2. Immunology/Inflammation Apoptosis
  3. SphK Apoptosis
  4. SphK1-IN-5

SphK1-IN-5 is an orally active selective inhibitor of sphingosine kinase 1 (SphK1) with an IC50 of 0.87 μM and a Ki of 1.05 μM. SphK1-IN-5 directly binds to the ATP-binding pocket of SphK1 and enhances the thermal stability of this protein. SphK1-IN-5 regulates sphingolipid homeostasis: it increases sphingosine (Sph) levels and decreases sphingosine-1-phosphate (S1P) levels by inhibiting SphK1-mediated conversion of Sph to S1P. SphK1-IN-5 induces apoptosis in MC38 colon cancer cells, causes cell cycle arrest, inhibits cell migration, and exerts broad-spectrum antiproliferative effects against various tumor cells. SphK1-IN-5 exhibits antitumor activity in a mouse colon tumor model. SphK1-IN-5 can be used for research on colon cancer.

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SphK1-IN-5

SphK1-IN-5 Chemical Structure

CAS No. : 3116900-85-4

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Description

SphK1-IN-5 is an orally active selective inhibitor of sphingosine kinase 1 (SphK1) with an IC50 of 0.87 μM and a Ki of 1.05 μM. SphK1-IN-5 directly binds to the ATP-binding pocket of SphK1 and enhances the thermal stability of this protein. SphK1-IN-5 regulates sphingolipid homeostasis: it increases sphingosine (Sph) levels and decreases sphingosine-1-phosphate (S1P) levels by inhibiting SphK1-mediated conversion of Sph to S1P. SphK1-IN-5 induces apoptosis in MC38 colon cancer cells, causes cell cycle arrest, inhibits cell migration, and exerts broad-spectrum antiproliferative effects against various tumor cells. SphK1-IN-5 exhibits antitumor activity in a mouse colon tumor model. SphK1-IN-5 can be used for research on colon cancer[1].

IC50 & Target[1]

SphK1

0.87 μM (IC50)

SphK1

1.05 μM (Ki)

In Vitro

SphK1-IN-5 (compound 9d) potently and selectively inhibits purified SphK1 with an IC50 of 0.87 μM, while it exhibits only weak activity against SphK2. It also acts as an ATP-competitive inhibitor of purified SphK1 with a Ki value of 1.05 μM, and directly binds to endogenous SphK1 in MC38 cells to enhance its thermal stability[1].
SphK1-IN-5 exhibits high specificity for SphK1, with no significant inhibitory effect on the other 27 purified kinases tested at a concentration of 10 μM[1].
SphK1-IN-5 (1-10 μM) increases Sph levels and decreases S1P levels in HepG2 cells in a dose-dependent manner by inhibiting SphK1 activity[1].
SphK1-IN-5 exhibits antiproliferative activity against HCT-116, MC38, Hepa1-6 and HepG2 tumor cells, but shows no activity against non-tumor NIH-3T3 cells or breast cancer MCF-7 cells[1].
SphK1-IN-5 (1-10 μM; 48 h) induces apoptosis in MC38 cells in a dose-dependent manner, and its activity at the concentration of 10 μM is superior to that of the reference inhibitor PF-543 (HY-15425)[1].
SphK1-IN-5 (1-10 μM; 24 h) induces G2/M and S phase cell cycle arrest in MC38 cells[1].
SphK1-IN-5 (1-10 μM; 12, 24 h) inhibits the migration of MC38 cells in a concentration- and time-dependent manner, and exhibits superior activity to PF-543 (HY-15425) at equivalent concentrations[1].

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

SphK1-IN-5 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MC38 cell
Concentration: 1, 5, 10 μM
Incubation Time: 48 h
Result: Induced apoptosis in MC38 cells in a dose-dependent manner, and its activity at the concentration of 10 μM is superior to that of the reference inhibitor PF-543.

Cell Cycle Analysis[1]

Cell Line: MC38 cell
Concentration: 1, 5, 10 μM
Incubation Time: 24 h
Result: Induced G2/M and S phase cell cycle arrest in MC38 cells.

Cell Migration Assay [1]

Cell Line: MC38 cell
Concentration: 1, 5, 10 μM
Incubation Time: 12, 24 h
Result: Inhibited the migration of MC38 cells in a concentration- and time-dependent manner, and exhibits superior activity to PF-543 (HY-15425) at equivalent concentrations.
Parmacokinetics
Species Dose Route T1/2 Cmax CL Vss Vz MRTlast AUClast F
Rat[1] 10 mg/kg i.v. 3.57 h 18.04 μg/mL 0.29 L/h/kg 0.45 L/kg 0.61 L/kg 2.46 h 81.99 μg·h/mL /
Rat[1] 20 mg/kg p.o. 4.19 h 10.80 μg/mL / / 1.34 L/kg 3.81 h 57.90 μg·h/mL 35.31 %
In Vivo

SphK1-IN-5 (compound 9d) (1 mg/kg; intravenous injection; single administration) significantly reduces serum S1P levels in healthy female C57BL/6J mice[1].
SphK1-IN-5 exhibits potent and well-tolerated antitumor activity in the mouse MC38 colon tumor model. Its efficacy as a monotherapy is comparable to that of 5-Fluorouracil (HY-90006), and its efficacy can be enhanced when used in combination with 5-Fluorouracil[1].

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

Animal Model: C57BL/6J (female, 8 weeks old)[1]
Dosage: 1 mg/kg
Administration: i.v.; single dose
Result: Significantly reduced serum S1P levels measured 2 hours post-dose.
Molecular Weight

427.86

Formula

C19H14ClN5O3S
CAS No.
SMILES

O=C(/C(C(N1)=O)=C/C2=CN(CCOC3=NC=NC(Cl)=C3)C4=C2C=CC=C4)NC1=S
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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SphK1-IN-5 Related Classifications

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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:

SphK1-IN-53116900-85-4SphKApoptosisSphingosine kinaseHCT-116Hepa1-6HepG2 cellsMC38 cellsSphK2sphingosine-1-phosphatemouse colon tumor modelsSphingosine kinase 1SphK1sphingosineInhibitorinhibitorinhibit

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