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Cat. No.: HY-15779

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K145

6 Cited Publications

고객리뷰

Based on 6 publication(s) in Google Scholar

K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC₅₀ of 4.3 µM and a K_i of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.

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CAS No.: 1309444-75-4
화학식: C₁₈H₂₄N₂O₃S
분자량:348.46

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

K145 Chemical Structure

CAS No.: 1309444-75-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (6)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

IC50: 4.3 µM (SphK2)^[1]
Ki: 6.4 µM (SphK2)^[1]

All SphK Isoforms :

SphK1
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.

Cell Viability Assay^[1]

Cell Line:

U937 cells
Concentration:

0 µM, 4 µM, 6 µM, 8 µM, 10 µM
Incubation Time:

24 hours, 48 hours, 72 hours
Result:

Significantly inhibited the growth of U937 cells in a concentration-dependent manner.

Apoptosis Analysis^[1]

Cell Line:

U937 cells
Concentration:

10 µM
Incubation Time:

24 hours
Result:

Significantly induced apoptosis in U937 cells.

Western Blot Analysis^[1]

Cell Line:

U937 cells
Concentration:

4 µM, 8 µM
Incubation Time:

3 hours
Result:

Phosphorylated ERK and Akt were decreased.

In Vivo

K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c-nu mice injected with U937 cells^[1]
Dosage:

50 mg/kg
Administration:

Oral gavage; daily; for 15 days
Result:

Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.

Chemical Information

CAS No. 1309444-75-4
분자량 348.46
화학식 C₁₈H₂₄N₂O₃S
SMILES

O=C(N(CCN)C/1=O)SC1=C/CCC2=CC=C(OCCCC)C=C2
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (6)

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Sci China Life Sci

NPC1-regulated dynamic of clathrin-coated pits is essential for viral entry. [Abstract]

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 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.
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 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.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Liu K, et al. Biological characterization of 3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione (K145) as a selective sphingosine kinase-2 inhibitor and anticancer agent. PLoS One. 2013;8(2):e56471. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (6)
순도&문서
References

1/16
1/16

K145 purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2019 Mar 1;9(3):546-561. [Abstract]

Customer Validation
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.
1/16

K145 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290. [Abstract]

Customer Validation
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.

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K145

Publications Citing Use of MedChemExpress (MCE) K145

All SphK Isoforms