| Size | Price | Stock | Qty |
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| 25mg |
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Purity: ≥98%
KY02111 (KY 02111; KY-02111) is a potent and selective inhibitor of the Wnt signaling pathway with important biological activity. It promotes the differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, and may also act downstream of APC and GSK3β. 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.
| Targets |
The target of KY02111 is not explicitly described in the literature [1]
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| ln Vitro |
KY02111 inhibits WNT signaling in hPSCs to enhance differentiation[1]. Cardiomyocytes expressed αMHC, NKH2.5, and HCN4 are induced by KY02111[1]. In HEK293 and IMR90-1 cells, KY02111 (1–10 μM; 12 hours, 24 hours) decreases WNT signaling in a dose-dependent manner[1]. Treatment of KY02111 with WNT signaling modulators results in robust cardiac differentiation of hPSCs in a defined media free of xeno-agents and recombinant hormones and cytokines, including insulin, BMP4, and Activin A[1].
KY02111 promotes cardiac differentiation of human pluripotent stem cells (hPSCs) under defined, cytokine- and xeno-free conditions. It significantly increases the proportion of cardiac troponin T (cTnT)-positive cells (cardiomyocytes) in a dose-dependent manner. At an optimal concentration of 10 μM, the percentage of cTnT-positive cells reaches 60-70% after 14 days of differentiation, compared to 20-30% in the control group without KY02111 [1] - KY02111 upregulates the expression of cardiac-specific transcription factors and structural genes, including Nkx2-5, GATA4, and α-MHC, as determined by quantitative real-time PCR (qPCR). The mRNA levels of these markers are increased by 3-5 fold compared to the control group [1] - KY02111 does not exhibit significant cytotoxicity at concentrations up to 20 μM, as assessed by cell viability assays (MTT and trypan blue exclusion). Cell viability remains above 90% compared to the control group [1] |
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| ln Vivo |
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| Cell Assay |
Cardiac differentiation assay: hPSCs were maintained in feeder-free, xeno-free conditions and dissociated into single cells using TrypLE Express. Cells were seeded onto Matrigel-coated plates at a density of 5 × 10⁴ cells/cm² and cultured in mTeSR1 medium. After 24 hours, the medium was replaced with cardiac differentiation medium (CD1 medium) containing KY02111 at various concentrations (0-20 μM). The medium was changed every other day. On day 14, cells were fixed with 4% paraformaldehyde and stained with anti-cTnT antibody for immunocytochemistry. The percentage of cTnT-positive cells was quantified by fluorescence microscopy [1]
- qPCR analysis: Total RNA was extracted from differentiated cells using TRIzol reagent on day 14. cDNA was synthesized using a reverse transcription kit, and qPCR was performed using gene-specific primers for Nkx2-5, GATA4, α-MHC, and GAPDH (housekeeping gene). Relative gene expression levels were calculated using the 2^(-ΔΔCT) method [1] - Cell viability assay: hPSCs were treated with KY02111 at concentrations of 0-20 μM for 72 hours. Cell viability was assessed using the MTT assay and trypan blue exclusion method. The absorbance at 570 nm was measured for the MTT assay, and cell viability was calculated as a percentage relative to the control group [1] |
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| Additional Infomation |
KY02111 is a small molecule compound that can efficiently induce human pluripotent stem cells (hPSCs) to differentiate into cardiomyocytes under well-defined, cytokine-free, and xenogeneic conditions. This avoids the use of animal-derived components and exogenous cytokines, thus providing a more controllable and reproducible cardiomyocyte generation system [1]. The mechanism of action of KY02111 is not fully elucidated, but it is speculated that it may involve the regulation of intracellular signaling pathways that are crucial for cardiomyocyte lineage differentiation. It may activate key transcription factors and signaling cascades involved in early cardiac development [1]. The ability of KY02111 to promote cardiomyocyte differentiation has potential applications in regenerative medicine, drug development, and disease modeling. It provides a valuable tool for generating functional cardiomyocytes that can be used to study cardiac development, explore cardiovascular diseases, and develop cell-based therapies [1].
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| Molecular Formula |
C18H17CLN2O3S
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| Molecular Weight |
376.86
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| Exact Mass |
376.064
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| CAS # |
1118807-13-8
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| Related CAS # |
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| PubChem CID |
8582409
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.661
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| LogP |
4.37
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
456
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LXFKEVQQSKQXPR-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
N-(6-Chloro-2-benzothiazolyl)-3,4-dimethoxybenzenepropanamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6535 mL | 13.2675 mL | 26.5351 mL | |
| 5 mM | 0.5307 mL | 2.6535 mL | 5.3070 mL | |
| 10 mM | 0.2654 mL | 1.3268 mL | 2.6535 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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