Thapsigargin

製品コードS7895 バッチS789501

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₃₄H₅₀O₁₂
	分子量	650.75	CAS No.	67526-95-8
Solubility (25°C)*	体外	DMSO	100 mg/mL (153.66 mM)
		Ethanol	100 mg/mL (153.66 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	Thapsigargin is a potent, non-competitive inhibitor of the sarco/endoplasmic reticulum Ca²⁺ ATPase (SERCA) with IC50 of 0.353 nM or 0.448 nM for the carbachol-evoked [Ca2+]i-transients with or without a KCl-prestimulation. Thapsigargin induces cell apoptosis. Thapsigargin is extracted from a plant, Thapsia garganica.
in vitro	In human SH-SY5Y neuroblastoma cells, two distinct intracellular Ca²⁺ stores, a KCl-/caffeine-sensitive and a carbachol-/IP₃-sensitive store, are demonstrated previously. Thapsigargin (0.05 nM–20 μM) induces a [Ca²⁺]_i-transient. Thapsigargin inhibits the carbachol-evoked [Ca²⁺]_i-transients with (IC50 = 0.353 nM) or without (IC50 = 0.448 nM) a KCl-prestimulation.^[1] Thapsigargin is effective in inducing Endoplasmic Reticulum (ER) stress in hepatocytes.^[3]
in vivo	TG at a dose of 0.5 ug/g/body weight is safe and does not elicit any adverse effects on survival in mice. TG treatment in mice results in significant expression of ER stress markers ATF6 and eIF2α in adipose tissue. TG treatment in mice fails to induce the expression of most ER stress and UPR proteins in the liver.^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human SH-SY5Y neuroblastoma cells
	濃度	0.05 nM–20 μM
	反応時間	5 min
	実験の流れ	The TG-treatment is conducted in several different modes as follows: (1) Applied prior to any stimulus: After a 5-min preincubation with 1.5 mM CaCl2, TG in different concentrations (0.05 nM–20 μM) is added to the cell suspension and the mixture is then incubated for further 5 min at 37 ℃. Stimulation starts with 100 mM KCl followed by 1 mM CAB or vice versa. (2) Applied between two stimuli: TG is added to cell suspension after the Ca²⁺-transient evoked by the first stimulant (100 mM KCl or 1 mM CAB) has reached its steady state. 5 min after the TG-addition, cells are then challenged for the second time by 1 mM CAB or 100 mM KCl. (3) Applied briefly after the first (KCl- or CAB-) stimulation: In this treatment mode, TG is added briefly ( ~ 10 s) after the first stimulant (100 mM KCl or 1 mM CAB) is applied, before the evoked [Ca²⁺]_i-transient reaches a new steady state. The second stimulant (1 mM CAB or 100 mM KCl) is then applied 5 min after the TG-addition. (4) Applied briefly after the second stimulation: In the CAB→KCl stimulation mode, TG is added briefly ( ~ 10 s) after the second stimulant, i.e. 100 mM KCl.
動物実験	動物モデル	Male Balb/c mice
	投薬量	0.5 mg/kg
	投与方法	IP

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：

TANGO6 regulates cell proliferation via COPI vesicle-mediated RPB2 nuclear entry [ Nat Commun, 2024, 15(1):2371]	PubMed: 38490996
Stress granules affect the dual PI3K/mTOR inhibitor response by regulating the mitochondrial unfolded protein response [ Cancer Cell Int, 2024, 24(1):38]	PubMed: 38238825
ER stress induces caspase-2-tBID-GSDME-dependent cell death in neurons lytically infected with herpes simplex virus type 2 [ EMBO J, 2023, e113118.]	PubMed: 37646198
Combination of RUNX1 inhibitor and gemcitabine mitigates chemo-resistance in pancreatic ductal adenocarcinoma by modulating BiP/PERK/eIF2α-axis-mediated endoplasmic reticulum stress [ J Exp Clin Cancer Res, 2023, 42(1):238]	PubMed: 37697370
Combination of RUNX1 inhibitor and gemcitabine mitigates chemo-resistance in pancreatic ductal adenocarcinoma by modulating BiP/PERK/eIF2α-axis-mediated endoplasmic reticulum stress [ J Exp Clin Cancer Res, 2023, 42(1):238]	PubMed: 37697370
HRS mediates tumor immune evasion by regulating proteostasis-associated interferon pathway activation [ Cell Rep, 2023, 10.1016/j.celrep.2023.113352]	PubMed: 37948180
Porcine reproductive and respiratory syndrome virus infection triggers autophagy via ER stress-induced calcium signaling to facilitate virus replication [ PLoS Pathog, 2023, 19(3):e1011295]	PubMed: 36972295
Simultaneous proteome localization and turnover analysis reveals spatiotemporal dynamics of unfolded protein responses [ bioRxiv, 2023, 2023.01.04.521821]	PubMed: 36711879
Protein palmitoylation-mediated palmitic acid sensing causes blood-testis barrier damage via inducing ER stress [ Redox Biol, 2022, 54:102380]	PubMed: 35803125
Silica nanoparticles induce cardiac injury and dysfunction via ROS/Ca2+/CaMKII signaling [ Sci Total Environ, 2022, 837:155733]	PubMed: 35526619

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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