sphk

SphK1&2-IN-1, a sphingosine kinase inhibitor, exhibits anti-inflammatory, antitumor, and hemostatic properties.

SphK1-IN-2 is a potent and selective SphK1 inhibitor that acts on both SphK1 (IC50: 19.81 nM) and SphK2 (IC50>10 nM). sphK1-IN-2 induces cell cycle arrest and apoptosis, exhibits anti-proliferative effects, and can be used to study cancer.

SphK2-IN-1 is an SphK2 inhibitor with an IC50 value of 0.359 μM. SphK2-IN-1 can be used to study cancer, inflammation, neurological and cardiovascular diseases.

SphK1-IN-1 is an inhibitor of SphK1 with anti-tumor activity. SphK1-IN-1 inhibits the ATPase of SphK1, IC50=2.48 μM. SphK1-IN-1 has the value of cancer research.

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

SKI II (SphK-I2) is a highly selective and non-ATP-competitive S1P receptor inhibitor (IC50: 0.5 μM) while exhibiting no inhibitory action on other kinases including PKCα, PI3K, and ERK2.

K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM. K145 hydrochloride can induce apoptosis and has strong antitumor activity.

Phorbol 12-myristate 13-acetate (PMA), a member of the phorbol ester group of natural products, activates PKC, SphK, and NF-κB, and induces THP1 cell differentiation.

PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 of 2.0 nM and Ki of 3.6 nM.

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

MP-A08 is a highly selective, ATP-competitive inhibitor of sphingosine kinase (SPHK1) that targets both SphK1 and SphK2 [Ki: 6.9 ± 0.8 μM and 27 ± 3 μM, respectively].

SKI V is a potent and noncompetitive non-lipid sphingosine kinase (SPHK; SK) inhibitor (GST-hSK,IC50 : 2 μM), and is a PI3K inhibitor(hPI3k,IC50 : 6 μM), induces apoptosis and has antitumor activity

SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.

Peretinoin (NIK333) is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as RXR and RAR.

sphingosine kinase (SphK) inhibitor

RB-042 is SphK inhibitor.

Methyl caprooyl tyrosinate (MHP) is an activator of sphingosine kinase (SPHK1) and significantly stimulates CAMP mRNA and protein production in KC.

Amgen-23 (compound 23) is a potent inhibitor of sphingosine kinase, acting on SPHK1 (IC50: 20 μM) and SPHK2 (IC50: 1.6 μM), and is useful in anticancer studies.

Opaganib (ABC294640) is an orally active and specific sphingosine kinase-2 (SphK2) inhibitor (IC50: 60 μM).

SLR080811 is a SphK inhibitor. Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis, and sickle cell disease.