| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C408328-1ml |
1ml |
现货  |
|
| 英文别名 | Tripterine | (2R,4aS,6aS,12bR,14aS,14bR)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2-carboxylic acid |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Celastrol (NSC 70931) |
| 生化机理 | Celastrol （NSC 70931，Tripterine）是一种强效蛋白酶体抑制剂，可抑制纯化的 20S 蛋白酶体的糜蛋白酶样活性，IC50 为 2.5 μM。塞拉斯托通过 ROS/JNK 信号通路诱导细胞凋亡和自噬。塞拉斯托通过激活有丝分裂抑制帕金森病多巴胺能神经元的死亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | G 蛋白信号调节抑制剂 17 |
| 产品介绍 |
存在于卫矛科植物雷公藤、南蛇藤等中的抗癌活性成分。该化合物结构载于2006年5月份Cancer Research杂志封面，并证实南蛇藤素通过抑制蛋白酶体活性进而诱发癌细胞凋亡，是有效的蛋白酶体抑制剂，其显著抑制了裸鼠身上前列腺癌的增生。因此，在癌症的预防和治疗方面，南蛇藤素是具有巨大开发潜力的天然蛋白酶体抑制剂。雷公藤红素是一种强力抗氧化，抗发炎剂。它是一种新型的HSP90的抑制剂（扰乱Hsp90/Cdc37复合物），抗癌（抗血管生成 - 抑制VEGFR的表达）;抗氧化剂（抑制脂质过氧化反应）和抗发炎活性（抑制iNOS及炎性细胞因子的生产）。 Information Celastrol (NSC 70931, Tripterine) is a potentproteasomeinhibitor for the chymotrypsin-like activity of a purified 20S proteasome withIC50of 2.5 μM. Celastrol inducesapoptosisandautophagyvia the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic ne Celastrol at 5 μM inhibits the chymotrypsin-like, PGPH-like, and trypsin-like activities of the purified 20S proteasome by 80%, 5%, and <1%, respectively, whereas at 10 μM, it inhibits these three proteasomal activities by ∼90%, 15%, and <1%, respectively. Celastrol significantly inhibits the proteasomal chymotrypsin activity in PC-3 cells in a concentration-dependent manner. Celastrol at 2.5 μM to 5 μM induces caspase-3 activity by 4.7-fold to 5.5-fold in PC-3 cells. Celastrol (5 μM) treated cells, the levels of the proteasome target proteins, IκB-α and Bax, are increased after 1 hour and further increased to its peak for 4 hours to 12 hours. Celastrol (2.5 μM) treatment induces proteasome inhibition by 40%, as shown by the decreased levels of chymotrypsin-like activity and increased accumulation of ubiquitinated proteins in LNCaP cells. Celastrol (2.5 μM) induces apoptosis in the Celastrol-treated LNCaP cells, as shown by increased levels of caspase-3 activity (up to 3.5-fold), PARP cleavage, and apoptotic morphology. Celastrol (300 nM) is found to suppress LPS-induced production of TNF-alpha and IL-1beta by human monocytes and macrophages. Celastrol (100 nM) also decreases LPS-induced expression of class II MHC molecules by microglia. Celastrol strongly inhibits LPS and IFN-y-induced NO production with IC50 of 200 nM in macrophage lineage cells. Celastrol strongly inhibits TNF-α and IFN-γ-induced NO production with IC50 of 200 nM in endothelial cells. Celastrol (2.5 μM) potentiates the apoptosis induced by TNF and chemotherapeutic agents and inhibits invasion, both regulated by NF-kappaB activation, in KBM-5 cells. Celastrol (2.5 μM) suppresses the expression of TNF induced the expression of gene products involved in antiapoptosis (IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP, and survivin), proliferation (cyclin D1 and COX-2), invasion (MMP-9), and angiogenesis (VEGF) in KBM-5 cells. Celastrol (5 μM) is found to inhibit the TNF-induced activation of IkappaBalpha kinase, IkappaBalpha phosphorylation, IkappaBalpha degradation, p65 nuclear translocation and phosphorylation, and NF-kappaB-mediated reporter gene expression. Celastrol inhibits proliferating of RPMI 8226, KATOIII, UM-SCC1, U251MG and MDA-MB-231 cells with IC50 of 0.52 μM, 0.54 μM, 0.76 μM, 0.69 μM and 0.67 μM, respectively. Celastrol (1 μM) inhibits growth of RPMI 8226 with a decrease in the levels of cyclin D1 and cyclin E, but concomitant increase in the levels of p21 and p27. Celastrol induces apoptosis in RPMI-8226 cells indicated by the activation of caspase-8, bid cleavage, caspase-9 activation, caspase-3 activation, PARP cleavage and through the down regulation of anti-apoptototic proteins. Celastrol (1 μM) suppresses Akt pathway and activates JNK kinase in RPMI-8226 cells. In vivo Celastrol (3 mg/kg) results in significant inhibition (up to 70%) of tumor growth in male nude mice bearing PC-3 tumors, associated with increased p27 levels and Bax level. Celastrol (3 mg/kg) results more apoptotic tumor cells with the appearance of various PARP cleavage fragments in tumor of male nude mice bearing PC-3 tumors. Celastrol (3 mg/kg) causes 35% of tumor inhibition, associated with decreased proteasome activity and decreased expression of AR protein in nude mice bearing C4-2B tumors. Celastrol (3 mg/kg) is found to suppress strongly joint swelling and other manifestations of adjuvant arthritis in mice. Celastrol (0.2 mg/kg) significantly improves the performance in memory, learning and psychomotor activity tests in rats. cell lines： Concentrations：~5 μM Incubation Time：2 hours Powder Purity:≥98% |
| EC号 | 636-472-5 |
|---|---|
| 分子类型 | 小分子 |
| Isomeric SMILES | CC1=C(C(=O)C=C2C1=CC=C3[C@]2(CC[C@@]4([C@@]3(CC[C@@]5([C@H]4C[C@](CC5)(C)C(=O)O)C)C)C)C)O |
| 关联CAS | 34157-83-0 |
| NSC Number | 70931 |
| UN Number | 2811 |
| MeSH Entry Terms | 3-hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid;celastrol;tripterin;tripterine |
| 分子量 | 450.61 |
| Reaxy-Rn | 5780870 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5780870&ln= |
| 溶解性 | Solubility (25°C) In vitro Water: 28 mg/mL (199.18 mM); DMSO: Insoluble; Ethanol: Insoluble; |
|---|---|
| 比旋光度 | -122.7° (C=0.1,CHCl3) |
| 熔点 | 203°C(lit.) |
| 象形图 | GHS06 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H301: 吞咽会中毒 |
| 预防措施声明 |
P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P301+P316: 如果吞咽：立即寻求紧急医疗救助。 |
| WGK Germany | 2 |
| 个人防护装备 | Eyeshields,Faceshields,Gloves,type P2 (EN 143) respirator cartridges |
| 1. Min Wei, Yi Liu, Dongsheng Li, Xingdong Wang, Xiaodong Wang, Yuping Li, Zhengcun Yan, Hengzhu Zhang. (2024) Celastrol alleviates secondary brain injury following intracerebral haemorrhage by inhibiting neuronal ferroptosis and blocking blood-brain barrier disruption. IBRO Neuroscience Reports, 17 (161). [PMID:39220228] [10.1016/j.ibneur.2024.08.003] |
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