Omaveloxolone (RTA-408)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Omaveloxolone (RTA-408) is a novel synthetic triterpenoid that binds to Kelch-like ECH-associated protein 1 (Keap1) and attenuate nuclear factor erythroid 2-related factor 2 (Nrf2) degradation [1].
Keap1 is involved in proteasomal degradation of Nrf2, thereby maintaining low basal levels of Nrf2. Binding to Keap1 and blocking its ability to promote Nrf2 degradation increase newly synthesized Nrf2 accumulated in the nucleus where Nrf2 increases the expression of antioxidant genes and decreases the expression of pro-inflammatory genes [1].
In interferon-γ-stimulated RAW 264.7 macrophage cells, low concentrations (≤ 25 nM) of RTA-408 activated Nrf2 and lowered nitric oxide and pro-inflammatory cytokine levels. At higher concentrations, RTA-408 inhibited tumor cell growth, with GI50 of 260 ± 74 nM. Meanwhile, RTA-408 increased caspase activity in tumor cell lines, but not in normal primary human cells.
In mice with radiation-induced dermatitis, topical application of RTA-408 (0.01%, 0.1% and 1.0%, q.d.) resulted in dose-dependent improvements in the appearance of skin, with 1.0% RTA-408 markedly reducing epidermal and collagen thickening, preventing dermal necrosis, and completely alleviating skin ulcers [2].
References:
[1]. Probst B L, Trevino I, McCauley L, et al. RTA 408, a novel synthetic triterpenoid with broad anticancer and anti-inflammatory activity. PLoS One, 2015, 10(4): e0122942.
[2]. Reisman S A, Lee C Y, Meyer C J, et al. Topical application of the synthetic triterpenoid RTA 408 protects mice from radiation-induced dermatitis. Radiation Research, 2014, 181(5): 512-520.
| Storage | Store at -20°C |
| M.Wt | 554.71 |
| Cas No. | 1474034-05-3 |
| Formula | C33H44F2N2O3 |
| Solubility | ≥55.5 mg/mL in DMSO; insoluble in H2O; ≥25.05 mg/mL in EtOH |
| SDF | Download SDF |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]: | |
|
细胞系 |
PANC-1，A549和A375细胞系 |
|
溶解方法 |
可溶于DMSO。为了获得更高浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
0~1000 nM，72小时 |
|
应用 |
RTA 408可抑制人类肿瘤细胞系的生长，并诱导肿瘤细胞凋亡（增加caspase酶的活性）。 |
| 动物实验[2]: | |
|
动物模型 |
BALB/c小鼠 |
|
剂量 |
每天局部涂抹（0.01％，0.1％或1.0％，溶于芝麻油中），持续35天 |
|
应用 |
RTA 408可以通过激活抗氧化转录因子Nrf2和抑制促炎转录因子核因子κB（NF-κB）来保护皮肤免受辐射诱发的皮炎。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
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References: [1] Probst BL, Trevino I, McCauley L, Bumeister R, Dulubova I, Wigley WC, Ferguson DA. RTA 408, A Novel Synthetic Triterpenoid with Broad Anticancer and Anti-Inflammatory Activity. PLoS One. 2015 Apr 21;10(4):e0122942. [2] Reisman SA, Lee CY, Meyer CJ, Proksch JW, Sonis ST, Ward KW. Topical application of the synthetic triterpenoid RTA 408 protects mice from radiation-induced dermatitis. Radiat Res. 2014 May;181(5):512-20. |
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质量控制和MSDS
- 批次:
化学结构
