SRJ-23

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

穿心莲内酯的一种新型半合成衍生物，直接靶向 Ras，阻断 GDP 与 GTP 的交换，从而防止 Ras 激活。

A novel semisynthetic derivative of andrographolide that directly target Ras to block the exchange of GDP for GTP and thus prevent Ras activation; significantly suppresses K-Ras GTP loading, whereas H-Ras and N-Ras GTP loading are much less sensitive; reduceds K-RasG12V GTP, phosphorylated ERK (ppERK) levels in K-RasG12V-transformed cells; induces G1 arrest and apoptosis in MCF-7 and HCT-116 cells, respectively.

KKL-35 exhibits broad-spectrum antibiotic activity. KKL-35 prevents growth of B. anthracis and M. smegmatis with minimum inhibitory concentration (MIC) values of less than 6 μM. KKL-35 inhibit trans-translation at some step before proteolysis of tagged proteins. KKL-35 inhibits tagging of DHFR-ns. A large amount of untagged DHFR is produced in reactions with the highest concentrations of KKL-35, indicating that KKL-35 does not inhibit translation. KKL-35 prevents growth of WT S. flexneri with a MIC of 6 μM, and addition of KKL-35 to a growing culture of S. flexneri stops growth. In an S. flexneri strain expressing ArfA and deleted for ssrA, addition of KKL-35 has little effect on viability or growth rate. KKL-35 inhibits the growth of E. coli ?tolC, which is deficient in small molecule efflux, with an MIC of 0.3 μM.

Evidence suggest that the in vivo effects of KKL-35 are caused by inhibition of the release of nonstop translation complexes by trans-translation. KKL-35 inhibits trans-translation and prevents growth of S. flexneri strains that require trans-translation. The correlation between inhibition of trans-translation and growth is supported by genetic and pharmacological experiments showing that alternative mechanisms to release nonstop translation complexes relieve the growth suppression of KKL-35.

SRJ23 | SRJ 23

MAPK/ERK Signaling

Ras

trans-translationtaggingreaction

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865285-29-6

317.704

C15H9ClFN3O2

>98% (HPLC)

DMSO: Soluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(NC1=NN=NN1CCC)C2=CC=CC(Cl)=C2

4-Chloro-N-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-benzamide

(-20℃)

With Ice Pack

≥ 2 years