sphk-1

SAR-114137 is a histone sphingomyelin kinase inhibitor used in the study of molluscum arteriosum and peripheral neuropathic pain.

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.

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a selective and potent inhibitor of sphingosine kinase 1 (SPHK1) and is an efficient inhibitor of 1-phosphate sphingosine (S1P) formation. It possesses anticancer, antifibrotic, and anti-inflammatory activities and can be used in research on colorectal cancer.

SK1-IN-1 is an orally available and potent sphingosine kinase 1 (SPHK1) inhibitor (IC50: 58 nM), with potential anticancer activity, and can be used to study cancer and neurodegenerative diseases.

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].

K6PC-5 is a ceramide derivative that acts as an activator of sphingosine kinase 1 (SPHK1), inducing a swift and temporary rise in intracellular calcium levels. With its potential applications in skin diseases associated with abnormal keratinocyte function, as well as in studies on neurodegeneration and virus infection, K6PC-5 presents a promising compound for research purposes.

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.

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.

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

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.

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.

SLP9101555 is a potent and selective sphingosine kinase 2 (SphK2) inhibitor with a Ki of 90 nM.SLP9101555 has a high affinity for SphK2, which is 200-fold higher than that of SphK1.SLP9101555 dramatically reduces extracellular S1P sphingosine 1-phosphate (S1P) levels.

BML-258 HCl was removed and discontinued.

Amgen-23 is a selective and highly potent sphingosine kinase 1 (SPHK1) inhibitor that inhibits SPHK2 and can be used in anticancer research.

RB-005 is a potent sphingosine kinase isoform 1 (SK1) inhibitor, which may serve as therapeutic agent for proliferative diseases, including hypertension. RB-005, (IC(50) = 3.6 μM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.

Phorbol 12-myristate 13-acetate (PMA) is a natural phorbol ester that acts as an activator of PKC, SphK, and NF-κB, and is commonly used to induce differentiation of THP-1 cells and establish dermatitis models.

Iso-SLR 080811 is an isomer of SLR 080811, suitable for relevant research in the life sciences. SLR080811 is a selective SphK2 inhibitor (Ki=1.3 μM) that elevates blood S1P levels in wild-type mice, reduces S1P levels in sphk1 knockout mice, and leaves S1P levels unchanged in SphK2 knockout mice.

CYM5442 is an S1P agonist, targeting to Sphingosine.

N,N-Dimethylsphingosine, an endogenous metabolite, is a potent competitive sphingosine kinase (SphK) inhibitor that selectively inhibits sphingosine phosphorylation without affecting its N-acylation.DMS is elevated in models of neuropathic pain, and may mediate mechanical nociception by increasing the release of IL-1β and MCP-1.

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