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cRIPGBM chloride, an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models.
| Molecular Weight | 446.9 |
| Formula | C26H20ClFN2O2 |
| CAS Number | 2361988-77-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 25 mg/mL (ultrasonic and warming and heat to 60°C) |
| Storage | 4°C, dry, sealed |
| Related RIPK Products |
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| Necrostatin-1
Necrostatin-1 (NEC-1) is a potent inhibitor of necroptosis, with an EC50 of 490 nM in Jurkat cells. Necrostin-1 is the first identified RIPK1 inhibitor, EC50=182 nM, that reduces inflammation and inhibits colitis associated tumorigenesis. Necrostatin-1 (Nec-1) is also an inhibitor of IDO. |
| GSK481
GSK481 is a highly effective, selective and specific RIPK1 inhibitor with an IC50 value of 1.3 nM, which can inhibit the phosphorylation of Ser166 in wild-type human RIPK1 (IC50 value of 2.8 nM). The IC50 value of GSK481 against U937 cells was 10 nM. |
| GSK583
GSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM. |
| Necrostatin-5
Necrostatin-5 is an inhibitor of necroptosis (non-apoptotic cell death pathway) by indirect inhibition of RIP1 kinase, with an EC50 value of 0.24 µM. |
| WEHI-345
WEHI-345 is a potent and selective RIPK2 inhibitor with IC50 of 0.13 μM. WEHI-345 delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation. |
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