K145 hydrochloride
Based on 6 publication(s) in Google Scholar
K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 μM and a Ki of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.
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- Purity : 99.62%
- CAS No.: 1449240-68-9
- 화학식: C18H25ClN2O3S
- 분자량:384.92
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) K145 hydrochloride
More- Sci China Life Sci. 2022 Feb;65(2):341-361. [Abstract]
- Channels. 2020 Dec;14(1):216-230. [Abstract]
- Exp Mol Pathol. 2016 Feb;100(1):51-8. [Abstract]
- Am J Cancer Res. 2019 Mar 1;9(3):546-561. [Abstract]
- Biochem Biophys Res Commun. 2021 Sep 28;580:1-6. [Abstract]
- Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290. [Abstract]
Customer Validation & Images
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WB
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WB
Biological Activity
제품 설명
IC50 & Target
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SphK2 |
In Vitro
K145 (0-10 μM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner[1].
K145 (10 μM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells[1].
K145 (4-8 μM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt[1].
Treatment with K145 (10 μM) causes a decrease of total cellular S1P without significant effects on ceramide levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:U937 cells
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Concentration:0 µM, 4 µM, 6 µM, 8 µM, 10 µM
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Incubation Time:24 hours, 48 hours, 72 hours
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Result:Significantly inhibited the growth of U937 cells in a concentration-dependent manner.
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Cell Line:U937 cells
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Concentration:10 µM
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Incubation Time:24 hours
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Result:Significantly induced apoptosis in U937 cells.
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Cell Line:U937 cells
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Concentration:4 µM, 8 µM
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Incubation Time:3 hours
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Result:Phosphorylated ERK and Akt were decreased.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu mice injected with U937 cells[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; daily; for 15 days
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Result:Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
Chemical Information
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CAS No. 1449240-68-9
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Appearance Solid
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분자량 384.92
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화학식 C18H25ClN2O3S
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Color White to off-white
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SMILES
O=C(N(CCN)C/1=O)SC1=C/CCC2=CC=C(OCCCC)C=C2.[H]Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Sci China Life Sci
2022 Feb;65(2):341-361. PMID: 34047913 -
Channels
Sphingosine kinase 2 inhibitor ABC294640 suppresses neuronal excitability and inhibits multiple endogenously and exogenously expressed voltage-gated ion channels in cultured cells. [Abstract]2020 Dec;14(1):216-230. PMID: 32615066 -
Exp Mol Pathol
Hypoxic preconditioning protects cardiomyocytes against hypoxia/reoxygenation-induced cell apoptosis via sphingosine kinase 2 and FAK/AKT pathway. [Abstract]2016 Feb;100(1):51-8. PMID: 26621495 -
Am J Cancer Res
Targeting sphingosine kinase 2 suppresses cell growth and synergizes with BCL2/BCL-XL inhibitors through NOXA-mediated MCL1 degradation in cholangiocarcinoma. [Abstract]2019 Mar 1;9(3):546-561. PMID: 30949409
K145 hydrochloride purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2019 Mar 1;9(3):546-561. [Abstract]
Western immunoblotting analysis of NOXA protein levels in RBE and HCCC9810 cells treated with different concentrations of K145 for 24 h. Data shown represents 2 independent experiments.
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Biochem Biophys Res Commun
The alleviating effect of sphingosine kinases 2 inhibitor K145 on nonalcoholic fatty liver. [Abstract]2021 Sep 28;580:1-6. PMID: 34607257 -
Biochem Biophys Res Commun
3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione (K145) ameliorated dexamethasone induced hepatic gluconeogenesis through activation of Akt/FoxO1 pathway. [Abstract]2017 Nov 4;493(1):286-290. PMID: 28911865
K145 hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290. [Abstract]
Inhibition of pAkt by API-2 effectively prevents K145 induced increasing phosphorylation of FoxO1 in response to insulin. API-2 also significantly reverses K145 suppressed PEPCK and G6Pase mRNA and protein expression.
용액&용해도
In Vitro:
DMSO : 50 mg/mL (129.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.83 mg/mL (2.16 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.83 mg/mL (2.16 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5979 mL | 12.9897 mL | 25.9794 mL | 64.9486 mL |
| 5 mM | 0.5196 mL | 2.5979 mL | 5.1959 mL | 12.9897 mL | |
| 10 mM | 0.2598 mL | 1.2990 mL | 2.5979 mL | 6.4949 mL | |
| 15 mM | 0.1732 mL | 0.8660 mL | 1.7320 mL | 4.3299 mL | |
| 20 mM | 0.1299 mL | 0.6495 mL | 1.2990 mL | 3.2474 mL | |
| 25 mM | 0.1039 mL | 0.5196 mL | 1.0392 mL | 2.5979 mL | |
| 30 mM | 0.0866 mL | 0.4330 mL | 0.8660 mL | 2.1650 mL | |
| 40 mM | 0.0649 mL | 0.3247 mL | 0.6495 mL | 1.6237 mL | |
| 50 mM | 0.0520 mL | 0.2598 mL | 0.5196 mL | 1.2990 mL | |
| 60 mM | 0.0433 mL | 0.2165 mL | 0.4330 mL | 1.0825 mL | |
| 80 mM | 0.0325 mL | 0.1624 mL | 0.3247 mL | 0.8119 mL | |
| 100 mM | 0.0260 mL | 0.1299 mL | 0.2598 mL | 0.6495 mL |
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