Proteases

SK1-IN-1 is a potent sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 58 nM.

PF-543 is a novel selective SK-1 inhibitor which inhibited SK-1 activity in a competitive manner with sphingosine.

PF-543 Citrate is a novel cell-permeant inhibitor of SphK1 with a K(i) of 3.6 nM, PF-543 is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.

SKI-II is a selective non-lipid inhibitor of sphingosine kinase (IC50 = 0.5 uM).

K145 is a selective SphK2 inhibitor with an IC50 of 4.30?? 0.06 μM , while no inhibition of SphK1 at concentrations up to 10 uM.

K145 is a selective sphingosine kinase-2 (SphK2) inhibitor and anticancer agent.

MP-A08 is a highly selective ATP competitive SK inhibitor that targets both SK1 and SK2 with Kivalues of 6.9 ±  0.8 uM and 27± 3 uM, respectively.

Peretinoin, also known as NIK-333 , orally available, acyclic retinoid with potential antineoplastic and chemopreventive activities. Peretinoin binds to and activates nuclear retinoic acid receptors (RAR), which in turn recruit coactivator proteins and promote, with other transcriptional complexes, the transcription of target genes. As a result, this agent may modulate the expression of genes involved in the regulation of cell proliferation, cell differentiation, and apoptosis of both normal and tumor cells.

MHP (Methyl caprooyl tyrosinate) is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production. MHP (Methyl caprooyl tyrosinate) enhances antimicrobial defense and innate immunity.

Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter.

SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor (IC50 = 0.1-1.8 μM). Induces CDK1-dependent apoptosis in human acute myeloid leukemia cell lines. Active in vivo.

SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK.