KY 02111

WNT signaling inhibitor CAS# 1118807-13-8

KY 02111

Catalog No. BCC3628----Order now to get a substantial discount!

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KY 02111: 5mg $35 In Stock
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Quality Control of KY 02111

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Chemical structure

KY 02111

3D structure

Chemical Properties of KY 02111

Cas No. 1118807-13-8 SDF Download SDF
PubChem ID 8582409 Appearance Powder
Formula C18H17ClN2O3S M.Wt 376.86
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 33.33 mg/mL (88.44 mM; Need ultrasonic)
Chemical Name N-(6-chloro-1,3-benzothiazol-2-yl)-3-(3,4-dimethoxyphenyl)propanamide
SMILES COC1=C(C=C(C=C1)CCC(=O)NC2=NC3=C(S2)C=C(C=C3)Cl)OC
Standard InChIKey LXFKEVQQSKQXPR-UHFFFAOYSA-N
Standard InChI 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of KY 02111

DescriptionPromotes differentiation of human ESCs and iPSCs into cardiomyocytes when used after day three in culture; differentiation efficiency increases when used after initial culture with CHIR 99021. Induces downregulation of Wnt signaling target genes; inhibits canonical Wnt signaling in a manner distinct from other known Wnt inhibitors.

KY 02111 Dilution Calculator

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KY 02111 Molarity Calculator

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Preparing Stock Solutions of KY 02111

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6535 mL 13.2675 mL 26.5351 mL 53.0701 mL 66.3376 mL
5 mM 0.5307 mL 2.6535 mL 5.307 mL 10.614 mL 13.2675 mL
10 mM 0.2654 mL 1.3268 mL 2.6535 mL 5.307 mL 6.6338 mL
50 mM 0.0531 mL 0.2654 mL 0.5307 mL 1.0614 mL 1.3268 mL
100 mM 0.0265 mL 0.1327 mL 0.2654 mL 0.5307 mL 0.6634 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on KY 02111

KY 02111 is a selective inhibitor of Wnt may by targeting the downstream from GSK3βand APC in β-catenin destruction complex [1].

Wnt signaling pathways are a group of signal transduction pathways made of proteins and play an important role in passing signals from outside of a cell through cell surface receptors to the inside of the cell. Wnt signaling initially was identified as a pivotal mediator in carcinogenesis, but has since been recognized for its function in embryonic development, including body axis patterning, cell fate specification, cell proliferation, and cell migration which are necessary for proper formation of important tissues including bone, heart, and muscle [2].

KY 02111 is a potent Wnt inhibitor and has a different selectivity with the reported Wnt inhibitors. When tested with IMR90-1 hiPSCs transfected with TCF receptor plasmids, KY 02111 (1 μM) significantly reduced luciferase activities in a dose-dependent manner by inhibiting canonical WNT signaling pathway. In cardiac colonies on the day 30, KY 02111 showed that nearly 73%-85% of IMR90-1 hiPSCs expressed the cardiac markers [1].

References:
[1].  Minami, I., et al., A small molecule that promotes cardiac differentiation of human pluripotent stem cells under defined, cytokine- and xeno-free conditions. Cell Rep, 2012. 2(5): p. 1448-60.
[2].  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.

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References on KY 02111

A new early-onset neuromuscular disorder associated with kyphoscoliosis peptidase (KY) deficiency.[Pubmed:27485408]

Eur J Hum Genet. 2016 Dec;24(12):1771-1777.

We describe a new early-onset neuromuscular disorder due to a homozygous loss-of-function variant in the kyphoscoliosis peptidase gene (KY). A 7.5-year-old girl with walking difficulties from 2 years of age presented with generalized muscle weakness; mild contractures in the shoulders, hips and feet; cavus feet; and lordosis but no scoliosis. She had previously been operated with Achilles tendon elongation. Whole-body MRI showed atrophy and fatty infiltration in the calf muscles. Biopsy of the vastus lateralis muscle showed variability in fiber size, with some internalized nuclei and numerous very small fibers with variable expression of developmental myosin heavy chain isoforms. Some small fibers showed abnormal sarcomeres with thickened Z-discs and small nemaline rods. Whole-exome sequencing revealed a homozygous one-base deletion (c.1071delG, p.(Thr358Leufs*3)) in KY, predicted to result in a truncated protein. Analysis of an RNA panel showed that KY is predominantly expressed in skeletal muscle in humans. A recessive variant in the murine ortholog Ky was previously described in a spontaneously generated mouse mutant with kyphoscoliosis, which developed postnatally and was caused by dystrophy of postural muscles. The abnormal distribution of Xin and Ky-binding partner filamin C in the muscle fibers of our patient was highly similar to their altered localization in ky/ky mouse muscle fibers. We describe the first human case of disease associated with KY inactivation. As in the mouse model, the affected child showed a neuromuscular disorder - but in contrast, no kyphoscoliosis.

A small molecule that promotes cardiac differentiation of human pluripotent stem cells under defined, cytokine- and xeno-free conditions.[Pubmed:23103164]

Cell Rep. 2012 Nov 29;2(5):1448-60.

Human pluripotent stem cells (hPSCs), including embryonic stem cells and induced pluripotent stem cells, are potentially useful in regenerative therapies for heart disease. For medical applications, clinical-grade cardiac cells must be produced from hPSCs in a defined, cost-effective manner. Cell-based screening led to the discovery of KY02111, a small molecule that promotes differentiation of hPSCs to cardiomyocytes. Although the direct target of KY02111 remains unknown, results of the present study suggest that KY02111 promotes differentiation by inhibiting WNT signaling in hPSCs but in a manner that is distinct from that of previously studied WNT inhibitors. Combined use of KY02111 and WNT signaling modulators produced robust cardiac differentiation of hPSCs in a xeno-free, defined medium, devoid of serum and any kind of recombinant cytokines and hormones, such as BMP4, Activin A, or insulin. The methodology has potential as a means for the practical production of human cardiomyocytes for regeneration therapies.

Description

KY02111 is a small molecule which can promote differentiation of hPSCs to cardiomyocytes.

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