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Search Results for " sphingosine kinase "

36

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8461	SKI V	Apoptosis; PI3K; S1P Receptor	Apoptosis; GPCR/G Protein; PI3K/Akt/mTOR signaling
	SKI V 是一种非竞争性非脂质鞘氨醇激酶抑制剂，对 GST-hSK 的IC50为 2 μM。它减少有丝分裂的第二信使鞘氨醇-1-磷酸的形成，可诱导细胞凋亡并具有抗肿瘤活性。它还抑制PI3K，对 hPI3k 的IC50为 6 μM。
T4658	MHP Methyl caprooyl tyrosinate	S1P Receptor	GPCR/G Protein
	MHP (Methyl caprooyl tyrosinate) 是一种鞘氨醇激酶 (SPHK1) 激活剂，可显著增加 CAMP mRNA 和蛋白水平，还可增强抗微生物防御能力和先天免疫力。
T16128	MP-A08	S1P Receptor	GPCR/G Protein
	MP-A08 是高度选择性和 ATP 竞争性的 SPHK1 抑制剂。
T8840	PF-543 hydrochloride PF-543	Apoptosis; S1P Receptor; Autophagy; LPL Receptor	Apoptosis; Autophagy; GPCR/G Protein
	PF-543 hydrochloride (PF-543) 是一种选择性可逆和鞘氨醇竞争性SPHK1抑制剂，对SPHK1的选择性是 SPHK2 的 100 倍以上。它还是全血中 1-磷酸鞘氨醇形成的有效抑制剂，诱导细胞凋亡、坏死和自噬。
T6750	Opaganib ABC294640	S1P Receptor	GPCR/G Protein
	Opaganib (ABC294640) 是选择性和竞争性的鞘氨醇激酶 2 (SK2) 抑制剂，Ki 为 9.8 μM。
T6673	SKI II SphK-I2	Apoptosis; Wnt/beta-catenin; S1P Receptor	Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Stem Cells
	SKI II (SphK-I2) 是一种口服有效的合成鞘氨醇激酶 (SK)抑制剂，抑制 SK1 和 SK2，IC50值分别为 78 μM 和 45 μM。它通过诱导溶酶体/蛋白酶体降解，不可逆地抑制SK1。
TQ0138	K145 hydrochloride K145盐酸盐	Apoptosis; S1P Receptor	Apoptosis; GPCR/G Protein
	K145 hydrochloride 是选择性的，底物竞争性的和口服有效的SphK2抑制剂，IC50为 4.3 µM，Ki 为 6.4 µM。它可诱导细胞凋亡，显示出强大的抗肿瘤活性。
T9014	SKI-178	Apoptosis; S1P Receptor	Apoptosis; GPCR/G Protein
	SKI-178 是一种鞘氨醇激酶-1(SphK1)和 SphK2抑制剂，以 CDK1 依赖性方式诱导人急性髓性白血病细胞凋亡。
T12148	N-Desmethyltamoxifen hydrochloride	Estrogen Receptor/ERR; Endogenous Metabolite; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; Endocrinology/Hormones; Metabolism
	N-Desmethyltamoxifen hydrochloride 是 Tamoxifen 在人体内主要的三苯氧胺代谢物。它是蛋白激酶 C 抑制剂，也是人体 AML 细胞神经酰胺代谢的有效调节因子，可限制神经酰胺糖基化、水解和鞘氨醇磷酸化。
TQ0064	Peretinoin NIK333	HCV Protease; Retinoid Receptor; S1P Receptor; Autophagy	Autophagy; GPCR/G Protein; Metabolism; Microbiology/Virology; Proteases/Proteasome
	Peretinoin (NIK333) 是口服非环状类视黄醇，靶向类视黄醇核受体，结构类维生素 A 。
T12436	PF-543 Citrate Sphingosine Kinase 1 Inhibitor II Citrate	S1P Receptor	GPCR/G Protein
	PF-543 Citrate is an inhibitor of sphingosine-competitive SPHK1(IC50 of 2 nM ).
T6085	PF-543 Sphingosine Kinase 1 Inhibitor II,PF 543	Apoptosis; S1P Receptor; Autophagy; LPL Receptor	Apoptosis; Autophagy; GPCR/G Protein
	PF-543 (Sphingosine Kinase 1 Inhibitor II) 是一种选择性可逆和鞘氨醇竞争性 SPHK1抑制剂，可诱导细胞凋亡、坏死和自噬。它对 SPHK1的选择性是 SPHK2 的 100 倍以上。它还抑制全血中 1-磷酸鞘氨醇形成，IC50为 26.7 nM。
T3148	MK-571 sodium L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid	Leukotriene Receptor; LTR	GPCR/G Protein; Immunology/Inflammation
	MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂，在豚鼠和人肺膜的 Ki 分别为0.22 和 2.1 nM。
T9992	SphK1&2-IN-1	S1P Receptor	GPCR/G Protein
	SphK1&2-IN-1 是一种鞘氨醇激酶抑制剂，具有抗炎、抗肿瘤和止血作用。
T63047	SLP9101555	S1P Receptor; LPL Receptor	GPCR/G Protein
	SLP9101555 是一种有效且具有选择性的鞘氨醇激酶 2（SphK2）抑制剂，Ki 为90 nM。SLP9101555对SphK2具有很高的亲和力，是 SphK1 的 200 倍。SLP9101555 显著降低细胞外 S1P 鞘氨醇 1- 磷酸（S1P）水平。
T27710	K6PC-5 K6PC5,K6PC 5	S1P Receptor	GPCR/G Protein
	K6PC-5 is a ceramide derivative that acts as an activator of sphingosine kinase 1 (SPHK1), inducing a swift and temporary rise in intracellular calcium levels. With its potential applications in skin diseases associated with abnormal keratinocyte function, as well as in studies on neurodegeneration and virus infection, K6PC-5 presents a promising compound for research purposes.
T23045	N,N-Dimethylsphingosine	Others	Others
	sphingosine kinase (SphK) inhibitor
T70816	(R)-FTY720-OMe
	(R)-FTY720-OMe is a structural analogue of FTY720 which acts as a specific competitive inhibitor of sphingosine kinase 2 (SK2). Furthermore, (R)-FTY720-OMe does not inhibit sphingosine kinase 1 (SK1) activity.
T24803	SKI 5C SKI5C,SKI-5C
	SKI 5C is a selective inhibitor of Sphingosine Kinase 1.
T22917	L-threo-Sphingosine C-18	Others	Others
	L-threo-Sphingosine C-18 is a protein kinase C inhibitor.
T83883	Biotin Sphingosine Biotinyl Sphingosine
	Biotin sphingosine（d18:1）是一种衍生自sphingosine的生物素化合物。它被用于检测细胞裂解物中sphingosine kinase 1 (SPHK1)和SPHK2的磷酸化活性的实验中。
T24044	Erythro-sphingosine, (+)- L-Erythro-c18-sphingosine,L-Erythro-sphingosine
	Erythro-sphingosine, (+)- is a cell-permeable and reversible inhibitor of protein kinase C (IC50: 12 µM) and enhances Src kinase activity.
T70613	SLP120701 HCl
	SLP120701 is a potent and selective sphingosine kinase 2 inhibitor. 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.
T12927	SK1-IN-1	S1P Receptor	GPCR/G Protein
	SK1-IN-1 is a potent inhibitor of sphingosine kinase 1 (SPHK1)(IC50 of 58 nM).
T70071	SLM6031434 (free base)
	SLM6031434 (free base) is an inhibitor of sphingosine kinase type 2 (SphK2). It consists of pedant 1-guanidino-2-phenyloxadiazolylpyrrolidine group.
T71393	(S)-FTY-720 Vinylphosphonate
	(S)-FTY-720 Vinylphosphonate inhibits sphingosine kinase 1 and promotes its proteasomal degradation in human pulmonary artery smooth muscle, breast cancer cells, and androgen-independent prostate cancer cells.
T70614	SLR080811 HCl
	SLR080811 is a SphK inhibitor. 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.
T70900	VT-ME6
	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 (SphK...
T71301	Opaganib HCl
	ABC294640, also known as Opaganib, is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. Upon administration, ABC294640 competitively binds to and inhibits SK2, thereby preventing the phosphorylation of the pro-apoptotic amino alcohol sphingosine to sphingosine 1-phosphate (S1P), the lipid mediator that is pro-survival and critical for immunomodulation. This may eventually lead to the induction of apoptosis a...
T70704	RB-005
	RB-005 is a potent sphingosine kinase isoform 1 (SK1) inhibitor, which may serve as therapeutic agent for proliferative diseases, including hypertension. RB-005, (IC(50) = 3.6 μM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.
T35781	Sphinganine (d20:0) Sphinganine (d20:0)
	Sphinganine (d20:0) is a natural isomer of dihydro-D-erythro-sphinganine (sphinganine (d18:0); that is a precursor of ceramide and sphingosine as well as a substrate for sphingosine kinases, which generate sphingosine-1-phosphate (d18:1) . In S. cerevisiae, the amount of sphinganine (d20:0) increases 10.8-fold in response to heat stress, indicating it is involved in heat stress adaptation. Sphinganine levels increase significantly in response to certain mycotoxins, including fumonisins as well ...
T37548	azido-FTY720 azido-FTY720
	FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs. FTY720 is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5). Down-regulation of S1P1 recept...
T12148L	N-Desmethyltamoxifen	Others	Others
	N-Desmethyltamoxifen, the principal metabolite of tamoxifen in humans, serves as an efficacious modulator of ceramide metabolism within human AML cells by inhibiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. Although it demonstrates weak antiestrogenic properties, it acts as a protein kinase C (PKC) inhibitor with a potency ten times greater than that of tamoxifen.
T63132	Amgen-23
	Amgen-23 (compound 23) 是一种鞘氨醇激酶 (SPHK) 的有效抑制剂，作用于 SPHK1 (IC50: 20 μM) 和 SPHK2 (IC50: 1.6 μM)。Amgen-23 能够用于抗癌的研究。
T38946	C8 Dihydroceramide C8 Dihydroceramide
	C8 Dihydroceramide acts as a negative control for C8 Ceramide, a cell-permeable analog of natural ceramides. C8 Ceramide, also known as N-Octanoyl-D-erythro-sphingosine, exhibits potent chemotherapeutic properties and anti-proliferation effects. Additionally, it stimulates dendritic cells to enhance T cell responses during viral infections. In vitro studies have also shown that C8 Ceramide induces a slight activation of protein kinase (PKC) [4].
T62022	SKI-I
	SKI-I 是有效的、选择性的人鞘氨醇激酶 (SK) 抑制剂。SKI-I 抑制ST-hSK 的IC50值为 1.2 μM。SKI-I 也是hERK2的抑制剂(IC50=11 μM)。SKI-I 诱导肿瘤细胞系的凋亡。

化合物

Cat.No: T8461

Target: Apoptosis, PI3K, S1P Receptor

Cat.No: T4658

Synonym: Methyl caprooyl tyrosinate

Target: S1P Receptor

Cat.No: T16128

Target: S1P Receptor

PF-543 hydrochloride

Cat.No: T8840

Synonym: PF-543

Target: Apoptosis, S1P Receptor, Autophagy, LPL Receptor

Cat.No: T6750

Synonym: ABC294640

Target: S1P Receptor

Cat.No: T6673

Synonym: SphK-I2

Target: Apoptosis, Wnt/beta-catenin, S1P Receptor

K145 hydrochloride

Cat.No: TQ0138

Synonym: K145盐酸盐

Target: Apoptosis, S1P Receptor

Cat.No: T9014

Target: Apoptosis, S1P Receptor

N-Desmethyltamoxifen hydrochloride

Cat.No: T12148

Target: Estrogen Receptor/ERR, Endogenous Metabolite, PKC

Cat.No: TQ0064

Synonym: NIK333

Target: HCV Protease, Retinoid Receptor, S1P Receptor, Autophagy

Cat.No: T12436

Synonym: Sphingosine Kinase 1 Inhibitor II Citrate

Target: S1P Receptor

Cat.No: T6085

Synonym: Sphingosine Kinase 1 Inhibitor II,PF 543

Target: Apoptosis, S1P Receptor, Autophagy, LPL Receptor

Cat.No: T3148

Synonym: L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid

Target: Leukotriene Receptor, LTR

Cat.No: T9992

Target: S1P Receptor

Cat.No: T63047

Target: S1P Receptor, LPL Receptor

Cat.No: T27710

Synonym: K6PC5,K6PC 5

Target: S1P Receptor

N,N-Dimethylsphingosine

Cat.No: T23045

Target: Others

Cat.No: T70816

Cat.No: T24803

Synonym: SKI5C,SKI-5C

L-threo-Sphingosine C-18

Cat.No: T22917

Target: Others

Biotin Sphingosine

Cat.No: T83883

Synonym: Biotinyl Sphingosine

Erythro-sphingosine, (+)-

Cat.No: T24044

Synonym: L-Erythro-c18-sphingosine,L-Erythro-sphingosine

Cat.No: T70613

Cat.No: T12927

Target: S1P Receptor

SLM6031434 (free base)

Cat.No: T70071

(S)-FTY-720 Vinylphosphonate

Cat.No: T71393

Cat.No: T70614

Cat.No: T70900

Cat.No: T71301

Cat.No: T70704

Sphinganine (d20:0)

Cat.No: T35781

Synonym: Sphinganine (d20:0)

Cat.No: T37548

Synonym: azido-FTY720

N-Desmethyltamoxifen

Cat.No: T12148L

Target: Others

Cat.No: T63132

C8 Dihydroceramide

Cat.No: T38946

Synonym: C8 Dihydroceramide

Cat.No: T62022

Cat. No.	Product Name	Target	Signaling Pathways
T5891	D-ERYTHRO-SPHINGOSINE trans-4-Sphingenine,erythro-C18-Sphingosine,Erythrosphingosine,鞘氨醇,D-鞘氨醇	Phosphatase; Endogenous Metabolite; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism
	D-erythro-Sphingosine (trans-4-Sphingenine) 是一种非常有效的p32激酶活化剂，EC50为 8 μM。它也是一种PP2A 激活剂，抑制蛋白激酶 C (PKC)。
TQ0198	Phorbol 12-myristate 13-acetate 佛波醇12-十四酸酯13-乙酸酯,PMA	NF-κB; S1P Receptor; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; GPCR/G Protein; NF-κB
	Phorbol 12-myristate 13-acetate (PMA) 属于佛波酯类天然产物，是一种 PKC、SphK、NF-κB 的激活剂。Phorbol 12-myristate 13-acetate 可诱导 THP1 细胞分化。
T38262	Sphingosine (d14:1)
	Sphingosine (d14:1) is a bioactive sphingolipid that has been found in B. mori (silkworm), P. clarkii (crayfish), and A. aurita (jellyfish) extracts. It increases the germination rate of N. rileyi, an entomopathogenic fungus, with an EC50 value of 10.2 nM. Sphingosine (d14:1) inhibits protein kinase C (PKC) in vitro (IC50 = 7.3 mol%) as well as superoxide generation induced by phorbol 12-myristate 13-acetate in neutrophils and reduces growth of CHO cells (IC50s = 19 and 8 μM, respectively).

天然产物

D-ERYTHRO-SPHINGOSINE

Cat.No: T5891

Synonym: trans-4-Sphingenine,erythro-C18-Sphingosine,Erythrosphingosine,鞘氨醇,D-鞘氨醇

Target: Phosphatase, Endogenous Metabolite, PKC

Phorbol 12-myristate 13-acetate

Cat.No: TQ0198

Synonym: 佛波醇12-十四酸酯13-乙酸酯,PMA

Target: NF-κB, S1P Receptor, PKC

Sphingosine (d14:1)

Cat.No: T38262

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