Sphingosine Kinase-2 Inhibitor, K145-Calbiochem

C₁₈H₂₄N₂O₃S

348.46

A cell permeable, orally bioavailable thiazolidine-2,4-dione derivative that acts as a selective, sphingosine competitive inhibitor of spingosine Kinase -2 (SphK2; IC₅₀ = 4.3 µM; Ki = 6.4 µM), but does not affect the activities of sphingosine kinase-1, ceremide kinase, and ceramide synthase even at high concentration (~10 micro;M). Shown to inhibit the growth of U937 human leukemic monocyte lymphoma cells by inducing apoptosis and inhibiting the phosphorylation of ERK and Akt. Blocks the growth of U937 cells in nude mice and inhibits the growth of JC tumor cells in BALB/c mice without any apparent toxicity.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell permeable, orally bioavailable thiazolidine-2,4-dione derivative that acts as a selective, sphingosine competitive inhibitor of spingosine Kinase -2 (SphK2; IC₅₀ = 4.3 µM; Ki = 6.4 µM), but does not affect the activities of sphingosine kinase-1, ceremide kinase, and ceramide synthase even at high concentration (~10 micro;M). Shown to inhibit the growth of U937 human leukemic monocyte lymphoma cells by inducing apoptosis and inhibiting the phosphorylation of ERK and Akt. Blocks the growth of U937 cells in nude mice and inhibits the growth of JC tumor cells in BALB/c mice without any apparent toxicity.

Cell permeable: yes
Primary Target
Sphk2

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

Liu, K., et al. 2013. PLos One8, e56471.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

powder

4.3 μM IC₅₀

Calbiochem^®

OK to freeze
protect from light

off-white

DMSO: 100 mg/mL
water: 2.5 mg/mL

2-8℃

Packaged under inert gas

11 - Combustible Solids

WGK 3