SK1-I (Synonyms: BML-258) |
カタログ番号GC61597
One-Click Copy Product Info
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スフィンゴシンの類似体である SK1-I (BML-258) は、Ki 値が 10 μM のアイソザイム特異的な競合 SPHK1 阻害剤です。 SK1-I は、SPHK1 PKCα、PKCδ、PKA、AKT1、ERK1、EGFR、CDK2、IKKβ、または CamK2β で活性を示しません。 SK1-I はオートファジーを増強し、抗腫瘍活性を持っています。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1072443-89-0
Sample solution is provided at 25 µL, 10mM.
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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].
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]. Cell Viability Assay[2] Cell Line: HCT116 cells and HCT116 cells bearing TP53 null cancer
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]
[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.
| Cas No. | 1072443-89-0 | SDF | |
| 同義語 | BML-258 | ||
| Canonical SMILES | OC[C@H]([C@H](/C=C/C1=CC=C(C=C1)CCCCC)O)NC | ||
| Formula | C17H27NO2 | M.Wt | 277.4 |
| 溶解度 | Storage | Store at -20°C | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6049 mL | 18.0245 mL | 36.049 mL |
| 5 mM | 721 μL | 3.6049 mL | 7.2098 mL |
| 10 mM | 360.5 μL | 1.8025 mL | 3.6049 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)