 22 is a high affinity, ATP-competitive casein kinase 2 (CK2) inhibitor with IC50/Ki of 0.1 uM/40 nM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.