1. Apoptosis Immunology/Inflammation
  2. Apoptosis SphK
  3. SphK2-IN-4

SphK2-IN-4 is a selective SphK2 inhibitor (IC50=6.2 μM) with extremely low activity against SphK1 (IC50 > 50 μM). SphK2-IN-4 exhibits broad-spectrum antiproliferative activity against colorectal cancer cells and induces apoptosis.

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SphK2-IN-4

SphK2-IN-4 Chemical Structure

CAS No. : 3082221-87-9

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Description

SphK2-IN-4 is a selective SphK2 inhibitor (IC50=6.2 μM) with extremely low activity against SphK1 (IC50 > 50 μM). SphK2-IN-4 exhibits broad-spectrum antiproliferative activity against colorectal cancer cells and induces apoptosis[1].

IC50 & Target

SphK2

 

In Vitro

SphK2-IN-4 (Q25) potently inhibits the proliferation of LOVO, SW480, SW620, and HT-29 human colorectal cancer cells with IC50 values ranging from 6.41 μM to 8.09 μM after 72 h of incubation[1].
SphK2-IN-4 (6 μM; 48 h) induces S-phase cell cycle arrest in SW480 human colorectal cancer cells after 48 h of treatment at 6 μM[1].
SphK2-IN-4 (3-6 μM; 48 h) dose-dependently induces apoptosis in SW480 human colorectal cancer cells[1].

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

Cell Proliferation Assay[1]

Cell Line: LOVO, SW480, SW620, HT-29 human colorectal cancer cell lines
Concentration: Serial concentrations
Incubation Time: 72 h
Result: Inhibited proliferation of LOVO cells with an IC50 of 8.09 μM.
Inhibited proliferation of SW480 cells with an IC50 of 7.77 μM.
Inhibited proliferation of SW620 cells with an IC50 of 7.38 μM.
Inhibited proliferation of HT-29 cells with an IC50 of 6.41 μM.

Cell Cycle Analysis[1]

Cell Line: SW480 human colorectal cancer cells
Concentration: 3-6 μM
Incubation Time: 48 h
Result: Significantly increased the proportion of SW480 cells in the S-phase compared to the control group at 6 μM.
Induced S-phase cell cycle arrest at 6 μM.

Apoptosis Analysis[1]

Cell Line: SW480 human colorectal cancer cells
Concentration: 3-6 μM
Incubation Time: 48 h
Result: Increased early apoptotic cells to 10.9% and late apoptotic cells to 12.2% at 6 μM, compared to 1.62% early and 0.02% late apoptotic cells in the control group.
Demonstrated dose-dependent induction of apoptosis.
Resulted in 23.1% total apoptotic cells at 6 μM after 48 h.
Molecular Weight

476.51

Formula

C21H27F3N2O5S

CAS No.
SMILES

CCCCCOC1=CC=C(CC/C=C2SC(N(CCN)C\2=O)=O)C=C1.O=C(O)C(F)(F)F

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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.

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Product Name:
SphK2-IN-4
Cat. No.:
HY-183338
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