Celastrol  (Synonyms: 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) significantly inhibits the proteasomal chymotrypsin activity in PC-3 cells in a concentration-dependent manner; at 2.5 μM it reaches ~55% inhibition, comparable to its potency to a purified 20S proteasome (IC₅₀=2.5 μM). Furthermore, increased levels of IκB-α, Bax, and p27 are observed, three well known target proteins of the proteasome in PC-3 cells treated with Celastrol^[1].

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

Treatment of PC-3 tumor-bearing nude mice with Celastrol (GMP) (1-3 mg/kg/d, i.p., 1-31 days) results in significant inhibition (65-93%) of the tumor growth^[1]. Following treatment with 3 and 6 mg/kg Celastrol (GMP), the levels of malondialdehyde (MDA) are significantly decreased by 35.2 and 36.7%, respectively. Treatment with 3 and 6 mg/kg Celastrol (GMP) markedly restores the GSH level to almost normal levels^[2].

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

450.61

C₂₉H₃₈O₄

34157-83-0

OC1=C(C2=CC=C3[C@](C)([C@]4(CC[C@]3(C2=CC1=O)C)C)CC[C@@]5(C)CC[C@@](C(O)=O)(C[C@]54[H])C)C

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]