化合物SBI-0640756 T5173

Product Introduction
Bioactivity


英文名: SBI-0640756

描述: SBI-0640756 (SBI-756) 是一种靶向 eIF4G1 并破坏 eIF4F 复合物的抑制剂。

细胞实验: Cells were rinsed with PBS and lysed as previously described. Protein concentration was determined using Coomassie Plus Protein Assay Reagent. Equal amounts of cell lysate proteins (50 μg) were separated on SDS-PAGE and transferred to polyvinylidene difluoride membranes. Membranes were blocked (5% BSA/TBST, 1 h) and incubated with primary antibodies (1 h at room temperate or overnight at 4°C), with shaking. Following three TBST washes, membranes were incubated for 1 h at room temperature secondary antibodies (1:10,000). Detection and quantifications were made using Odyssey Infrared Imaging System, or by exposing them to X-ray film. Antibodies against p-AKT, p-PRAS40, p-IKK, p-IκB, p-TSC, p-mTOR, p-p70S6K, p-RPS6, p-4E-BP1, pSGK3, AKT, PRAS40, IKK, IκB, mTOR, p70S6K, RPS6, 4E-BP1, GSK3, eIF4G1, and eIF4E were purchased from Cell Signaling Technology. Antibodies against β-actin and α-tubulin were obtained from Santa Cruz Biotechnology. Secondary antibodies were goat anti-rabbit Alexa-680 F(ab')2 and goat anti-mouse IRDye 800 F(ab')2. All antibodies were used according to the suppliers' recommendations.

体外活性: SBI-756 effectively dissociated eIF4G1 from the eIF4E in a dose-dependent manner, which was accompanied by a concomitant increase in 4E-BP1:eIF4E binding, reflective of impaired eIF4F complex formation. SBI-756 also inhibits the AKT/mTORC1 signaling and mTORC1 inhibition disrupts the eIF4F complex via activation of 4E-BPs. Whereas torin1 induced dissociation of eIF4G1 from eIF4E in WT but not in 4E-BP DKO MEFs, SBI-756 reduced eIF4G1:eIF4E association in both WT and 4E-BP DKO MEFs. Likewise, SBI-756 but not torin1 attenuated the proliferation of E1A/RAS-transformed 4E-BP DKO MEFs.

体内活性: Administration of SBI-756 only, starting 11 weeks after genetic inactivation of Ink4a and induction of NRasQ61E (about 10–14 days prior to tumor appearance), delayed tumor onset (from 20–26 weeks) and reduced tumor incidence, by 50%, compared with the control non-treated group. The growth of established tumors was largely inhibited by treatment with either BRAFi alone or a combination of BRAFi plus SBI-756.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : Insoluble
DMSO : 50 mg/mL (123.51 mM)


关键字: Autophagy | SBI-0640756 | Inhibitor | SBI 756 | SBI756 | Eukaryotic Initiation Factor (eIF) | inhibit | SBI0640756

相关产品: MK-28 | ISRIB (trans-isomer) | Briciclib | PERK-IN-6 | SHP099 | ATPγS tetralithium salt | BAY 2965501 | 4E1rcat | Vaccarin | Salubrinal

相关库: Anti-Aging Compound Library | Bioactive Compounds Library Max | Endoplasmic Reticulum Stress Compound Library | Inhibitor Library | Kinase Inhibitor Library | Apoptosis Compound Library | Autophagy Compound Library | Reprogramming Compound Library | NO PAINS Compound Library | Bioactive Compound Library

化合物SBI-0640756 T5173信息由TargetMol中国为您提供，如您想了解更多关于化合物SBI-0640756 T5173报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途