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Thapsigargin

ATPase inhibitor
 
BML-PE180-0001 1 mg 66.00 USD
 
BML-PE180-0005 5 mg 279.00 USD
Do you need bulk/larger quantities?
 
Replaces Prod. #: ALX-350-004

Cell permeable tumor promoter. Induces the release of intracellular stored Ca2+ without hydrolysis of inositolphospholipids via inhibition of the (sarco)endoplasmatic reticulum Ca2+-ATPase (SERCA) (IC50=30nM). Inhibition of SERCA reveals a significant change in intracellular Ca2+ homeostasis and pH regulation in tumor cells. May be used to distinguish between discrete intracellular Ca2+ pools. Thapsigargin-induced tumor promotion and down regulation of the EGF receptor is independent of PKC activation. Increases Ca2+-dependent Na+ influx in human platelets in a dose-dependent manner. Induces apoptosis. Stimulates nitric oxide (NO) production, contributing to hepatocyte apoptosis.

Product Specification

Formula:C34H50O12
 
MW:650.8
 
CAS:67526-95-8
 
MI:14: 9272
 
Purity:≥95% (HPLC)
 
Appearance:Colorless wax or white solid.
 
Solubility:Soluble in DMSO (20mg/ml), 100% ethanol (20mg/ml) or acetone.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Stable for at least 1 year after receipt when stored, as supplied, at -20°C.
 
Handling:USE CAUTION – product is a tumor promoter. Solutions may lose activity after one week. For longer term storage, dissolve in acetone or ethanol, aliquot and evaporate solvent to dryness with a stream of nitrogen or argon. Store aliquots of neat compound at -20°C or colder. Protect from light and oxygen.
 
Technical Info/Product Notes:Replacement for ADI-908-298.
 
350-004
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350-004

Product Literature References

Agonist-Mediated Activation of STING Induces Apoptosis in Malignant B Cells: C.A. Tang, et al.; Cancer Res. 76, 2137 (2016), Application(s): Stimulated cells, Abstract; Full Text
AMPK-independent inhibition of human macrophage ER stress response by AICAR: M. Boß, et al.; Sci. Rep. 6, 32111 (2016), Application(s): Cell culture, assessing ER stress responses in macrophages, Abstract; Full Text
Comparative effects of nodularin and microcystin-LR in zebrafish: 2. Uptake and molecular effects in eleuthero-embryos and adult liver with focus on endoplasmic reticulum stress: S. Faltermann, et al.; Aquat. Toxicol. 171, 77 (2016), Application(s): Positive control for ER-stress induction, Abstract;
HERPUD1 protects against oxidative stress-induced apoptosis through downregulation of the inositol 1,4,5-trisphosphate receptor: F. Paredes, et al.; Free Radic. Biol. Med. 90, 206 (2016), Application(s): Cell culture , Abstract;
Stromal Interaction Molecule 1 Rescues Store-Operated Calcium Entry and Protects NG115-401L Cells Against Cell Death Induced by Endoplasmic Reticulum and Mitochondrial Oxidative Stress: C. Zhang, et al.; Neurochem. Int. 97, 137 (2016), Application(s): Cell culture, Abstract;
Camphene isolated from essential oil of Piper cernuum (Piperaceae) induces intrinsic apoptosis in melanoma cells and displays antitumor activity in vivo: N. Girola, et al.; Biochem. Biophys. Res. Commun. 467, 928 (2015), Application(s): Cell Culture, Abstract;
ER localization is critical for DsbA-L to Suppress ER Stress and Adiponectin Down-Regulation in Adipocytes: M. Liu, et al.; J. Biol. Chem. 290, 10143 (2015), Application(s): Cell Culture, Abstract; Full Text
Stress of endoplasmic reticulum modulates differentiation and lipogenesis of human adipocytes: M. Koc, et al.; Biochem. Biophys. Res. Commun. 460, 684 (2015), Application(s): Cell Culture, Abstract;
Transient receptor potential canonical 1 (TRPC1) channels as regulators of sphingolipid- and VEGF receptor expression: implications for thyroid cancer cell migration and proliferation: M.Y. Asghar, et al.; J. Biol. Chem. 290, 16116 (2015), Application(s): Cell Culture, Abstract; Full Text
Unfolded protein response signaling by transcription factor XBP-1 regulates ADAM10 and is affected in Alzheimer's disease: S. Reinhardt, et al.; FASEB J. 28, 978 (2014), Abstract;
Autophagy-mediated insulin receptor down-regulation contributes to endoplasmic reticulum stress-induced insulin resistance: L. Zhou, et al.; Mol. Pharmacol. 76, 596 (2009), Abstract;
Thapsigargin, a selective inhibitor of sarco-endoplasmic reticulum Ca2+ -ATPases, modulates nitric oxide production and cell death of primary rat hepatocytes in culture: N.K. Canova, et al.; Cell Biol. Toxicol. 23, 337 (2007), Abstract;
Changes in intracellular Ca2+ and pH in response to thapsigargin in human glioblastoma cells and normal astrocytes: G.G. Kovacs, et al.; Am. J. Physiol. Cell. Physiol. 289, C361 (2005), Abstract;
Thapsigargin induces a calmodulin/calcineurin-dependent apoptotic cascade responsible for the death of prostatic cancer cells: B. Tombal, et al.; Prostate 43, 303 (2000), Abstract;
Thapsigargin induces apoptosis in cultured human aortic smooth muscle cells: C. Peiro, et al.; J. Cardiovasc. Pharmacol. 36, 676 (2000), Abstract;
Nitric oxide is involved in apoptosis induced by thapsigargin in rat mesangial cells: A.M. Rodriguez-Lopez, et al.; Cell Physiol. Biochem. 9, 285 (1999), Abstract;
Signal transduction of thapsigargin-induced apoptosis in osteoblast: H.J. Chae, et al.; Bone 25, 453 (1999), Abstract;
Baculovirus p35 and Z-VAD-fmk inhibit thapsigargin-induced apoptosis of breast cancer cells: X.M. Qi, et al.; Oncogene 15, 1207 (1997), Abstract;
Role of EGR-1 in thapsigargin-inducible apoptosis in the melanoma cell line A375-C6: S. Muthukkumar, et al.; Mol. Cell. Biol. 15, 6262 (1995), Abstract; Full Text
Intracellular Ca2+ signals activate apoptosis in thymocytes: studies using the Ca(2+)-ATPase inhibitor thapsigargin: S. Jiang, et al.; Exp. Cell Res. 212, 84 (1994), Abstract;
The role of calcium, pH, and cell proliferation in the programmed (apoptotic) death of androgen-independent prostatic cancer cells induced by thapsigargin: Y. Furuya, et al.; Cancer Res. 54, 6167 (1994), Abstract;
Thapsigargin, a Ca(2+)-ATPase inhibitor, depletes the intracellular Ca2+ pool and induces apoptosis in human hepatoma cells: A. Tsukamoto & Y. Kaneko; Cell Biol. Int. 17, 969 (1993), Abstract;
Brefeldin A, thapsigargin, and AIF4- stimulate the accumulation of GRP78 mRNA in a cycloheximide dependent manner, whilst induction by hypoxia is independent of protein synthesis: B.D. Price, et al.; J. Cell. Physiol. 152, 545 (1992), Abstract;
Demonstration of two forms of calcium pumps by thapsigargin inhibition and radioimmunoblotting in platelet membrane vesicles: B. Papp, et al.; J. Biol. Chem. 266, 14593 (1991), Abstract;
Identification of intracellular calcium pools. Selective modification by thapsigargin: J.H. Bian, et al.; J. Biol. Chem. 266, 8801 (1991), Abstract;
Thapsigargin, a tumor promoter, discharges intracellular Ca2+ stores by specific inhibition of the endoplasmic reticulum Ca2(+)-ATPase: O. Thastrup, et al.; Proc. Natl. Acad. Sci. USA 87, 2466 (1990), Abstract;
Activation of calcium entry by the tumor promoter thapsigargin in parotid acinar cells. Evidence that an intracellular calcium pool and not an inositol phosphate regulates calcium fluxes at the plasma membrane: H. Takemura, et al.; J. Biol. Chem. 264, 12266 (1989), Abstract;
Phosphorylation at threonine-654 is not required for negative regulation of the epidermal growth factor receptor by non-phorbol tumor promoters: B.A. Friedman, et al.; Proc. Natl. Acad. Sci. USA 86, 812 (1989), Abstract;
A novel tumour promoter, thapsigargin, transiently increases cytoplasmic free Ca2+ without generation of inositol phosphates in NG115-401L neuronal cells: T.R. Jackson, et al.; Biochem. J. 253, 81 (1988), Abstract;
Thapsigargin, a novel promoter, phosphorylates the epidermal growth factor receptor at threonine 669: K. Takishima, et al.; Biochem. Biophys. Res. Commun. 157, 740 (1988), Abstract;
Palytoxin is a non-12-O-tetradecanoylphorbol-13-acetate type tumor promoter in two-stage mouse skin carcinogenesis: H. Fujiki, et al.; Carcinogenesis 7, 707 (1986), Abstract;

General Literature References

A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca(2+)-ATPases: M. Treiman, et al.; TIPS 19, 131 (1998), (Review), Abstract;
The sarcoplasmic reticulum Ca2+ pump: inhibition by thapsigargin and enhancement by adenovirus-mediated gene transfer: G. Inesi, et al.; Ann. NY Acad. Sci. 853, 195 (1998), (Review), Abstract; Full Text
Use of thapsigargin to study Ca2+ homeostasis in cardiac cells: T.B. Rogers, et al.; Biosci. Rep. 15, 341 (1995), (Review), Abstract;
Thapsigargin, a high affinity and global inhibitor of intracellular Ca2+ transport ATPases: G. Inesi and Y. Sagara; Arch. Biochem. Biophys. 298, 313 (1992), (Review), Abstract;
Role of Ca2(+)-ATPases in regulation of cellular Ca2+ signalling, as studied with the selective microsomal Ca2(+)-ATPase inhibitor, thapsigargin: O. Thastrup; Agents Actions 29, 8 (1990), (Review), Abstract;

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