SphK Inhibitor

SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC₅₀ values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation.

Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with K_i of 9.8 μM.

Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC₅₀ of 9 μM.

N,N-Dimethylsphingosine is a sphingosine kinase inhibitor. N,N-Dimethylsphingosine binds competitively to sphingosine kinase and blocks the conversion of sphingosine to sphingosine-1-phosphate. N,N-Dimethylsphingosine inhibits sphingosine-1-phosphate release and aggregation of platelets, and also exerts pro-apoptotic effects by resetting ceramide/sphingosine-1-phosphate homeostasis. N,N-Dimethylsphingosine can be used in cancer-related research.

SKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells.

SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC₅₀ of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC₅₀=11 μM). SKI-I induces apoptosis in tumor cell lines.

SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC₅₀ of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC₅₀ of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity.

SLP9101555 (compound 14c) is a potent and selective SphK2 (sphingosine kinase 2) inhibitor (K_i=90 nM) with 200-fold selectivity over SphK1. SLP9101555 markedly decreases extracellular S1P (sphingosine 1-phosphate) levels.

SphK2-IN-2 (21g) is a potent and selective SphK2 inhibitor with an IC₅₀ value of 0.23 μM.

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.

Peretinoin (Standard) is the analytical standard of Peretinoin. This product is intended for research and analytical applications. Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1[1]. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression[2]. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM[3].

SPHK2 Human Pre-designed siRNA Set A contains three designed siRNAs for SPHK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

(R)-FTY720-vinylphosphonate is a sphingosine kinase 1 (SK1) inhibitor. (R)-FTY720-ene-phosphonate is also an FTY720 analogue. (R)-FTY720-vinylphosphonate is promising for research of solid tumors like breast cancer.

Sphk1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Sphk1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

SPHK1 Human Pre-designed siRNA Set A contains three designed siRNAs for SPHK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Sphk2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sphk2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Sphk1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Sphk1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Opaganib (Standard) is the analytical standard of Opaganib. This product is intended for research and analytical applications. Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.

SK1-IN-1 (Standard) is the analytical standard of SK1-IN-1 (HY-101805). This product is intended for research and analytical applications. SK1-IN-1 is a potent sphingosine kinase 1 (SPHK1) inhibitor with an IC₅₀ of 58 nM.

SphK2-IN-3 (compound 12q) is a selective active sphingosine kinase-2 inhibitor. SphK2-IN-3 has anti-proliferative activity against various cancer cells, inducing G2 phase arrest and apoptosis in liver cancer cells HepG2.