SK1-I

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SK1-I

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1072443-89-0

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品名称

BML-258

产品介绍

SK1-I (BML-258) 是鞘氨醇的类似物，是同功酶特异性SPHK1竞争抑制剂，K_i值为 10 μM。SK1-I 对 SPHK2，PKCα，PKCδ，PKA，AKT1，ERK1，EGFR，CDK2，IKKβ 或 CamK2β 无活性。SK1-I 增强自噬并具有抗肿瘤活性。

生物活性

SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitiveSPHK1inhibitor with aK_ivalue of 10 μM^[1]. SK1-I shows no activity atSPHK1PKCα,PKCδ,PKA,AKT1,ERK1,EGFR,CDK2, IKKβ or CamK2β. SK1-I enhancesautophagyand has antitumor activity^[2].

IC₅₀& Target

Ki: 10 μM (SPHK1)^[1]

体外研究
(In Vitro)

SK1-I (0-10 μM; 24 hours) attenuates cancer cell growth and survival in a TP53-dependent manner in HCT116 cells and HCT116 cells bearingTP53null cancer^[2].
SK1-I (0-20 μM; 12 hours) induces more CASP3 cleavage in HCT116 cells, compared to HCT116 cells lacking TP53, leading to a hallmark of apoptosis^[2].

Cell Viability Assay^[2]

Cell Line:	HCT116 cells and HCT116 cells bearingTP53null cancer
Concentration:	0 μM, 2.5 μM, 5 μM, 7.5 μM, 10 μM
Incubation Time:	24 hours
Result:	Decreased cancer cell growth and survival.

Western Blot Analysis^[2]

Cell Line:	HCT116 cells and HCT116 cells bearingTP53null cancer
Concentration:	0 μM, 5 μM, 10 μM, 20 μM
Incubation Time:	12 hours
Result:	Induced more CASP3 cleavage in HCT116 cells, compared to HCT116 cells lacking TP53.

体内研究
(In Vivo)

Pre-treatment with SK1-I (BML-258; intraperitoneal (i.p.) injection; once; 24 hours prior to baseline mean arterial blood pressure (MAP) measurement; 75 mg/kg) before anandamide (i.v. injection; two doses; 1 and 10 mg/kg) significantly decreases the hypotensive response^[3].

Animal Model:	Male C57BL/6 mice (24 ± 3.5 g)^[3]
Dosage:	75 mg/kg
Administration:	Intraperitoneal (i.p.) injection; once; 24 hours prior to baseline MAP measurement
Result:	Significantly lowered baseline mean arterial blood pressure (MAP).

分子量

277.40

Formula

C₁₇H₂₇NO₂

CAS 号

1072443-89-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.