Art. -Nr.: HY-12892

SKI-178

1 Cited Publications

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SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC₅₀ concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.

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Reinheit: 99.29%
CAS. Nr.: 1259484-97-3
Formel: C₂₁H₂₂N₄O₄
Molecular Weight:394.42

Speicherung:

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

SKI-178 Chemical Structure

CAS. Nr.: 1259484-97-3

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

SphK1

SphK2

Alle SphK Isoform-spezifische Produkte anzeigen :

SphK1
SphK2

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.3 μM Compound: 20	Cytotoxicity against human A549 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human A549 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
BXPC-3	IC₅₀	0.2 μM Compound: 20	Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
HL-60	IC₅₀	0.2 μM Compound: 20	Cytotoxicity against human HL60 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human HL60 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
HL-60	IC₅₀	0.2 μM Compound: 20	Cytotoxicity against VCR-resistance human HL60 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against VCR-resistance human HL60 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
HL-60	IC₅₀	470 nM Compound: SKI-178	Cytotoxicity against human HL-60 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HL-60 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 32736077]
KG-1a	IC₅₀	0.5 μM Compound: 20	Cytotoxicity against human KG1a cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human KG1a cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
MCF7	IC₅₀	1.3 μM Compound: 20	Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
MCF7	IC₅₀	1.8 μM Compound: 20	Cytotoxicity against human tamoxifen-resistant MCF7 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human tamoxifen-resistant MCF7 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
MIA PaCa-2	IC₅₀	0.1 μM Compound: 20	Cytotoxicity against human MIAPaCa2 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human MIAPaCa2 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
NCI-H226	IC₅₀	0.3 μM Compound: 20	Cytotoxicity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
NCI-H460	IC₅₀	0.3 μM Compound: 20	Cytotoxicity against human H460 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human H460 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
PANC-1	IC₅₀	0.1 μM Compound: 20	Cytotoxicity against human PANC1 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human PANC1 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
SH-SY5Y	IC₅₀	0.3 μM Compound: 20	Cytotoxicity against human SH-SY5Y cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human SH-SY5Y cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
U-251	IC₅₀	0.5 μM Compound: 20	Cytotoxicity against human U251 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human U251 cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]
U-87MG ATCC	IC₅₀	0.6 μM Compound: 20	Cytotoxicity against human U87MG cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human U87MG cells after 48 hrs by sulforhodamine B assay	[PMID: 21050755]

In Vitro

SKI-178 (5 μM; 24 hours)-induced apoptotic cell death correlates with prolonged Bcl-2 phosphorylation^[1].

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

Apoptosis Analysis^[1]

Cell Line:

HL-60 cells
Concentration:

5 μM
Incubation Time:

24 hours
Result:

JNK activity (indicated by phosphorylation at Thr183/Tyr185) increased in a time-dependent manner starting as early as 2 hours continued to increase for at least 24 hours. There was a concomitant increase in apoptotic cell death indicated by the cleavage of caspase-7. Bcl-2 phosphorylation at Ser70 increased with time in response to SKI-178 treatment, reaching maximal levels at 8 hours, which was consistent with the timing of caspase-7 activation.

In Vivo

SKI-178 (20 mg/kg; retro-orbital injection under isoflurane anesthesia) inhibits leukemic progression in the MLL-AF9 model^[3].

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

Animal Model:

MLL-AF9 mouse model (leukemic mice)^[3]
Dosage:

20 mg/kg
Administration:

Retro-orbital injection under isoflurane anesthesia; three times per week for 1 and 3 weeks
Result:

White blood cell (WBC) counts decreased from their initial 104 cells/μL levels and continued to decline after 3 weeks of treatment until they reached normal levels (~4×103 cells/μL).

Chemical Information

CAS. Nr. 1259484-97-3
Appearance Solid
Molecular Weight 394.42
Formel C₂₁H₂₂N₄O₄
Color White to off-white
SMILES

O=C(C1=CC(C2=CC=C(OC)C=C2)=NN1)N/N=C(C3=CC=C(OC)C(OC)=C3)\C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

J Nat Med

Chaihu Guizhi Ganjiang Decoction ameliorates chronic pancreatitis by modulating the SK1/S1P signaling pathway. [Abstract]

2025 Apr 3. PMID: 40178769

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (126.77 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

2.5354 mL

12.6768 mL

25.3537 mL

5 mM

0.5071 mL

2.5354 mL

5.0707 mL

10 mM

0.2535 mL

1.2677 mL

2.5354 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: 2.5 mg/mL (6.34 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (614 KB)
- English - EN (614 KB)
- Français - FR (614 KB)
- Deutsch - DE (614 KB)
- Norwegian - NO (614 KB)
- Español - ES (614 KB)
- Swedish - SV (614 KB)
- Italian - IT (614 KB)
- Korean - KR (614 KB)
- Portuguese - PT (614 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)

Verweise

[1]. Hengst JA, et al. SKI-178: A Multitargeted Inhibitor of Sphingosine Kinase and Microtubule Dynamics Demonstrating Therapeutic Efficacy in Acute Myeloid Leukemia Models. Cancer Transl Med. 2017;3(4):109-121. [Content Brief]

[2]. Hengst JA, et al. Development of a sphingosine kinase 1 specific small-molecule inhibitor. Bioorg Med Chem Lett. 2010;20(24):7498-7502. [Content Brief]

[3]. Dick TE, et al. The apoptotic mechanism of action of the sphingosine kinase 1 selective inhibitor SKI-178 in human acute myeloid leukemia cell lines. J Pharmacol Exp Ther. 2015;352(3):494-508. [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	2.5354 mL	12.6768 mL	25.3537 mL	63.3842 mL
	5 mM	0.5071 mL	2.5354 mL	5.0707 mL	12.6768 mL
	10 mM	0.2535 mL	1.2677 mL	2.5354 mL	6.3384 mL
	15 mM	0.1690 mL	0.8451 mL	1.6902 mL	4.2256 mL
	20 mM	0.1268 mL	0.6338 mL	1.2677 mL	3.1692 mL
	25 mM	0.1014 mL	0.5071 mL	1.0141 mL	2.5354 mL
	30 mM	0.0845 mL	0.4226 mL	0.8451 mL	2.1128 mL
	40 mM	0.0634 mL	0.3169 mL	0.6338 mL	1.5846 mL
	50 mM	0.0507 mL	0.2535 mL	0.5071 mL	1.2677 mL
	60 mM	0.0423 mL	0.2113 mL	0.4226 mL	1.0564 mL
	80 mM	0.0317 mL	0.1585 mL	0.3169 mL	0.7923 mL
	100 mM	0.0254 mL	0.1268 mL	0.2535 mL	0.6338 mL

Keywords

SKI-178

1 Cited Publications

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SKI-178

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Cysteine Targeted Covalent Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SKI-178

Alle SphK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SKI-178

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Cysteine Targeted Covalent Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SKI-178

Alle SphK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SKI-178 Related Classifications

HY-12892 Related Classifications