Recilisib (Ex-RAD) |
| رقم الكتالوجGC33130 |
Recilisib (Ex-RAD) (ON 01210) هو واقي إشعاعي ، يمكنه تنشيط أنشطة AKT و PI3K في الخلايا.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 334969-03-8
Sample solution is provided at 25 µL, 10mM.
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Recilisib (Ex-RAD) is a radiation protection agent that can activate the activities of AKT and PI3K in cells [1]. Recilisib can promote autophagy, enhance cell viability, and reduce cell apoptosis by activating the PI3K/AKT/mTOR pathway [2]. Recilisib can alter the cell cycle distribution pattern of cancer cells receiving radiotherapy and can be used for the treatment of acute radiation syndrome [3].
In vitro, treatment with Recilisib (10μM; 24h) significantly upregulated the protein expressions of p-PI3K, p-AKT, and p-p65 in Caco-2 cells, while the number of apoptotic cells increased, Bax and C-caspase3 expressions were upregulated, and Bcl-2 expression was decreased [4]. Treatment with Recilisib (50μM; 24h) reversed the autophagy induced by MG-132 in vascular smooth muscle cells (VSMCs), and reduced the expressions of autophagy-related proteins p-PI3K/PI3K, p-AKT/AKT, and p-mTOR/mTOR [5].
In vivo, treatment with Recilisib (10mg/kg/day; 7 days; i.p.) exacerbated the damage to the integrity of the blood-brain barrier in a mouse model of anti-N-methyl-d-aspartate receptor (NMDAR) encephalitis, reduced the expressions of ZO-1 and Claudin-5, and had no significant effect on the neurological damage of the mice [6]. Treatment with Recilisib (3, 100, 50, and 10mg/kg/day; i.p.) significantly increased the content of gallstones in a mouse model treated with LPS and aggravated the damage to the gallbladder mucosa [7].
References:
[1] Kang AD, et al. ON01210.Na (Ex-RAD) mitigates radiation damage through activation of the AKT pathway. PLoS One. 2013;8(3):e58355.
[2] Geng X, Zou Y, Li J, et al. BDNF alleviates Parkinson's disease by promoting STAT3 phosphorylation and regulating neuronal autophagy[J]. Cell and Tissue Research, 2023, 393(3): 455-470.
[3] Kamran M Z, Ranjan A, Kaur N, et al. Radioprotective agents: strategies and translational advances[J]. Medicinal research reviews, 2016, 36(3): 461-493.
[4] Niu M, Yin L, Duan T, et al. Asperosaponin VI alleviates TNBS-induced Crohn's disease-like colitis in mice by reducing intestinal epithelial cell apoptosis via inhibiting the PI3K/AKT/NF-κB signaling pathway[J]. Nan fang yi ke da xue xue bao= Journal of Southern Medical University, 2024, 44(12): 2335-2346.
[5] Shu Z, Li X, Zhang W, et al. MG-132 activates sodium palmitate-induced autophagy in human vascular smooth muscle cells and inhibits senescence via the PI3K/AKT/mTOR axis[J]. Lipids in health and disease, 2024, 23(1): 282.
[6] Gong Z, Lao D, Wu Y, et al. Inhibiting PI3K/Akt-Signaling pathway improves neurobehavior changes in anti-NMDAR encephalitis mice by ameliorating blood–brain barrier disruption and neuronal damage[J]. Cellular and Molecular Neurobiology, 2023, 43(7): 3623-3637.
[7] Yu J, Meng Z, Liu X, et al. Lipopolysaccharide in bile promotes the neutrophil extracellular Traps-Induced gallstone formation by activating the gallbladder immune barrier[J]. ImmunoTargets and Therapy, 2024: 789-803.
| Cell experiment [1]: | |
Cell lines | Vascular smooth muscle cells (VSMCs) |
Preparation Method | The VSMCs were cultured in serum-free medium supplemented with 10% fetal bovine serum, passaged, and utilized for experiments the following day once they reached a cell density of 90% in the culture dish. The experimental groups included: a control group - cultured in serum-free medium; a palmitate (PA) group - cultured in serum-free medium containing 40µM PA; PA + MG-132 group - cultured in serum-free medium containing 40µM PA and 40µM MG-132; a PA + MG-132 + Pictilisib group - cultured in serum-free medium containing 40µM PA and 2nM Pictilisib; and a PA + MG-132 + Recilisib group cultured in serum-free medium containing 40µM PA, 40µM MG-132, and 50µM Recilisib. After each group of cells was cultured in the modified medium for 24 hours, autophagy staining determination and protein blotting determination were carried out. |
Reaction Conditions | 50μM; 24h |
Applications | The treatment with Recilisib reduced the expression of autophagy-related proteins p-PI3K/PI3K, p-AKT/AKT and p-mTOR/mTOR. |
| Animal experiment [2]: | |
Animal models | C57BL / 6J mice (anti-NMDAR encephalitis mouse model) |
Preparation Method | The mice were subcutaneously immunized with 200μg of the polypeptide mixture, of which the mice in the control group were subcutaneously immunized with a mixture of equal volumes of CFA and phosphate-buffered saline (PBS). A booster injection was given 4 weeks after the immunization. All mice were intraperitoneally injected with 200ng pertussis toxin on the day of immunization and 48h after immunization. Animals were randomly divided into 4 groups: control group, model group, model + LY294002 group, and model + Recilisib group. Mice in the treatment group were intraperitoneally administered LY294002 (PI3K inhibitor, 8mg/kg) or Recilisib (10mg/kg) every day. The above treatments were given once a day for 7 consecutive days. All PI3K inhibitors and agonists were dissolved in dimethyl sulfoxide/saline (1:10). The same amount of sterile solvent was injected intraperitoneally into the control group and model group. The BBB permeability of mice was detected by the sodium fluorescein method. |
Dosage form | 10mg/kg/day for 7 days; i.p. |
Applications | Recilisib exacerbated the damage to the blood-brain barrier integrity in the mouse model of anti-NMDAR encephalitis. |
References: | |
| Cas No. | 334969-03-8 | SDF | |
| Canonical SMILES | O=C(O)C1=CC=C(/C=C/S(=O)(CC2=CC=C(Cl)C=C2)=O)C=C1 | ||
| Formula | C16H13ClO4S | M.Wt | 336.79 |
| الذوبان | DMSO: 35.71 mg/mL (106.03 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9692 mL | 14.846 mL | 29.6921 mL |
| 5 mM | 593.8 μL | 2.9692 mL | 5.9384 mL |
| 10 mM | 296.9 μL | 1.4846 mL | 2.9692 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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