Pristimerin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Pristimerin 具有抗癌活性，Pristimerin 治疗可能是通过逆转缺氧诱导的干细胞特征和癌细胞 EMT 来抑制缺氧诱导的转移的潜在策略。

Pristimerin has anticancer activity , treatment with Pristimerin may be a potential strategy for the suppression of hypoxia-induced metastasis through the reversal of hypoxia-induced stem cell characteristics and EMT in cancer cells. Pristimerin down-regulates the expression of pro-inflammatory mediators through blocking of NF-κB activation by inhibiting interconnected ROS/IKK/NF-κB signaling pathways, can effectively inhibit both arthritic inflammation and cartilage and bone damage in the joints.

Pristimerin inhibits the activity of purified MGL with an IC50 of 93±8 nM and that of non-purified MGL (cell lysates of MGL-transfected HeLa cells) with an IC50 of 398±68 nM. Pristimerin inhibits MGL through a mechanism that is rapid, reversible and non-competitive. The binding of pristimerin to MGL might be strengthened by formation of a polar interaction with a regulatory cysteine, possibly Cys208. Pristimerin inhibits HFLS-RA and HUVEC cell viability in a dose- and time-dependent manner. Pristimerin decreases VEGF-induced autophosphorylation of VEGFR2 and attenuates the activation of the VEGF-induced VEGFR2-mediated signaling pathway .

Pristimerin inhibits inflammation and tumor angiogenesis. Pristimerin significantly reduces vessel density in synovial membrane tissues of inflamed joints and reduces the expression of pro-angiogenic factors in sera, including TNF-α, Ang-1, and MMP-9.

Pristimerin | Celastrol-methylether | UNII-28ZK7PR57S

Chromatin/Epigenetic

Sirtuin

NF-κB

Cancer

——

1258-84-0

464.64

C30H40O4

>98% (HPLC)

DMSO : 20 mg/mL 43.04 mM; H2O : < 0.1 mg/mL

CC1=C(C(=O)C=C2C1=CC=C3C2(CCC4(C3(CCC5(C4CC(CC5)(C)C(=O)OC)C)C)C)C)O

methyl (2S,4aS,6aR,12bR,14aR,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-carboxylate

(-20℃)

With Ice Pack

≥ 2 years