SphK1 Inhibitor

PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC₅₀ of 2 nM and a K_i of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC₅₀ of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy.

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC₅₀ of 2 nM and a K_i of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC₅₀ of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy.

SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a K_i value of 10 μM. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity.

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

RB-042 is a SK1 and SK2 inhibitor with IC₅₀ values of 5.3 μM and 5.0 μM, respectively. RB-042 is applicable to the research of inflammatory diseases.

SphK1-IN-5 is an orally active selective inhibitor of sphingosine kinase 1 (SphK1) with an IC₅₀ of 0.87 μM and a K_i of 1.05 μM. SphK1-IN-5 directly binds to the ATP-binding pocket of SphK1 and enhances the thermal stability of this protein. SphK1-IN-5 regulates sphingolipid homeostasis: it increases sphingosine (Sph) levels and decreases sphingosine-1-phosphate (S1P) levels by inhibiting SphK1-mediated conversion of Sph to S1P. SphK1-IN-5 induces apoptosis in MC38 colon cancer cells, causes cell cycle arrest, inhibits cell migration, and exerts broad-spectrum antiproliferative effects against various tumor cells. SphK1-IN-5 exhibits antitumor activity in a mouse colon tumor model. SphK1-IN-5 can be used for research on colon cancer.

ABC294735 is an orally active SK1/SK2 inhibitor. Combination of ABC294735 with Sorafenib (HY-10201) reduces pERK. ABC294735 exhibits anticancer activity against pancreatic adenocarcinoma and renal cell carcinoma. ABC294735 can be used in research related to pancreatic adenocarcinoma and renal cell carcinoma.

SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC₅₀ concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.

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

Amgen-23 (compound 23) is a potent sphingosine kinases (SPHK) inhibitor with IC₅₀ values of 20 nM and 1.6 μM for SPHK1 and SPHK2, respectively. Amgen-23 can be used for researching anticancer.

SLM6031434 hydrochloride is the hydrochloride salt form of SLM6031434 (HY-120268). SLM6031434 is a highly selective sphingosine kinase 2 (SphK2) inhibitor with an IC₅₀ value of 0.4 μM for SphK2. SLM6031434 exerts anti-fibrotic effects by increasing sphingosine accumulation and Smad7 expression. SLM6031434 demonstrates effective anti-fibrotic efficacy in a unilateral ureteral obstruction (UUO)-induced tubulointerstitial fibrosis mouse model. SLM6031434 can be used for the study of proteinuric kidney diseases or chronic kidney disease (CKD).

SphK1&2-IN-1 is a SphK inhibitor targeting to SphK1 and SphK2. SphK1&2-IN-1 has thermal stability.

CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC₅₀ of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research.

SLP7111228 hydrochloride is a selective sphingosine kinase 1 (SphK1) inhibitor and anti-inflammatory agent. SLP7111228 hydrochloride selectively inhibits SphK1 and reduces the production of sphingosine-1-phosphate. SLP7111228 hydrochloride decreases lipopolysaccharide-induced TNFα and IL-1β levels. SLP7111228 hydrochloride alleviates obliterative pulmonary arteriopathy, increases cardiac index and decreases total pulmonary vascular resistance index. SLP7111228 hydrochloride can be used in research related to neuroinflammatory diseases and pulmonary hypertension.

PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC₅₀ of 2 nM and a K_i of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC₅₀ of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.

SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC₅₀ values of 19.81 nM and ＞10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research.

SLM6031434 is a highly selective sphingosine kinase 2 (SphK2) inhibitor with an IC₅₀ value of 0.4 μM for SphK2. SLM6031434 exerts anti-fibrotic effects by increasing sphingosine accumulation and Smad7 expression. SLM6031434 demonstrates effective anti-fibrotic efficacy in a unilateral ureteral obstruction (UUO)-induced tubulointerstitial fibrosis mouse model. SLM6031434 can be used for the study of proteinuric kidney diseases or chronic kidney disease (CKD).

SphK1-IN-4 (Compound 6b) is a sphingosine kinase 1 (SphK1) inhibitor. SphK1-IN-4 can be used for the research of cancer, such as lung cancer.

SphK1-IN-1 (compound 48) is a SphK1 inhibitor with effective antitumor activity. SphK1-IN-1 inhibits SphK1 ATPase with an IC₅₀ value of 4.02 μM. SphK1-IN-1 can be used for the research of cancer.

SLP7111228 is a selective sphingosine kinase 1 (SphK1) inhibitor and anti-inflammatory agent. SLP7111228 selectively inhibits SphK1 and reduces the production of sphingosine-1-phosphate. SLP7111228 decreases lipopolysaccharide-induced TNFα and IL-1β levels. SLP7111228 alleviates obliterative pulmonary arteriopathy, increases cardiac index and decreases total pulmonary vascular resistance index. SLP7111228 can be used in research related to neuroinflammatory diseases and pulmonary hypertension.