SphK

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

ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity.

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.

SKI-349 is a dual-target inhibitor of sphingosine kinase 1 and 2 (SPHK1/2) and modulates microtubule assembly (MDA). This compound exhibits significant anticancer activity, effectively reducing cell viability and invasion in liver cancer. SKI-349 also disrupts the AKT/mTOR signaling pathway, making it a valuable tool for investigating mechanisms of cancer progression and potential therapeutic strategies in oncology research.

PF-543 hydrochloride is a potent and selective inhibitor of Sphingosine Kinase 1 (SPHK1), exhibiting an IC50 of 2 nM and a Ki of 3.6 nM. It demonstrates over 100-fold selectivity for SPHK1 compared to SPHK2, making it a valuable tool for studying sphingosine-mediated signaling pathways. PF-543 hydrochloride effectively inhibits the formation of sphingosine 1-phosphate (S1P) in whole blood with an IC50 of 26.7 nM, and it has been shown to induce apoptosis, necrosis, and autophagy in various cell types, highlighting its potential in cancer and therapeutic research applications.

SphK1-IN-2 is a selective inhibitor targeting sphingosine kinase 1 (SphK1), exhibiting an IC50 value of 19.81 nM for SphK1 while demonstrating minimal inhibition of SphK2 (IC50 > 10 μM). This compound demonstrates anti-proliferative properties, induces cell cycle arrest, and promotes apoptosis in various cancer cell lines. SphK1-IN-2 is applicable in cancer research, providing insights into the role of sphingolipid metabolism in tumor progression and potential therapeutic strategies.

4α-TPA is an inactive analog of TPA, serving as a negative control in TPA-mediated experiments. This reagent is critical for distinguishing specific TPA-activated events from non-specific responses in biological assays. It aids researchers in validating experimental outcomes related to TPA signaling pathways and discerning the effects of TPA on various cellular processes.

K6PC-5 is a ceramide derivative that acts as an activator of sphingosine kinase 1 (SPHK1). This compound induces a rapid and transient increase in intracellular calcium levels, making it a valuable tool in studies related to skin diseases characterized by abnormal keratinocyte activity, as well as neurodegeneration and viral infections. Its ability to modulate cellular signaling pathways positions K6PC-5 as a significant reagent in various biological research applications.

SphK1-IN-4 is a selective inhibitor of sphingosine kinase 1 (SphK1), an enzyme involved in sphingolipid metabolism. This compound has demonstrated potent inhibitory effects on SphK1 activity, making it a valuable tool for investigating the role of sphingosine kinase in cancer biology, particularly in lung cancer research. Its application can facilitate the exploration of therapeutic strategies targeting SphK1 in various cancer models.

SK1-I is a competitive inhibitor of sphingosine kinase 1 (SPHK1) with an isozyme-specific mechanism, exhibiting a Ki value of 10 μM. This compound selectively targets SPHK1 without affecting other kinases such as PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ, or CamK2β. SK1-I is noted for its ability to enhance autophagy and exhibits potential antitumor activity, making it a valuable reagent for cancer research and studies involving lipid metabolism.

N,N-Dimethylsphingosine is a potent inhibitor of sphingosine kinase (SphK), a key enzyme involved in sphingolipid metabolism. This compound exhibits significant biological activity by modulating sphingosine-1-phosphate levels, which can influence cell proliferation, survival, and migration. It is commonly utilized in research applications related to cancer biology, neurobiology, and inflammation studies, providing insights into the roles of sphingolipids in various pathological conditions.

Amgen-23 is a selective inhibitor of sphingosine kinase 1 (SPHK1), exhibiting an IC50 value of 20 nM, while demonstrating lower potency against sphingosine kinase 2 (SPHK2) with an IC50 of 1.6 µM. This compound is valuable for investigating the role of SPHK1 in cancer biology and may facilitate the development of novel anticancer therapies. Its use in research settings can enhance the understanding of sphingolipid metabolism and cellular signaling pathways in tumorigenesis.

SphK1&2-IN-1 is a potent inhibitor of sphingosine kinases 1 and 2 (SphK1 and SphK2), key enzymes involved in sphingosine-1-phosphate biosynthesis. This compound exhibits thermal stability, making it suitable for various biochemical assays. SphK1&2-IN-1 is used in research applications focused on cancer, inflammation, and neurodegenerative diseases, providing valuable insights into sphingolipid signaling pathways.

SLM6031434 hydrochloride is a selective inhibitor of sphingosine kinase 2 (SphK2), exhibiting an IC50 of 0.4 μM. This compound is known for its anti-fibrotic properties, primarily by promoting sphingosine accumulation and enhancing Smad7 expression. Research indicates that SLM6031434 effectively reduces tubulointerstitial fibrosis in a unilateral ureteral obstruction (UUO) mouse model, making it valuable for investigations into proteinuric kidney diseases and chronic kidney disease (CKD).

SphK2-IN-1 is a selective inhibitor of sphingosine kinase 2 (SphK2), exhibiting an IC50 of 0.359 μM. This compound plays a crucial role in modulating sphingolipid metabolism, making it valuable in the study of various diseases. SphK2-IN-1 is particularly relevant for research involving cancer, inflammation, and neurological and cardiovascular disorders, providing insights into the therapeutic potential of targeting sphingosine signaling pathways.

CAY10621 is a selective inhibitor of sphingosine kinase 1 (SPHK1) with an IC50 value of 3.3 μM. This compound exhibits low cellular toxicity, making it suitable for biological studies. CAY10621 holds potential for research applications involving resistant cancer tumors, contributing to the understanding of therapeutic strategies targeting sphingosine metabolism.

SphK2-IN-2 is a potent and selective inhibitor of sphingosine kinase 2 (SphK2) with an IC50 value of 0.23 μM. This compound demonstrates significant biological activity in regulating sphingolipid metabolism, making it a valuable tool for research applications related to cancer, neurodegenerative diseases, and inflammation. SphK2-IN-2 can aid in elucidating the role of SphK2 in various cellular pathways and the pathophysiology of related disorders.

SLM6031434 is a selective inhibitor of sphingosine kinase 2 (SphK2) with an IC50 value of 0.4 μM. This compound promotes sphingosine accumulation and enhances Smad7 expression, leading to anti-fibrotic effects. SLM6031434 has demonstrated significant efficacy in reducing tubulointerstitial fibrosis in a mouse model of unilateral ureteral obstruction (UUO). It serves as a valuable tool for investigating proteinuric kidney diseases and chronic kidney disease (CKD).

SLP7111228 is an inhibitor of sphingosine kinase 1 (SphK1), a key enzyme in sphingolipid metabolism. This compound effectively reduces lipopolysaccharide (LPS)-induced production of pro-inflammatory cytokines TNFα and IL-1β. SLP7111228 is valuable for research applications related to neuroinflammatory diseases, providing insights into the modulation of inflammatory responses.

SLR080811 is a selective inhibitor of sphingosine kinase 2 (SphK2), with an inhibition constant (Ki) of 1.3 μM and approximately 10-fold selectivity over sphingosine kinase 1 (SphK1) with a Ki of 12 μM. This compound effectively reduces sphingosine 1-phosphate (S1P) levels in vitro, while also promoting a SphK1-dependent increase in S1P in in vivo mouse models. SLR080811 is suitable for research applications related to cancer and fibrosis, offering valuable insights into the role of sphingosine kinases in these disease processes.

(R)-FTY720-OMe is a selective inhibitor of sphingosine kinase 2 (SphK2), exhibiting an IC50 of 16.5 μM. This compound is valuable in research applications related to cancer, fibrosis, Alzheimer's disease, and sickle cell disease. Its ability to modulate sphingolipid metabolism makes it an important tool for studying these pathological conditions and their underlying mechanisms.

VT-ME6 is a selective inhibitor of sphingosine kinase 2 (SphK2), demonstrating a Ki value of 8 µM. This compound plays a pivotal role in the study of inflammatory diseases by modulating sphingolipid metabolism. Its specificity for SphK2 allows researchers to explore mechanisms underlying inflammation and related pathologies, making it a valuable tool for biochemical and pharmacological investigations.

Opaganib hydrochloride is a selective, competitive inhibitor of sphingosine kinase 2 (SK2) with a Ki of 9.8 μM. This compound is valuable in studying sphingosine metabolism and signaling pathways. Its biological activities make it a potential therapeutic agent in various cancer models and inflammatory diseases. Researchers can utilize Opaganib hydrochloride to investigate the role of SK2 in disease progression and to explore novel treatment strategies.