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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Chelerythrine
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
34316-15-9
- 规格：
20mg/10mg/5mg
| 规格： | 20mg | 产品价格： | ￥960.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥640.0 |
| 规格： | 5mg | 产品价格： | ￥440.0 |
| 基本信息 | |
| CAS | No.34316-15-9 |
| 中文名称 | 白屈菜红碱 |
| 英文名称 | Chelerythrine |
| 别名 | Toddalin;Broussonpapyrine |
| 分子式 | C21H18NO4 |
| 分子量 | 348.37 |
| 溶解性 | Soluble in DMSO ≥10mg/mL |
| 纯度 | HPLC≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 251-930-0 |
| MDL | MFCD00270393 |
| SMILES | C[N+]1=CC2=C(OC)C(OC)=CC=C2C(C=CC3=C4)=C1C3=CC5=C4OCO5 |
| InChIKey | LLEJIEBFSOEYIV-UHFFFAOYSA-N |
| InChI | InChI=1S/C21H18NO4/c1-22-10-16-13(6-7-17(23-2)21(16)24-3)14-5-4-12-8-18-19(26-11-25-18)9-15(12)20(14)22/h4-10H,11H2,1-3H3/q+1 |
| PubChem CID | 2703 |
| 靶点 | PKC |
| 通路 | TGF-beta/Smad;Epigenetics |
| 背景说明 | Chelerythrine 是一种生物碱,为有效、选择性的 Ca2+/磷脂依赖性 PKC 拮抗剂。 |
| 生物活性 | Chelerythrine is a natural alkaloid， acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist， with an IC50 of 0.7 μM[1]. Chelerythrine has antitumor， antidiabetic and anti-inflammatory activity[2]. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy[3][4]. |
| IC50 | IC50:0.7μM(PKC)[1] |
| In Vitro | Chelerythrine interacted with the catalytic domain of PKC， was a competitive inhibitor with respect to the phosphate acceptor (histone IIIS) (Ki = 0.7 microM) and a non-competitive inhibitor with respect to ATP. This effect was further evidenced by the fact that chelerythrine inhibited native PKC and its catalytic fragment identically and did not affect [3H]- phorbol 12，13 dibutyrate binding to PKC.[1]Western Blot Analysis[4]:Cell Line:A549 and NCI-H1299 cells;Concentration:10， 15， 20 μM;Incubation Time:24 h;Result:Induced expression of LC3-II in a beclin 1-dependent way. |
| 细胞实验 | CHE displayed significant anti - inflammatory effects in experimentally induced mice endotoxic shock model in vivo through inhibition of LPS - induced tumor necrosis factor - alpha (TNF - α) level and nitric oxide (NO) production in serum.[5]。Animal Model: Unilateral ureteral obstruction (UUO) induced neonatal rats[2];Dosage:5 mg/kg;Administration:i.p.， daily;Result:Attenuated kidney injury (Increased kidney weight and restored renal function).Inhibited UUO-induced upregulated kidney injury molecule-1 expression， apoptosis， and renal fibrosis. |
| 数据来源文献 | [1]. Herbert JM， et al. Chelerythrine is a potent and specific inhibitor of protein kinase C. Biochem Biophys Res Commun. 1990 Nov 15;172(3):993-9. [2]. Shi B， et al. Protein kinase C inhibitor chelerythrine attenuates partial unilateral ureteral obstruction induced kidney injury in neonatal rats. Life Sci. 2019 Jan 1;216:85-91. [3]. Chan SL， et al.Identification of chelerythrine as an inhibitor of BclXL function.J Biol Chem. 2003 Jun 6;278(23):20453-6. [4]. Tang ZH， et al.Induction of reactive oxygen species-stimulated distinctive autophagy by chelerythrine in non-small cell lung cancer cells.Redox Biol. 2017 Aug;12:367-376. [5]. Li W， et al. Effect of chelerythrine against endotoxic shock in mice and its modulation of inflammatory mediators in peritoneal macrophages through the modulation of mitogen-activated protein kinase (MAPK) pathway. Inflammation. 2012 Dec;35(6):1814-24. [6]. He N， et al. Antibacterial mechanism of chelerythrine isolated from root of Toddalia asiatica (Linn) Lam. BMC Complement Altern Med. 2018 Sep 26;18(1):261. |
| 单位 | 瓶 |
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文献和实验CDllb 常用单克隆抗体或代号：Mol，OKM1；(Macl，CR3，整合素αM) 主要表达细胞：G，M，T， B， DC， NK，Mac[AS] 分子质量(kDa)和结构：gp170(整合素α) 功 能：iC3b和Fs受体，与ICAM-l和X因子结合，黏附，调理吞噬；结合JAM-3 CDllc 常用单克隆抗体或代号：LeuM乳(CR4．整合素αX) 主要表达细胞：M，G，B
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