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RIPK2 modulator, pro-drug of cRIPGM. cRIPGM binds RIPK2 (apparent Kd = 2.3 μM). Selectively induces apoptosis in glioblastoma multiforme cancer stem cell lines (EC50 is <500 nM). Five-fold selective for CSCs compared with control cell types. Reduces the formation of a prosurvival RIPK2/ TAK1 complex and increases the formation of a proapoptotic RIPK2/caspase 1 complex. Inhibits tumor formation and growth in vivo. Orally bioavailable and brain penetrant.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 428.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.1 mM||23.34 mL||116.7 mL||233.39 mL|
|0.5 mM||4.67 mL||23.34 mL||46.68 mL|
|1 mM||2.33 mL||11.67 mL||23.34 mL|
|5 mM||0.47 mL||2.33 mL||4.67 mL|
References are publications that support the biological activity of the product.
Lucki et al (2019) A cell type-selective apoptosis-inducing small molecule for the treatment of brain cancer. Proc.Natl.Acad.Sci.USA. 116 6435 PMID: 30846550
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Keywords: RIPGBM, RIPGBM supplier, Pro-drug, cRIPGM, RIPK2, modulators, modulates, apoptosis, glioblastoma, multiforme, cancer, orally, bioavailable, and, brain, penetrant., RIP, Kinases, 6892, Tocris Bioscience
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