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Didesmethylrocaglamide

CAS No. : 177262-30-5

MCE 站：Didesmethylrocaglamide

产品活性：Didesmethylrocaglamide 是一种 Rocaglamide 的衍生物，也是一种有效的真核起始因子 4A (eIF4A) 抑制剂。Didesmethylrocaglamide 具有有效的生长抑制活性，IC₅₀ 为 5 nM。Didesmethylrocaglamide 抑制多种促进生长的信号通路，并诱导肿瘤细胞凋亡 (apoptosis)。抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：Eukaryotic Initiation Factor (eIF)  |  Apoptosis

In Vitro: Didesmethylrocaglamide (5 nM, and 10 nM; 72 hours; MPNST cells) treatment arrests MPNST cells at G2-M, increases the sub-G1 population, induces cleavage of caspases and PARP, and elevates the levels of the DNA-damage response marker γH2A.X, while decreasing the expression of AKT and ERK1/2.
Didesmethylrocaglamide inhibits MPNST cell proliferation by inducing cell cycle arrest at G2/M and subsequently, cell death. Didesmethylrocaglamide-treated 697-R cells exhibits IC₅₀ values is very similar to those of parental 697 cells (4 vs 3nM of IC₅₀, respectively).
Didesmethylrocaglamide induces apoptosis in both neurofibromatosis type 1 (NF1)-expressing and NF1-deficient MPNST cells, possibly subsequent to the activation of the DNA damage response. Didesmethylrocaglamide-treated sarcoma cells show decreased levels of multiple oncogenic kinases, including insulin-like growth factor-1 receptor.

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