SphK Inhibitor

SphK Inhibitors (49):

Cat. No.	Product Name	Effect	Purity

HY-15425

PF-543	Inhibitor	99.85%
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.

HY-15425A

PF-543 Citrate	Inhibitor	99.47%
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.

HY-13822

SKI II	Inhibitor	99.25%
SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC₅₀ values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation.

HY-16015

Opaganib	Inhibitor	99.67%
Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with K_i of 9.8 μM.

HY-124368

RB-042	Inhibitor
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.

HY-12896

SLR080811	Inhibitor
SLR080811 is a guanidine-based selective sphingosine kinase 2 (SphK2) inhibitor with a K_i of 1.3 μM, exhibiting ~10-fold selectivity over SphK1 (K_i = 12 μM). SLR080811 reduces sphingosine 1-phosphate (S1P) levels in vitro, but drives a SphK1-dependent increase in S1P in mice. SLR080811 can be used for cancers and fibrosis research.

HY-112385

ABC294735	Inhibitor
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.

HY-15779A

K145 hydrochloride	Inhibitor	99.63%
K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC₅₀ of 4.3 μM and a K_i of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.

HY-100008

Peretinoin	Inhibitor	99.79%
Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC₅₀ of 9 μM.

HY-108491

N,N-Dimethylsphingosine	Inhibitor	99.93%
N,N-Dimethylsphingosine is a sphingosine kinase inhibitor. N,N-Dimethylsphingosine binds competitively to sphingosine kinase and blocks the conversion of sphingosine to sphingosine-1-phosphate. N,N-Dimethylsphingosine inhibits sphingosine-1-phosphate release and aggregation of platelets, and also exerts pro-apoptotic effects by resetting ceramide/sphingosine-1-phosphate homeostasis. N,N-Dimethylsphingosine can be used in cancer-related research.

HY-119016

SK1-I	Inhibitor	98.83%
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.

HY-12892

SKI-178	Inhibitor	99.29%
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.

HY-19794

MP-A08	Inhibitor	98.0%
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.

HY-101805

SK1-IN-1	Inhibitor	98.10%
SK1-IN-1 is a potent sphingosine kinase 1 (SPHK1) inhibitor with an IC₅₀ of 58 nM.

HY-162143

SKI-349	Inhibitor	99.48%
SKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells.

HY-147282

Amgen-23	Inhibitor	98.11%
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.

HY-115735

SKI-I	Inhibitor	99.73%
SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC₅₀ of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC₅₀=11 μM). SKI-I induces apoptosis in tumor cell lines.

HY-12895

SKI V	Inhibitor	98.95%
SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC₅₀ of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC₅₀ of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity.

HY-120268A

SLM6031434 hydrochloride	Inhibitor	99.1%
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).

HY-148707

SphK1&2-IN-1	Inhibitor	98.47%
SphK1&2-IN-1 is a SphK inhibitor targeting to SphK1 and SphK2. SphK1&2-IN-1 has thermal stability.

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