SK1-I hydrochloride-武汉科斯坦生物科技有限公司

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SK1-I hydrochloride

英文名称：SK1-I hydrochloride

品牌：Chemstan

货号：CS-119016A

cas：2366222-05-9

价格： ￥500/mg
发布日期： 2021-03-10
更新日期： 2025-09-19

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产地
品牌	Chemstan
货号	CS-119016A
用途	科研
英文名称	SK1-I hydrochloride
包装规格	100 mg
纯度	98%%
CAS编号	2366222-05-9
别名
分子式
是否进口	否

Description

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

IC₅₀ & Target

Ki: 10 μM (SPHK1)^[1]

In Vitro

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].

MCE 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.

In Vivo

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].

MCE 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).

Molecular Weight

313.86

Formula

C??H??ClNO?

CAS No.

2366222-05-9

SMILES

OC[C@H]([C@H](/C=C/C1=CC=C(C=C1)CCCCC)O)NC.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References

[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.