Ossirene (AS101)

Catalog No.S8301 Batch:S830102

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Technical Data

Formula

C2H4Cl3O2Te.H4N
Molecular Weight 312.05 CAS No. 106566-58-9
Solubility (25°C)* In vitro DMSO 62 mg/mL (198.68 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.
Targets
IL-1β converting enzyme [1]
In vitro Treatment of caspase-1 (interleukin-1 [IL-1] converting enzyme [ICE]) with AS101 inhibits its enzymatic activity in a dose-dependent manner. Moreover, AS101 treatment 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 AS101 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[1]. 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 AS101 (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[2].
In vivo 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, AS101 also exerted beneficial effects[1]. AS101 treated rats showed a large increase in SIRT1 protein levels in the liver and kidney extracts of rats treated with AS101. AS101 prevents development of insulin resistance in vivo. AS101 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[2].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Human peripheral blood mononuclear cells (PBMC)

  • Concentrations

    0.01, 0.05, 0.5, 1, 1.5, 2 μg/mL

  • Incubation Time

    24 h

  • Method

    In vitro, PBMCs were first treated with various concentrations of AS101, and after 1 h SAC (10-3 v/v) was added. After 24 h, supernatants were collected and evaluated for cytokine content.
Animal Study:

[1]
  • Animal Models

    c57BL/6J and BALB/c mice

  • Dosages

    10 μg/mouse

  • Administration

    i.p.

Selleck's Ossirene (AS101) has been cited by 9 publications

Extensive jejunal injury is repaired by migration and transdifferentiation of ileal enterocytes in zebrafish [ Cell Rep, 2023, 42(7):112660] PubMed: 37342912
Multiomics Analysis of a DNAH5-Mutated PCD Organoid Model Revealed the Key Role of the TGF-β/BMP and Notch Pathways in Epithelial Differentiation and the Immune Response in DNAH5-Mutated Patients [ Cells, 2022, 11(24)4013] PubMed: 36552777
Regulation of STUB1 expression and its biological significance in mouse Sertoli cells [ Syst Biol Reprod Med, 2022, 1-15] PubMed: 35343345
IL-10-/- Enhances DCs Immunity Against Chlamydia psittaci Infection via OX40L/NLRP3 and IDO/Treg Pathways [ Front Immunol, 2021, 12:645653] PubMed: 34093535
Prior transfusion of umbilical cord mesenchymal stem cells can effectively alleviate symptoms of motion sickness in mice through interleukin 10 secretion [ World J Stem Cells, 2021, 13(2):177-192] PubMed: 33708346
Macrophage-Derived IL-1β Regulates Emergency Myelopoiesis via the NF-κB and C/ebpβ in Zebrafish [ J Immunol, 2020, 205(10):2694-2706] PubMed: 33077646
P-selectin glycoprotein ligand 1 deficiency prevents development of acute pancreatitis by attenuating leukocyte infiltration [ World J Gastroenterol, 2020, 26(41):6361-6377] PubMed: 33244198
IL-10 knockdown with siRNA enhances the efficacy of Doxorubicin chemotherapy in EBV-positive tumors by inducing lytic cycle via PI3K/p38 MAPK/NF-kB pathway. [ Cancer Lett, 2019, 10.1016/j.canlet.2019.07.016] PubMed: 31352079
Extracellular RNAs from lung cancer cells activate epithelial cells and induce neutrophil extracellular traps. [ Int J Oncol, 2019, 55(1):69-80] PubMed: 31115506

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.