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SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $41 | In Stock | |
5 mg | $66 | In Stock | |
10 mg | $116 | In Stock | |
25 mg | $226 | In Stock | |
50 mg | $363 | In Stock | |
100 mg | $547 | In Stock | |
500 mg | $1,170 | In Stock | |
1 mL x 10 mM (in DMSO) | $73 | In Stock |
Description | SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1. |
Targets&IC50 | SPHK1:0.1-1.8 μM |
In vitro | SKI-178 is a multi-targeted agent that functions both as an inhibitor of the SphKs as well as a disruptor of the microtubule network.?SKI-178 induced apoptosis arises from a synergistic interaction of these two activities.?SKI-178 is safe and effective in mouse models of AML, supporting its further development as a multi-targeted anti-cancer therapeutic agent[1]. |
Molecular Weight | 394.42 |
Formula | C21H22N4O4 |
Cas No. | 1259484-97-3 |
Smiles | COc1ccc(cc1)-c1cc([nH]n1)C(=O)N\N=C(/C)c1ccc(OC)c(OC)c1 |
Relative Density. | 1.24 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (126.77 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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