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

SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC50 values of 19.81 nM and ＞10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research.

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

SphK1-IN-2 Chemical Structure

SphK1-IN-2 Chemical Structure

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SphK1-IN-2 Related Antibodies

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Description

SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC50 values of 19.81 nM and ＞10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research[1].

IC50 & Target[1]

SphK1

19.81 nM (IC50)

SphK2

＞10 μM (IC50)

In Vitro

SphK1-IN-2 (4-24 μM; 72 hours; cancer cell lines) has anti-proliferative activity on cancer cells[1].
SphK1-IN-2 (10-30 μM; 48 hours; HT-29 cells and MDA-MB-231 cells) induces G0/G1 phase arrest and apoptosis in colon cancer cells[1].

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

SphK1-IN-2 Related Antibodies

Cell Viability Assay[1]

Cell Line: HT-29, SW480, MDA-MB231 and MCF-7 cells
Concentration: 4-24 μM
Incubation Time: 72 hours
Result: Had inhibitory activity against HT-29 and MDA-MB-231 with IC50 of 3.85 and 7.14 μM, respectively.

Cell Cycle Analysis[1]

Cell Line: HT-29 cells and MDA-MB-231 cells
Concentration: 10 and 30 μM
Incubation Time: 72 hours
Result: Arrestd cell cycle at G0/G1 phase and reduced the expression of cyclin A, cyclin E1, cyclin D1, and CDK6.

Apoptosis Analysis[1]

Cell Line: HT-29 cells and MDA-MB-231 cells
Concentration: 10 and 30 μM
Incubation Time: 48 hours
Result: Induced cell apoptosis in a dose-dependent manner.
In Vivo

SphK1-IN-2 (50-100 mg/kg; i.p.; daily; for 14 days; female BALB/c nude mice) inhibits the growth of colon tumors and breast tumors in vivo[1].
SphK1-IN-2 (2-50 mg/kg; p.o., i.p. and i.v.; female BALB/c nude mice) exhibits a long half-life (T1/2=8.13 h) and high plasma exposure (AUClast = 8061 h*ng/mL)[1].

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

Animal Model: Female BALB/c nude mice[1]
Dosage: 2, 20 and 50 mg/kg(Pharmacokinetic Analysis)
Administration: Oral administration, intraperitoneal injection and intravenous injection
Result: 1.19
admin. p.o. i.p. i.v.
Tmax (min) 0.83 0.18
Cmax (ng/mL) 171 78582
AUClast (h*ng/mL) 242 8061 408
T1/2 (h) 8.13 4.20 2.23
CL_obs (mL/min/kg) 81.10
F (%) 2.38 79.00
Animal Model: Female BALB/c nude mice[1]
Dosage: 50 and 100 mg/kg
Administration: Intraperitoneal injection; daily; for 14 days
Result: Inhibited the growth of HT29 tumors at a dose of 50 mg/kg and inhibited the growth of MDA-MB-231 breast tumors in a dose-dependent manner.
Molecular Weight

544.50

Formula

C27H30BrNO4S
SMILES

OC[C@@H]1N(CC2=CC=C(COC3=CC(CS(=O)(C4=CC=CC=C4)=O)=C(Br)C(C)=C3)C=C2)CCC1
Shipping

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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SphK1-IN-2 Related Classifications

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× = ×
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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-2SphKApoptosisSphingosine kinaseSphK1anticancerapoptosisInhibitorinhibitorinhibit

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