Celastrol  (Synonyms: 雷公藤红素 (GMP); Tripterine; Tripterin)

Celastrol (GMP) (Tripterine (GMP)) is Celastrol (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH^[1][2][3].

Celastrol (Tripterine；Tripterin) (GMP) 以浓度依赖性方式显著抑制 PC-3 细胞中蛋白酶体胰凝乳蛋白酶的活性；在 2.5 μM 时，它达到约 55% 的抑制，与其对纯化的 20S 蛋白酶体的效力相当 (IC₅₀=2.5 μM)。此外，观察到 IκB-α、Bax 和 p27 水平升高，这是用 Celastrol 处理的 PC-3 细胞中蛋白酶体的三种众所周知的靶蛋白^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

用 Celastrol (1-3 mg/kg/d，腹腔注射，1-31 天) 处理携带 PC-3 肿瘤的裸鼠导致显著抑制肿瘤生长 (65-93%)^[1]。
用 3 和 6 mg/kg Celastrol 处理后，丙二醛 (MDA) 水平分别显著降低 35.2% 和 36.7% (P<0.05)。用 3 和 6 mg/kg 的 Celastrol 处理可显著将 GSH 水平 (P<0.05) 恢复到几乎正常的水平^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

450.61

C₂₉H₃₈O₄

34157-83-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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  [Content Brief]

  [2]. Guan Y, et al. Celastrol attenuates oxidative stress in the skeletal muscle of diabetic rats by regulating the AMPK-PGC1α-SIRT3 signaling pathway. Int J Mol Med. 2016 May;37(5):1229-38.  [Content Brief]

  [3]. Yuan Z, et al. Celastrol Combats Methicillin‐Resistant Staphylococcus aureus by Targeting Δ1‐Pyrroline‐5‐Carboxylate Dehydrogenase[J]. Advanced Science, 2023, 10(25): 2302459.  [Content Brief]