N-[2-(Benzoylamino)-6-benzothiazolyl]tricyclo[3.3.1.13,7]decane-1-carboxamide

Description

NVP-231 (362003-83-6) is a reversible inhibitor of ceramide kinase (IC50 = 12 nM).1 At 10 nM, it inhibited ceramide-1-phosphate formation by >50% and at 100 nM it completely inhibited its formation in cell culture. NVP-231 was inactive against hSphK1/2, hPI3Ka, hPI4Kb, hVps34, hGCS, hSMS-1, CERT, and 500-fold less potent against hDAGKa. NVP-231 inhibited breast and lung cancer cell proliferation via M phase arrest.2 It potently blocked cell migration and invasion in PANC-1 pancreatic cancer cells3 as well as MDA-MB-231 breast cancer cells4.

Uses

A ceramide kinase inhibitors that completely inhibits binding of ceramide to CerK and protects against C2-Cer-induced cell death.

storage

Store at +4°C

References

[1] CHRISTINE GRAF. Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor.[J]. Molecular Pharmacology, 2008, 74 4: 925-932. DOI:10.1124/mol.108.048652
[2] OLEKSANDR PASTUKHOV. The ceramide kinase inhibitor NVP-231 inhibits breast and lung cancer cell proliferation by inducing M phase arrest and subsequent cell death[J]. British Journal of Pharmacology, 2014, 171 24: 5829-5844. DOI:10.1111/bph.12886
[3] IO-GUANÉ RIVERA . Ceramide 1-phosphate regulates cell migration and invasion of human pancreatic cancer cells[J]. Biochemical pharmacology, 2016, 102: Pages 107-119. DOI:10.1016/j.bcp.2015.12.009
[4] STEPHANIE SCHWALM. Ceramide Kinase Is Upregulated in Metastatic Breast Cancer Cells and Contributes to Migration and Invasion by Activation of PI 3-Kinase and Akt.[J]. International Journal of Molecular Sciences, 2020, 21 4. DOI:10.3390/ijms21041396