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  • SK1-I hydrochloride
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SK1-I hydrochloride

SK1-I hydrochloride (BML-258 hydrochloride) 是鞘氨醇的类似物,是同功酶特异性 SPHK1 竞争抑制剂,Ki 值为 10181M。SK1-I hydrochloride 对 SPHK2,PKCα,PKCδ,PKA,AKT1,ERK1,EGFR,CDK2,IKKβ 或 CamK2β 无活性。SK1-I hydrochloride 增强自噬并具有抗肿瘤活性。

原价
¥3775-26712
价格
3020-21370
SK1-I hydrochloride的二维码

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  • 货号: ajcx32916
  • CAS: 2366222-05-9
  • 别名: BML-258 hydrochloride
  • 分子式: C17H28ClNO2
  • 分子量: 313.86
  • 纯度: >98%
  • 溶解度: DMSO : 250 mg/mL (796.53 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity[2].


SK1-I hydrochloride (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 hydrochloride (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].


Pre-treatment with SK1-I hydrochloride (BML-258 hydrochloride; 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].


[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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