Cofttek holdings limited

Wnt&Beta catenin

KY02111 (1118807-13-8)

KY02111 promotes differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, may act downstream of APC and GSK3β.

Not Intended for Therapeutic Use. For research use only.

CAS: 1118807-13-8 Category

KY02111 (1118807-13-8) Description

KY02111 is a small molecule which can promote differentiation of hPSCs to cardiomyocytes. IC50 value: Target: Wnt signaling inhibitor KY02111 Induces downregulation of Wnt signaling target genes; inhibits canonical Wnt signaling in a manner distinct from other known Wnt inhibitors. KY02111 (10 μM) increases the ratio of beating cardiac colonies as much as 70%-94% in cell aggregates of two hESC lines (KhES-1 and KhES-3), four hiPSC lines (253G1, IMR90-1, IMR90-4, and RCHIPC0003), and a mouse ESC line (R1). KY02111 (10 μM) results in 73%-85% postive IMR90-1 hiPSCs expressing the cardiac markers, cardiac troponin T (cTnT), αActinin, or NKX2.5, whereas only a few DMSO-treated cells are positive for the markers. KY02111 (10 μM) results in 16% postive IMR90-1 hiPSCs expressing the cardiac pacemaker marker, HCN4, whereas the ratio of Vimentin-positive cells (fibroblasts) decreases 3.3-fold. KY02111-induced cardiomyocytes (KY-CMs) expresses the cardiac markers, αMHC, NKH2.5, and HCN4, and that all of the ion channel genes examined are expressed at levels similar to those of adult heart tissue. KY02111 (10 μM) downregulates the expression of 72.7% target genes of canonical WNT signaling in IMR90-1 hiPSCs, suggesting that KY02111 inhibits canonical WNT signaling in hPSCs. KY02111 (10 μM) clearly reduces luciferase activities in both IMR90-1 hiPSCs and HEK293 cells in a dose-dependent manner in the TOPflash assay. KY02111 (10 μM-25 μM) increases cardiac differentiation about 80-fold in transgenic monkey ESCs compared to the control and does not show toxicity to cells even at high concentration. KY02111 (10 μM) significantly reduces luciferase activity in the TOPflash assay in SW480 cells, whereas XAV939 and IWP-2 does not. KY02111 (10 μM) dramatically reduces luciferase activity induced by GSK3β inhibitor BIO in SW480 cells, compared to that of XAV939 and IWP-2. KY02111 alone produces approximately 80% cTnT-positive cells, KY02111 in combination with other WNT inhibitors does not significantly increase differentiation efficiency, which shows that KY02111 effectively produces a high proportion of functional cardiomyocytes from hPSCs.

 

KY02111 (1118807-13-8) Specifications

Product Name KY02111
Synonyms KY02111; KY 02111; KY-02111
Chemical Names N-(6-Chloro-2-benzothiazolyl)-3,4-dimethoxybenzenepropanamide
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 1118807-13-8
Molecular Formula C18H17ClN2O3S
Molecular Weight 376.86
Monoisotopic Mass 376.065 g/mol
MDL number  
InChIKey LXFKEVQQSKQXPR-UHFFFAOYSA-N
InChi Code InChI=1S/C18H17ClN2O3S/c1-23-14-7-3-11(9-15(14)24-2)4-8-17(22)21-18-20-13-6-5-12(19)10-16(13)25-18/h3,5-7,9-10H,4,8H2,1-2H3,(H,20,21,22)
SMILES O=C(NC1=NC2=CC=C(Cl)C=C2S1)CCC3=CC=C(OC)C(OC)=C3
Form Powder
Color Pale yellow
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application A Wnt inhibitor

 


=

RIDADR NONH for all modes of transport

References:

  • 1: Morgan JT, Raghunathan VK, Chang YR, Murphy CJ, Russell P. Wnt inhibition induces persistent increases in intrinsic stiffness of human trabecular meshwork cells. Exp Eye Res. 2015 Mar;132:174-8. doi: 10.1016/j.exer.2015.01.025. Epub 2015 Jan 30. PubMed PMID: 25639201; PubMed Central PMCID: PMC4352377.
  • 2: Minami I, Yamada K, Otsuji TG, Yamamoto T, Shen Y, Otsuka S, Kadota S, Morone N, Barve M, Asai Y, Tenkova-Heuser T, Heuser JE, Uesugi M, Aiba K, Nakatsuji N. A small molecule that promotes cardiac differentiation of human pluripotent stem cells under defined, cytokine- and xeno-free conditions. Cell Rep. 2012 Nov 29;2(5):1448-60. doi: 10.1016/j.celrep.2012.09.015. Epub 2012 Oct 25. PubMed PMID: 23103164.
  • 3: Stamatakou, E., M. Hoyos-Flight, and P.C. Salinas, Wnt Signalling Promotes Actin Dynamics during Axon Remodelling through the Actin-Binding Protein Eps8. PLoS One, 2015. 10(8): p. e0134976.
  • 4: Wnt inhibition induces persistent increases in intrinsic stiffness of human trabecular meshwork cells. Morgan JT, Raghunathan VK, Chang YR, Murphy CJ, Russell P. Exp Eye Res. 2015 Mar;132:174-8. doi: 10.1016/j.exer.2015.01.025. Epub 2015 Jan 30.

1 review for KY02111 (1118807-13-8)

  1. Cofttek

    Never had such good experience before,The KY02111 (1118807-13-8) is high purity,also customer service is pretty nice !gotta try!!

Add a review

Your email address will not be published. Required fields are marked *