SPHK
Inhibitory Selectivity
SPHK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7176 |
SKI IISKI II (SphK-I2) is a highly selective and non ATP-competitive sphingosine kinase (SphK) inhibitor with IC50 of 0.5 μM, while exhibiting no inhibitory action on other kinases including PI3K, PKCα and ERK2. |
Transwell migration and invasion assays were performed. The stained cells were counted in five random fields at ×200 magnification, and the average number was taken. The average number of Control group (cells transduced with pLVX and treated with DMSO) was set as 100%, and relative migration and invasion of other groups was calculated by comparison of the cell number with the average number of control group. ***P < 0.001 versus pLVX + DMSO; ###P < 0.001 versus pLVX-p53 + DMSO.
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| S7177 |
PF-543PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 induces apoptosis, necrosis, and autophagy. |
(C) Western blot analysis of mature TGF-β1, FN and Col-I protein levels in sham, sham+ PF-543, UUO and UUO +PF-543 groups at 7 days (n =3). (average ± SEM; ANOVA; *P < 0.05, **P < 0.01 versus sham group. #P < 0.05 versus UUO group). (D) Periodic acid-Schiff staning showed that tubular atrophy was evident in the obstructed kidneys at UUO 7 days after PF-543 treatment (n =6). (E) Masson's trichrome staining showed that matrix accumulation increased in the obstructed kidneys at UUO 7 days after PF-543 treatment(n = 6). (original magnification, ×400, scale bar =50 μm).
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| S0817 |
SKI-VSKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity. |
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| S5989New |
SKI-178SKI-178 is a potent inhibitors of sphingosine kinase-1 (SphK1) and SphK2 with IC50 values ranging from ∼500 nM to ∼1 μM depending on AML cell lines. |
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| S6512 |
Defensamide (MHP)Defensamide (MHP) is an activator of sphingosine kinase (SPHK1). It can modulate the innate epidermal immune response by potentiating SPHK1 activity and inducing cAMP production. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7176 |
SKI IISKI II (SphK-I2) is a highly selective and non ATP-competitive sphingosine kinase (SphK) inhibitor with IC50 of 0.5 μM, while exhibiting no inhibitory action on other kinases including PI3K, PKCα and ERK2. |
Transwell migration and invasion assays were performed. The stained cells were counted in five random fields at ×200 magnification, and the average number was taken. The average number of Control group (cells transduced with pLVX and treated with DMSO) was set as 100%, and relative migration and invasion of other groups was calculated by comparison of the cell number with the average number of control group. ***P < 0.001 versus pLVX + DMSO; ###P < 0.001 versus pLVX-p53 + DMSO.
|
|
| S7177 |
PF-543PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 induces apoptosis, necrosis, and autophagy. |
(C) Western blot analysis of mature TGF-β1, FN and Col-I protein levels in sham, sham+ PF-543, UUO and UUO +PF-543 groups at 7 days (n =3). (average ± SEM; ANOVA; *P < 0.05, **P < 0.01 versus sham group. #P < 0.05 versus UUO group). (D) Periodic acid-Schiff staning showed that tubular atrophy was evident in the obstructed kidneys at UUO 7 days after PF-543 treatment (n =6). (E) Masson's trichrome staining showed that matrix accumulation increased in the obstructed kidneys at UUO 7 days after PF-543 treatment(n = 6). (original magnification, ×400, scale bar =50 μm).
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| S0817 |
SKI-VSKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity. |
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| S5989New |
SKI-178SKI-178 is a potent inhibitors of sphingosine kinase-1 (SphK1) and SphK2 with IC50 values ranging from ∼500 nM to ∼1 μM depending on AML cell lines. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S6512 |
Defensamide (MHP)Defensamide (MHP) is an activator of sphingosine kinase (SPHK1). It can modulate the innate epidermal immune response by potentiating SPHK1 activity and inducing cAMP production. |
