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KY02111 Wnt/beta-catenin inhibitor

Cat.No.S7096

KY02111 promotes differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, may act downstream of APC and GSK3β.
KY02111 Wnt/beta-catenin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 376.86

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Quality Control

Batch: S709601 DMSO]75 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.77%
99.77

Chemical Information, Storage & Stability

Molecular Weight 376.86 Formula

C18H17ClN2O3S

 Storage (From the date of receipt)
CAS No. 1118807-13-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(C=C(C=C1)CCC(=O)NC2=NC3=C(S2)C=C(C=C3)Cl)OC

Solubility

In vitro
Batch:

DMSO : 75 mg/mL ( (199.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Mechanism of Action

Features
May act downstream of APC and GSK3β in the canonical WNT signaling pathway.
Targets/IC50/Ki
Wnt [1]
In vitro
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). This compound 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. It 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. This chemical downregulates the expression of 72.7% target genes of canonical WNT signaling in IMR90-1 hiPSCs, suggesting that it inhibits canonical WNT signaling in hPSCs. It clearly reduces luciferase activities in both IMR90-1 hiPSCs and HEK293 cells in a dose-dependent manner in the TOPflash assay. This compound (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. It significantly reduces luciferase activity in the TOPflash assay in SW480 cells, whereas XAV939 and IWP-2 does not. It dramatically reduces luciferase activity induced by GSK3β inhibitor BIO in SW480 cells, compared to that of XAV939 and IWP-2. This chemical alone produces approximately 80% cTnT-positive cells, and in combination with other WNT inhibitors does not significantly increase differentiation efficiency, which shows that it effectively produces a high proportion of functional cardiomyocytes from hPSCs. [1]
References

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Signaling Pathway Map