K145 Hydrochloride is a selective, substrate competitive and oral inhibitor of SphK2, IC50 4.3 µM and Ki 6.4 µM. K145 hydrochloride has no activity against SphK1 and other protein kinases. K145 Hydrochloride induces apoptosis and has strong anti-tumor activity.
| Molecular Weight | 384.92 |
| Formula | C18H24N2O3S.HCl |
| CAS Number | 1449240-68-9 |
| Solubility (25°C) | Water 90 mg/mL DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related SPHK Products |
|---|
| SLM6031434 hydrochloride
SLM6031434 hydrochloride is a highly selective sphingosine kinase 2 (SphK2) inhibitor with Kis of 0.4 μM, 0.5 μM, >20 μM, 22 μM for mSphK2, rSphK2, mSphK1 and rSphK1, respectively. SLM6031434 hydrochloride decrease Sphingosine 1-phosphate (S1P) levels in U937 monocytic leukemia cells. SLM6031434 hydrochloride has the potential for renal fibrosis research. |
| N,N-Dimethylsphingosine
N,N-Dimethylsphingosine is a potent inhbitor of SphK (sphingosine kinase) as an endogenous metabolite of sphingosine produced in various tissues and tumor cell lines. |
| SKI-V
SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity. |
| WAY-604116
WAY-604116 is a sphingosine kinase inhibitor |
| WAY-358981
WAY-358981 is a Sphingosine kinase inhibitor |
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