SML4175
TH-Z145
≥90% (HPLC), powder, geranylgeranyl diphosphate synthase inhibitor
别名:
(2-(3-(Octyloxy)phenyl)ethane-1,1-diyl)bis(phosphonic acid), P,P′-[2-[3-(Octyloxy)phenyl]ethylidene]bis[phosphonic acid]
质量水平
方案
≥90% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
O=P(O)(C(P(O)(O)=O)CC1=CC(OCCCCCCCC)=CC=C1)O
一般描述
TH-Z145 is a potent and selective geranylgeranyl diphosphate synthase(GGPPS) inhibitor (IC50 = 210 nM; FPPS IC50 > 30 µM) that stimulates immune responses by blocking the mevalonate (MVA) pathway-mediated post-translational protein geranylgeranylation. When co-administered with antigen in mice in vivo, TH-Z145 triggers strong adjuvant responses, increasing OVA-specific antibody titres (in mice immunized with 100 μg OVA + 100 μgTH-Z145) and protecting against death caused by live influenza virus PR8 challenge (in mice immunized with 5 μg PR8 HA1 subunit containing TH-Z145). TH-Z145 adjuvant efficacy is blocked by GGPP and synergized with HMG-CoA inhibitor simvastatin.
应用
TH-Z145 may be usedas a research tool in studies investigating the mevalonate pathway and itsimplications in various biological processes, including cancer andinflammation. It may also be used as a potent vaccine adjuvant to enhanceimmune responses by targeting the mevalonate pathway to improve the efficacy ofvaccines.
生化/生理作用
Potent and selective mevalonate (MVA) pathway geranylgeranyl diphosphate synthase (GGPPS) inhibitor that stimulates immune responses in vivo.
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Chenchen Guo et al.
Nature cancer, 3(5), 614-628 (2022-04-23)
Small cell lung cancer (SCLC) lacks effective treatments to overcome chemoresistance. Here we established multiple human chemoresistant xenograft models through long-term intermittent chemotherapy, mimicking clinically relevant therapeutic settings. We show that chemoresistant SCLC undergoes metabolic reprogramming relying on the mevalonate
Statin-induced Mitochondrial Priming Sensitizes Multiple Myeloma Cells to BCL2 and MCL-1 Inhibitors.
Dennis Juarez et al.
Cancer research communications, 3(12), 2497-2509 (2023-11-13)
The BCL2 inhibitor venetoclax promotes apoptosis in blood cancer cells and is approved for treatment of chronic lymphocytic leukemia and acute myeloid leukemia. However, multiple myeloma cells are frequently more dependent on MCL-1 for survival, conferring resistance to venetoclax. Here
Yun Xia et al.
Cell, 175(4), 1059-1073 (2018-10-03)
Motivated by the clinical observation that interruption of the mevalonate pathway stimulates immune responses, we hypothesized that this pathway may function as a druggable target for vaccine adjuvant discovery. We found that lipophilic statin drugs and rationally designed bisphosphonates that
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