Cat. No.: HY-119016

SK1-I

(Synonyms: BML-258)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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

Purity: 98.83%
CAS No.: 1072443-89-0
Formula: C₁₇H₂₇NO₂
Molecular Weight:277.40

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SK1-I Chemical Structure

CAS No.: 1072443-89-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a K_i 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

SphK1

All SphK Isoforms :

SphK1
SphK2

All CaMK Isoforms :

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.

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).

Chemical Information

CAS No. 1072443-89-0
Appearance Solid
Molecular Weight 277.40
Formula C₁₇H₂₇NO₂
Color Off-white to light yellow
SMILES

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

BML-258
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

Publications (1)

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Journal Impact Factor

PLoS Pathog

Enzymatic independent role of sphingosine kinase 2 in regulating the expression of type I interferon during influenza A virus infection. [Abstract]

2022 Sep 7;18(9):e1010794. PMID: 36070294

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.6049 mL

18.0245 mL

36.0490 mL

5 mM

0.7210 mL

3.6049 mL

7.2098 mL

10 mM

0.3605 mL

1.8025 mL

3.6049 mL

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

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

Mass

Concentration

Volume

Molecular Weight

Dilution Calculator

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

Concentration _(start)

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Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SK1-I

All SphK Isoforms

All CaMK Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SK1-I

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SK1-I

All SphK Isoforms

All CaMK Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SK1-I Related Classifications

Cat. No.: HY-119016