SK1-I(Synonyms: BML-258)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SK1-I (Synonyms: BML-258)

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，Ki 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。

SK1-I(Synonyms: BML-258)

SK1-I Chemical Structure

CAS No. : 1072443-89-0

规格 价格 是否有货
5 mg ￥3500 询问价格 & 货期
10 mg ￥5800 询问价格 & 货期
25 mg ￥11000 询问价格 & 货期
50 mg ￥17000 询问价格 & 货期
100 mg ￥25000 询问价格 & 货期

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SK1-I 的其他形式现货产品:

SK1-​I hydrochloride

生物活性

SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. 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[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 bearing TP53 null 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: HCT116 cells and HCT116 cells bearing TP53 null 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 bearing TP53 null 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.
参考文献

  • [1]. Melissa R Pitman, et al. Inhibitors of the sphingosine kinase pathway as potential therapeutics. Curr Cancer Drug Targets. 2010 Jun;10(4):354-67.

    [2]. Santiago Lima, et al. TP53 is required for BECN1- and ATG5-dependent cell death induced by sphingosine kinase 1 inhibition. Autophagy. 2018;14(6):942-957.

    [3]. Fiona H Greig, et al. Requirement for sphingosine kinase 1 in mediating phase 1 of the hypotensive response to anandamide in the anaesthetised mouse. Eur J Pharmacol. 2019 Jan 5;842:1-9.

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