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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C27H33N3O3S.C2HF3O2 |
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分子量 | 593.66 | CAS No. | 1217457-86-7 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (168.44 mM) | ||||||||
Ethanol | 100 mg/mL (168.44 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | GGTI 298 is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis. |
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in vitro | The geranylgeranyltransferase I inhibitor GGTI-298 has been shown to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis. Treatment of the human lung carcinoma cell line Calu-1 with GGTI-298 results in inhibition of the phosphorylation of retinoblastoma protein, a critical step for G1/S transition. The kinase activities of two G1/S cyclin-dependent kinases, CDK2 and CDK4, are inhibited in Calu-1 cells treated with GGTI-298. GGTI-298 has little effect on the expression levels of CDK2, CDK4, CDK6, cyclins D1 and E, but decreases the levels of cyclin A. GGTI-298 increases the levels of the cyclin-dependent kinase inhibitors p21 and p15 and had little effect on those of p27 and p16. GGTI-298 promotes binding of p21 and p27 to CDK2 while decreasing their binding to CDK6. Its treatment results in an increased binding of p15 to CDK4, which is paralleled with decreased binding to p27. Pretreatment of fibroblasts with GGTI-298, blocks PDGF- and epidermal growth factor-dependent tyrosine phosphorylation of their corresponding tyrosine kinase receptors. GGTI-298 has antiproliferative effects on fibroblasts, epithelial, and smooth muscle cells, and this cell growth inhibition appears to be mediated through a G1 phase arrest[1]. |
in vivo | GGTI-298 inhibits tumor growth in nude mice[3]. |
細胞アッセイ | 細胞株 | human lung carcinoma cell line Calu-1 |
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濃度 | 15 μM | |
反応時間 | 48 h | |
実験の流れ | Cells were treated with GGTI-298 (15 μM) for 48 h, harvested, and lysed in HEPES lysis buffer. Proteins were then resolved by 12.5% or 7% SDS-PAGE gel and immunoblotted with antibodies. The ECL blotting system was used for detection of positive antibody reactions. |
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動物実験 | 動物モデル | Nude mice |
投薬量 | 1.16 mg/kg | |
投与方法 | s.c. |
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Cholesterol biosynthesis inhibition synergizes with AKT inhibitors in triple-negative breast cancer [ bioRxiv, 2024, 10.1101/2024.01.16.575899] | PubMed: none |
Epigenetic suppression of PGC1α (PPARGC1A) causes collateral sensitivity to HMGCR-inhibitors within BRAF-treatment resistant melanomas [ Nat Commun, 2023, 14(1):3251] | PubMed: 37277330 |
Mevalonate Pathway-mediated ER Homeostasis Is Required for Haploid Stability in Human Somatic Cells [ Cell Struct Funct, 2021, 46(1):1-9] | PubMed: 33361684 |
Cellular basis underlying the intolerance to haploidy in vertebrates [ HOKKAIDO UNIVERSITY, 2021, 10.14943/doctoral.k14392] | PubMed: None |
Depletion of essential isoprenoids and ER stress induction following acute liver-specific deletion of HMG-CoA reductase [ J Lipid Res, 2020, 61(12):1675-1686] | PubMed: 33109681 |
LUBAC controls chromosome alignment by targeting CENP-E to attached kinetochores [ Nat Commun, 2019, 10(1):273] | PubMed: 30655516 |
FBXW7 regulates endothelial barrier function by suppression of the cholesterol synthesis pathway and prenylation of RhoB [ Mol Biol Cell, 2019, 30(5):607-621] | PubMed: 30601691 |
Inhibition of YAP reverses primary resistance to EGFR inhibitors in colorectal cancer cells. [ Oncol Rep, 2018, 40(4):2171-2182] | PubMed: 30106444 |
Inhibition of YAP reverses primary resistance to EGFR inhibitors in colorectal cancer cells [ Oncol Rep, 2018, 40(4):2171-2182] | PubMed: 30106444 |
Palmitoylated SCP1 is targeted to the plasma membrane and negatively regulates angiogenesis [ Elife, 2017, 6e22058] | PubMed: 28440748 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。