GGTI 298 TFA salt

製品コードS7466 バッチS746601

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₇H₃₃N₃O₃S.C₂HF₃O₂
	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
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	human lung carcinoma cell line Calu-1
	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.
動物実験	動物モデル	Nude mice
	投薬量	1.16 mg/kg
	投与方法	s.c.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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