research use only
Cat.No.S8301
| Related Targets | PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Anti-infection Antioxidant COX Histamine Receptor |
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| Other Interleukins Inhibitors | SC144 Diacerein Ac-YVAD-cmk Apilimod mesylate EC330 Sodium Thiocyanate IQ 3 Raleukin Cp2-SO4 Suplatast Tosylate |
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In vitro |
DMSO
: 62 mg/mL
(198.68 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 312.05 | Formula | C2H4Cl3O2Te.H4N |
Storage (From the date of receipt) | |
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| CAS No. | 106566-58-9 | Download SDF | Storage of Stock Solutions |
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| Targets/IC50/Ki |
IL-1β converting enzyme
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| In vitro |
Treatment of caspase-1 (interleukin-1 [IL-1] converting enzyme [ICE]) with Ossirene (AS101) inhibits its enzymatic activity in a dose-dependent manner. Moreover, it causes a significant reduction in the active form of IL-18 and IL-1 in peripheral blood mononuclear cells (PBMC) and in human HaCat keratinocytes. The inhibitory effect of this compound does not involve nitric oxide (NO) or interferon- (IFN- ), two possible regulators of IL-18 production, and does not occur at the mRNA level. It may exert effects through a posttranscriptional mechanism. AS101 induced SIRT1 expression in a dose dependent manner in three different cell lines, HEK293, HL-60 and Rin-5f. Incubation of HEK293 and HL-60 cell lines with it (0.1-2.5μg/ml) resulted in a dose dependent reduction in PPARγ protein expression relative to the control cells, and the reduction of PPARγ expression is in parallel to increased SIRT1 expression.
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| In vivo |
Ossirene (AS101) downregulates IL-18 and IL-1 serum levels in a mouse model of lipopolysaccharide (LPS)-induced sepsis, resulting in increased survival. It has also been shown to be protective against lethal and sublethal effects of irradiation and chemotherapy. In a model of cecal ligation and puncture (CLP)-induced sepsis in mice, this compound also exerted beneficial effects. Treated rats showed a large increase in SIRT1 protein levels in the liver and kidney extracts. It prevents development of insulin resistance in vivo and affects SIRT1 related metabolic pathways by changing the insulin levels. AS101 treatment prevents hyperglycemia associated with T2D(type 2 diabetes) and some of the symptoms of the disease in the HFD(high fat diet)+STZ(Streptozotocin) rat model.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01943630 | Unknown status | External Genital Warts |
BioMAS Ltd |
January 2015 | Phase 2 |
| NCT01010373 | Suspended | Acute Myeloid Leukemia|Myelodysplastic Syndrome |
BioMAS Ltd |
January 2015 | Phase 2 |
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