sphk2

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

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.

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.

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.

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

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.

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].

K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity. K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM.

SLC4101431 is a potent SphK2 inhibitor with Ki value of 90 nM.

SLC5111312 is an inhibitor of SphK1 and SphK2.

SLM6031434 HCl is a SphK2 inhibitor with anti-fibrotic effects that reduces LPS-induced TNFα and IL-1β production and can be used to study renal fibrosis.

SK1-I hydrochloride is the salt form of SK1-I(BML-258). SK1-I is a selective and competitive sphingosine kinase 1 (SphK1) inhibitor and sphingosine analog that is inactive against SphK2 and a variety of other protein kinases, and possesses anti-leukemic potential to inhibit tumor cell growth and promote apoptosis.

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

SLM6031434 (free base) is an inhibitor of sphingosine kinase type 2 (SphK2). It consists of pedant 1-guanidino-2-phenyloxadiazolylpyrrolidine group.

VT-ME6 is a potent and selective sphingosine kinase 2 inhibitor. VT-ME6, contained a quaternary ammonium group as a warhead and established that a positively charged moiety is necessary for engaging key amino acid residues in the enzyme binding pocket.13,14 This compound is moderately potent (Ki = 8 lM) and displays three-fold selectivity for SphK2 over SphK1. 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.