2. Immunology/Inflammation
  3. SphK
  4. SK1-I

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

For research use only. We do not sell to patients.

SK1-I Chemical Structure

SK1-I Chemical Structure

CAS No. : 1072443-89-0

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Based on 1 publication(s) in Google Scholar

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SK1-I Related Antibodies

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1 Publications Citing Use of MCE SK1-I

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Description

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]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
10 μM
Compound: 7, SK1-I
Competitive inhibition of V5-His-tagged human SphK2 expressed in HEK293 cells assessed as S1P production using sphingosine and [gamma-32P]ATP as substrate by thin layer chromatography
Competitive inhibition of V5-His-tagged human SphK2 expressed in HEK293 cells assessed as S1P production using sphingosine and [gamma-32P]ATP as substrate by thin layer chromatography
[PMID: 24471412]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SK1-I Related Antibodies

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.
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].

MedChemExpress (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

277.40

Formula

C17H27NO2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (360.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6049 mL 18.0245 mL 36.0490 mL
5 mM 0.7210 mL 3.6049 mL 7.2098 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6049 mL 18.0245 mL 36.0490 mL 90.1226 mL
5 mM 0.7210 mL 3.6049 mL 7.2098 mL 18.0245 mL
10 mM 0.3605 mL 1.8025 mL 3.6049 mL 9.0123 mL
15 mM 0.2403 mL 1.2016 mL 2.4033 mL 6.0082 mL
20 mM 0.1802 mL 0.9012 mL 1.8025 mL 4.5061 mL
25 mM 0.1442 mL 0.7210 mL 1.4420 mL 3.6049 mL
30 mM 0.1202 mL 0.6008 mL 1.2016 mL 3.0041 mL
40 mM 0.0901 mL 0.4506 mL 0.9012 mL 2.2531 mL
50 mM 0.0721 mL 0.3605 mL 0.7210 mL 1.8025 mL
60 mM 0.0601 mL 0.3004 mL 0.6008 mL 1.5020 mL
80 mM 0.0451 mL 0.2253 mL 0.4506 mL 1.1265 mL
100 mM 0.0360 mL 0.1802 mL 0.3605 mL 0.9012 mL
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SK1-I Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SK1-I1072443-89-0BML-258BML258BML 258SphKSphingosine kinasecompetitiveantitumorautophagyInhibitorinhibitorinhibit

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