Thapsigargin |
カタログ番号GC11482
One-Click Copy Product Info
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ThapsigarginはThapsia garganicaから単離されたセスキテルペンラクトンであり、不可逆的なサルコ/小胞体Ca²⁺-ATPase（SERCA）阻害剤として作用する。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 67526-95-8
Sample solution is provided at 25 µL, 10mM.
ThapsigarginはThapsia garganicaから単離されたセスキテルペンラクトンであり、不可逆的なサルコ/小胞体Ca²⁺-ATPase（SERCA）阻害剤として作用する。Thapsigarginは、SERCAを阻害することで細胞内カルシウムの貯蔵量を枯渇させ、よって折り畳まれないタンパク質応答（UPR）とATF3/ATF4経路を活性化する。このプロセスは、腫瘍細胞でアポトーシスを誘発するか、または宿主細胞で広いスペクトルの抗ウイルス状態を惹起する。同時に、カルシウム恒常性異常により、複数のストレスシグナルが活性化され、よって炎症性とオートファジー反応が増幅する。Thapsigarginは、腫瘍の治療、広いスペクトルの抗ウイルス応用（COVID-19など）に関する研究に使える[1-4]。
In vitro（体外）実験で、HT29、HCT116とSW1116大腸癌細胞を0.1μMまたは10μMのThapsigarginで24時間処理したところ、細胞死が誘発された[5]。β-TC-6膵臓β細胞を0.1μMのThapsigarginで24時間処理したところ、アポトーシスが誘発された[6]。MH7Aヒト関節リウマチの滑膜細胞を0.001μM、0.1μMまたは1μMのThapsigarginで2または4日間処理したところ、時間と用量依存的に、細胞の増殖が阻害され、アポトーシスが誘発された[7]。
In vivo（体内）実験で、AOM/DSS誘発性大腸炎の雄Swissアルビノマウス（10週齢）に、1mg/kg Thapsigarginを5週間連続的に、週に一回腹腔内注射した。Thapsigarginは、体重減少と疾患活性指数スコアを軽減し、結腸の重量-長さの比を低下させ、結腸腫瘍数と異常陰窩巣の形成を減らし、結腸上皮の超微細構造と組織の構造を改善した[8]。SW-13ヒト副腎皮質癌細胞を皮下接種した雄のBALB/cヌードマウスに、1mg/kg Thapsigarginを15日間、毎日腹腔内注射した。Thapsigarginは、異種移植腫瘍の増殖を阻害し、腫瘍の体積と重量を減らし、マウスの体重を影響しなかった[9]。
| 細胞実験 [1]: | |
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細胞株 |
β-TC-6細胞（マウス膵臓β細胞株） |
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調製方法 |
15%のウシ胎児血清を添加したDulbecco's改変Eagles'培地（DMEM）で培養した。細胞を48時間血清欠乏させ、その後は0.1μMのThapsigarginで24時間処理した。 |
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反応条件 |
0.1μM；24時間 |
|
応用 |
Thapsigarginにより、β-TC-6細胞のアポトーシスが誘発され、切断型カスパーゼ-3の含有量が増えた。 |
| 動物実験 [2]: | |
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動物モデル |
雄BALB/cヌードマウス（4-5週齢；20-22g）；200 μLの培地の中の2×10⁶ SW-13ヒト副腎皮質癌細胞を各マウスの左肩に注射することで皮下副腎皮質異種移植モデルを作製した。 |
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調製方法 |
皮下腫瘍が約0.2×0.2cm²のサイズに増殖した時、マウスに、Thapsigargin（1mg/kg）と溶媒（0.5%のメチルセルロース）を毎日腹腔内注射した。マウスの体重と腫瘍のサイズを定期的に記録し、15日後、異種移植腫瘍組織を採取した。 |
|
剤形 |
1mg/kg；腹腔内注射；15日間、毎日 |
|
応用 |
ThapsigarginはSW-13異種移植腫瘍の増殖を阻害し、腫瘍の体積と重量を減らし、溶媒群と比べ、マウスの体重の著しい変化はなかった。異種移植腫瘍組織で、p-JNK、p-ERK、p-MAPK、p-PERK、IRE1とGRP78タンパク質のレベルが上方制御され、JNK、ERK、PERKとMAPKの総タンパク質レベルは変わらぬままであった。 |
| Cas No. | 67526-95-8 | SDF | |
| Chemical Name | (3S,3aR,4S,6S,6aR,7S,8S,9bS)-6-acetoxy-4-(butyryloxy)-3,3a-dihydroxy-3,6,9-trimethyl-8-(((Z)-2-methylbut-2-enoyl)oxy)-2-oxo-2,3,3a,4,5,6,6a,7,8,9b-decahydroazuleno[4,5-b]furan-7-yl octanoate | ||
| Canonical SMILES | O[C@@]([C@H]1OC(CCC)=O)([C@]2(C)O)[C@H](C([C@H]([C@@H]3OC(CCCCCCC)=O)[C@@](C1)(C)OC(C)=O)=C(C)[C@@H]3OC(/C(C)=C\C)=O)OC2=O | ||
| Formula | C34H50O12 | M.Wt | 650.76 |
| 溶解度 | 30mg/ml in ethanol, DMSO, DMF | Storage | Store at -20°C, sealed storage, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5367 mL | 7.6833 mL | 15.3666 mL |
| 5 mM | 307.3 μL | 1.5367 mL | 3.0733 mL |
| 10 mM | 153.7 μL | 768.3 μL | 1.5367 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
RHBDF1 is critical for maintaining BiP protein stability in breast cancer cells.c, d BiP levels in MCF-7 cells (MT or R1KO) treated with Thapsigargin (TG, 10 μM).
When the cells were further treated with thapsigargin (TG)(GlpBio), an ER stress inducer, the BiP protein level progressively increased in the control cells; however, this increase was significantly slower in R1KO cells
Acta Pharmacol Sin (2023): 1-13. PMID: 37798352 IF: 8.1996 -
Related Biological Data
SPC alleviates AngII-induced cardiac hypertrophy by inhibiting CaM. c, d, g, h Surface area of CMs was determined by TRITC Phalloidin staining and data analysis.
To explore whether SPC inhibits Ang II-induced cardiac hypertrophy through its interactions with CaM, we conducted an in vitro experiment by treating cells with siCaM and TG(GlpBio) to decrease or increase CaM levels, respectively.
Acta Pharmacol Sin (2023): 1-15. PMID: 37833535 IF: 8.1996 -
Related Biological Data
DAPA inhibited ER stress in Ang II-induced cardiomyocytes. a, b The protein levels of Bcl-2, Bax, and cleaved caspase 3 in each group were detected.
To confirm whether the DAPA-induced inhibition of ERS attenuates Ang II-induced apoptosis, we used TG to activate ERS and measured the levels of apoptosis biomarkers, including Bcl-2,cleaved caspase 3, and Bax.
Acta Pharmacol Sin (2021): 1-12. PMID: 34853445 IF: 6.152 -
Related Biological Data
TG and 3-MA treatment partially restores SEEC function after BMS30940 suppression of FABP4 (a, b) Expression levels of key proteins in the endoplasmic reticulum stress signaling pathway after combined treatment with hormones, BMS309403, and TG.
In the case of TG (1 μM)(Glpbio) or 3-MA (5 mM) treatment groups, TG and 3-MA were added 1 h prior to the addition of IFN-τ. The total treatment duration for all cells was 24 h.
J Reprod Develop (2023). PMID: 37779094 IF: 1.7998
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