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Tripterin

Tripterin

产品编号 T3028   CAS 34157-83-0
别名: Celastrol, Tripterine, 雷公藤红素

Tripterin (Celastrol) 属于天然产物,是一种蛋白酶体抑制剂,抑制 20S 蛋白酶体的胰凝乳蛋白酶样活性 (IC50=2.5 μM)。Tripterin 具有抗炎、抗感染和免疫调节的作用。

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Tripterin Chemical Structure
Tripterin, CAS 34157-83-0
规格 价格/CNY 货期 数量
5 mg ¥ 427 现货
10 mg ¥ 698 现货
25 mg ¥ 1,230 现货
50 mg ¥ 1,822 现货
100 mg ¥ 2,698 现货
1 mL * 10 mM (in DMSO) ¥ 716 现货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Tripterin (T3028)
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纯度: 99.8%
纯度: 99.58%
纯度: 99.48%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Tripterin (Celastrol) is a natural product, a proteasome inhibitor that inhibits the pancreatic rennet-like activity of the 20S proteasome (IC50=2.5 μM). Tripterin has anti-inflammatory, anti-infectious, and immunomodulatory properties.
靶点活性 20S proteasome:2.5 μM
体外活性 方法:人前列腺癌细胞 PC-3 用 Tripterin (0.5-5 µM) 处理 12 h,使用 Z-GGL-AMC 检测蛋白酶体糜蛋白酶样活性。
结果:Tripterin 以浓度依赖的方式显著抑制 PC-3 细胞中蛋白酶体糜蛋白酶的活性,在 2.5 µM 时,达到约 55% 的抑制作用。[1]
方法:人慢性髓白血病细胞 KBM-5 用 Tripterin (2.5 µM) 孵育 6 h,随后用 TNF (1 nM) 处理 6-24 h,使用 Western Blot 检测靶点蛋白表达水平。
结果:TNF 以时间依赖的方式诱导抗凋亡蛋白 IAP1、IAP2、Bcl-2、Bcl-XL、c-FLIP 和 survivin 的表达,Tripterin 抑制了表达。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 Tripterin (1-3 mg/kg,10% DMSO+70% Cremophor/ethanol (3:1)+20% PBS) 腹腔注射给携带人前列腺癌肿瘤 PC-3 的 nude immunodeficient 小鼠,每天一次,持续十六天。
结果:Tripterin 治疗显著抑制前列腺癌症异种移植物的生长,并抑制体内蛋白酶体活性和诱导细胞凋亡。[1]
方法:为检测体内抗肿瘤活性,将 Tripterin (1.25 mg/kg) 腹腔注射给携带前庭神经鞘瘤 SC4 的 BALB/c (nu/nu) 小鼠,每三天一次,持续两周。
结果:Tripterin 显著抑制肿瘤生长而不显示毒性。[3]
激酶实验 Inhibition of purified 20S proteasome activity: A purified rabbit 20S proteasome (0.1 μg) is incubated with 40 μM of various fluorogenic peptide substrates in 100 μL assay buffer (20 mM Tris-HCl (pH 7.5)), in the presence of Celastrol at different concentrations or in the solvent DMSO for 2 hours at 37 ℃, followed by measurement of inhibition of each proteasomal activity.
细胞实验 The anti-proliferative effect of celastrol on various human tumor cell lines is determined by the MTT uptake method. Briefly, 5×103 cells are incubated with Celastrol in triplicate in a 96-well plate at 37 ℃. MTT solution is then added to each well. After a 2 hours incubation at 37 ℃, extraction buffer (20% SDS, 50% dimethylformamide) is added, cells are incubated overnight at 37 ℃, and the optical density is then measured at 570 nm using a Tecan plate reader.(Only for Reference)
别名 Celastrol, Tripterine, 雷公藤红素
分子量 450.61
分子式 C29H38O4
CAS No. 34157-83-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 60 mg/mL (133.15 mM)

Ethanol: 33.8 mg/mL (75 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.2192 mL 11.0961 mL 22.1921 mL 55.4803 mL
5 mM 0.4438 mL 2.2192 mL 4.4384 mL 11.0961 mL
10 mM 0.2219 mL 1.1096 mL 2.2192 mL 5.548 mL
20 mM 0.111 mL 0.5548 mL 1.1096 mL 2.774 mL
50 mM 0.0444 mL 0.2219 mL 0.4438 mL 1.1096 mL
DMSO 100 mM 0.0222 mL 0.111 mL 0.2219 mL 0.5548 mL

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TargetMol Library Books参考文献

1. Yang H, et al. Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. Cancer Res. 2006 May 1;66(9):4758-65. 2. Sethi G, et al. Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kappaB-regulated gene products and TAK1-mediated NF-kappaB activation. Blood. 2007 Apr 1;109(7):2727-35. 3. Kim NH, et al. Celastrol suppresses the growth of vestibular schwannoma in mice by promoting the degradation of β-catenin. Acta Pharmacol Sin. 2022 Nov;43(11):2993-3001. 4. Kannaiyan R, et al. Apoptosis, 2011, 16(10), 1028-1041. 5. Liu Q, Yue Y, Wang S, et al. Celastrol Attenuates the Remodeling of Pulmonary Vascular and Right Ventricular in Monocrotaline-Induced Pulmonary Arterial Hypertension in Rats[J]. 2021 6. Jiang X, Chen S, Zhang Q, et al. Celastrol is a novel selective agonist of cannabinoid receptor 2 with anti-inflammatory and anti-fibrotic activity in a mouse model of systemic sclerosis[J]. Phytomedicine. 2019: 153160.

TargetMol Library Books文献引用

1. Qing T, Yan L, Wang S, et al.Celastrol alleviates oxidative stress induced by multi-walled carbon nanotubes through the Keap1/Nrf2/HO-1 signaling pathway.Ecotoxicology and Environmental Safety.2023, 252: 114623. 2. Zhang H, Cai J, Li C, et al.Wogonin inhibits latent HIV-1 reactivation by downregulating histone crotonylation.Phytomedicine.2023: 154855. 3. Zhao W, Xu C, Peng L, et al.cAMP/PKA signaling promotes AKT deactivation by reducing CIP2A expression, thereby facilitating decidualization.Molecular and Cellular Endocrinology.2023: 111946. 4. Li S, Hao L, Hu X, et al.A systematic study on the treatment of hepatitis B-related hepatocellular carcinoma with drugs based on bioinformatics and key target reverse network pharmacology and experimental verification.Infectious Agents and Cancer.2023, 18(1): 41. 5. Liu X, Hu Q, Wang W, et al. A protein-fragment complementation assay reveals that celastrol and gambogic acid suppress ERα mutants in breast cancer. Biochemical Pharmacology. 2021, 188: 114583. 6. Jiang X, Chen S, Zhang Q, et al. Celastrol is a novel selective agonist of cannabinoid receptor 2 with anti-inflammatory and anti-fibrotic activity in a mouse model of systemic sclerosis. Phytomedicine. 2019: 153160 7. Liu Q, Yue Y, Wang S, et al. Celastrol Attenuates the Remodeling of Pulmonary Vascular and Right Ventricular in Monocrotaline-Induced Pulmonary Arterial Hypertension in Rats. Cardiovascular Diagnosis and Therapy. 2022 Feb;12(1):88-102. doi: 10.21037/cdt-21-360.
Dehydrotrametenolic acid Notopterol Droxinostat ZM 336372 Larotrectinib sulfate Brassinolide Ziyuglycoside I Importazole

相关化合物库

该产品包含在如下化合物库中:
中药单体化合物库 抗癌活性化合物库 高通量筛选天然产物库 抑制剂库 天然产物库 已知活性化合物库 自噬库 共价抑制剂库 泛素化化合物库 抗纤维化化合物库

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Tripterin 34157-83-0 Apoptosis Autophagy Proteases/Proteasome Ubiquitination Mitophagy Proteasome Celastrol inhibit Tripterine Endogenous Metabolite Mitochondrial Autophagy Inhibitor 雷公藤红素 inhibitor

 

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