SK1-​I hydrochloride BML-258 hydrochloride,99.49%

产品编号:Bellancom-119016A| CAS NO:2366222-05-9| 分子式:C17H28ClNO2| 分子量:313.86

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-119016A
3500.00 杭州 北京(现货)
Bellancom-119016A
5800.00 杭州 北京(现货)
Bellancom-119016A
11000.00 杭州 北京(现货)
Bellancom-119016A
17000.00 杭州 北京(现货)
Bellancom-119016A
25000.00 杭州 北京(现货)

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SK1-​I hydrochloride BML-258 hydrochloride

产品介绍 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 10 µM。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。
生物活性

SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. 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.

体外研究

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice (24 ± 3.5 g)
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).
体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice (24 ± 3.5 g)
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).
体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice (24 ± 3.5 g)
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).
性状Liquid
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (796.53 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1861 mL 15.9307 mL 31.8613 mL
5 mM 0.6372 mL 3.1861 mL 6.3723 mL
10 mM 0.3186 mL 1.5931 mL 3.1861 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.63 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.63 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.63 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

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