SPHK

抑制剂选择性比较

SPHK产品

所有产品(6) SPHK抑制剂(5) SPHK激活剂(1)

目录号	产品描述	文献引用	实验数据
S7176	SKI II SKI II (SphK-I2)是一种高度选择性的，非ATP竞争性的sphingosine kinase (SphK)抑制剂，IC50为0.5 μM，对其他激酶，包括PI3K， PKCα和ERK2没有抑制作用。	Clin Transl Med, 2022, 12(2):e695 Cell Death Discov, 2022, 8(1):48 Elife, 2020, 9e60541	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-543 PF-543 是一种新型Sphingosine kinase 1 (SphK1， SK1) （鞘氨醇激酶）抑制剂，K_i为3.6 nM。PF-543 可诱导细胞凋亡、坏死和自噬。	Cell Res, 2022, 10.1038/s41422-022-00614-0 Cell Death Discov, 2022, 8(1):48 Molecules, 2022, 27(6)2020	(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).
S0817	SKI-V SKI V是一种非竞争性且有效的非脂质sphingosine kinase抑制剂，对GST-hSK的IC50为 2 μM。SKI-V 还抑制 PI3K，对hPI3k的 IC50 为 6 μM。SKI-V 减少促有丝分裂第二信使sphingosine-1-phosphate(S1P)的形成，并通过抗肿瘤活性诱导细胞凋亡。	Cell Death Discov, 2022, 8(1):48
S5989	SKI-178 SKI-178 是一种有效的鞘氨醇激酶-1 (SphK1) 和 SphK2 抑制剂，在急性髓细胞白血病（AML）细胞系中， IC50范围为约500 nM-1 μM。
S7174	Opaganib (ABC294640) Opaganib (ABC294640)是一种口服生物可利用的选择性sphingosine kinase-2 (SphK2)抑制剂，IC50约为 60 μM。Phase 1/2。	Cell Res, 2022, 10.1038/s41422-022-00614-0 Clin Transl Med, 2022, 12(2):e695 Front Mol Biosci, 2021, 8:598218	Macrophages treated with ABC294640 at concentrations of 0, 0.5, 1, 5, 10, 50, or 100 nM. Ratios of OD/OD (NC) are presented as means ± standard deviation. *p < 0.05 vs. NC group (1‰ DMSO).
S6512	Defensamide (MHP) Defensamide (MHP)是sphingosine kinase (SPHK1)激活剂。它可通过增强SPHK1活性、诱导cAMP生成来调节表皮免疫反应。

目录号	产品描述	文献引用	实验数据
S7176	SKI II SKI II (SphK-I2)是一种高度选择性的，非ATP竞争性的sphingosine kinase (SphK)抑制剂，IC50为0.5 μM，对其他激酶，包括PI3K， PKCα和ERK2没有抑制作用。	Clin Transl Med,2022, 12(2):e695 Cell Death Discov,2022, 8(1):48 Elife,2020, 9e60541	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-543 PF-543 是一种新型Sphingosine kinase 1 (SphK1， SK1) （鞘氨醇激酶）抑制剂，K_i为3.6 nM。PF-543 可诱导细胞凋亡、坏死和自噬。	Cell Res,2022, 10.1038/s41422-022-00614-0 Cell Death Discov,2022, 8(1):48 Molecules,2022, 27(6)2020	(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).
S0817	SKI-V SKI V是一种非竞争性且有效的非脂质sphingosine kinase抑制剂，对GST-hSK的IC50为 2 μM。SKI-V 还抑制 PI3K，对hPI3k的 IC50 为 6 μM。SKI-V 减少促有丝分裂第二信使sphingosine-1-phosphate(S1P)的形成，并通过抗肿瘤活性诱导细胞凋亡。	Cell Death Discov,2022, 8(1):48
S5989	SKI-178 SKI-178 是一种有效的鞘氨醇激酶-1 (SphK1) 和 SphK2 抑制剂，在急性髓细胞白血病（AML）细胞系中， IC50范围为约500 nM-1 μM。
S7174	Opaganib (ABC294640) Opaganib (ABC294640)是一种口服生物可利用的选择性sphingosine kinase-2 (SphK2)抑制剂，IC50约为 60 μM。Phase 1/2。	Cell Res,2022, 10.1038/s41422-022-00614-0 Clin Transl Med,2022, 12(2):e695 Front Mol Biosci,2021, 8:598218	Macrophages treated with ABC294640 at concentrations of 0, 0.5, 1, 5, 10, 50, or 100 nM. Ratios of OD/OD (NC) are presented as means ± standard deviation. *p < 0.05 vs. NC group (1‰ DMSO).

目录号

产品描述

文献引用

实验数据

S6512

Defensamide (MHP)

Defensamide (MHP)是sphingosine kinase (SPHK1)激活剂。它可通过增强SPHK1活性、诱导cAMP生成来调节表皮免疫反应。