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

SK1-​I hydrochloride  (Synonyms: BML-258 hydrochloride)

Cat. No.: HY-119016A Purity: 99.49%
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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.

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

SK1-​I hydrochloride Chemical Structure

SK1-​I hydrochloride Chemical Structure

CAS No. : 2366222-05-9

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5 mg USD 350 In-stock
10 mg USD 580 In-stock
25 mg USD 1100 In-stock
50 mg USD 1700 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of SK1-​I hydrochloride:

SK1-​I hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SK1-​I hydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM[1]. 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[2].

IC50 & Target

SphK1

 

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].

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

SK1-​I hydrochloride 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 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].

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

313.86

Formula

C17H28ClNO2
CAS No.
Appearance

Liquid

Color

Colorless to light yellow

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

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (796.53 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 3.1861 mL 15.9307 mL 31.8613 mL
5 mM 0.6372 mL 3.1861 mL 6.3723 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 (sealed storage, away from moisture). 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 3.1861 mL 15.9307 mL 31.8613 mL 79.6534 mL
5 mM 0.6372 mL 3.1861 mL 6.3723 mL 15.9307 mL
10 mM 0.3186 mL 1.5931 mL 3.1861 mL 7.9653 mL
15 mM 0.2124 mL 1.0620 mL 2.1241 mL 5.3102 mL
20 mM 0.1593 mL 0.7965 mL 1.5931 mL 3.9827 mL
25 mM 0.1274 mL 0.6372 mL 1.2745 mL 3.1861 mL
30 mM 0.1062 mL 0.5310 mL 1.0620 mL 2.6551 mL
40 mM 0.0797 mL 0.3983 mL 0.7965 mL 1.9913 mL
50 mM 0.0637 mL 0.3186 mL 0.6372 mL 1.5931 mL
60 mM 0.0531 mL 0.2655 mL 0.5310 mL 1.3276 mL
80 mM 0.0398 mL 0.1991 mL 0.3983 mL 0.9957 mL
100 mM 0.0319 mL 0.1593 mL 0.3186 mL 0.7965 mL
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SK1-​I hydrochloride 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-​I2366222-05-9BML-258BML258BML 258SphKSphingosine kinasecompetitiveantitumorautophagyInhibitorinhibitorinhibit

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