Inhibitor

1232

Wortmannin

$89.00
Information
MW: 
428.44
Solubility: 
Soluble to 50 mM in DMSO and to 5 mM in ethanol
Activity: 

Potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM). Also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).

Use & Storage
Storage: 
Desiccate at -20°C
Literature
References: 

Arcaro and Wymann (1993) Wortmannin is a potent phophatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol 3,4,5-trisphosphate in neutrophil responses. Biochem.J. 296 297. PMID: 8257416.

Powis et al (1994) Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase. Cancer Res. 542419. PMID: 8162590.

Schultz et al (1995) In vitro and in vivo antitumor activity of the phosphatidylinositol-3-kinase inhibitor wortmannin. Anticancer Res. 15 1135. PMID: 7653991.

Liu et al (2005) Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalian polo-like kinase. Chem.Biol. 12 99. PMID: 15664519.

UK Price: 
65 199
Euro Price: 
95 305
CHF Price: 
105 380
SKK Price: 
800 2655
DKK Price: 
650 2260
NOK Price: 
725 2330

3516

Tunicamycin

$155.00
Information
MW: 
844.95
Solubility: 
Soluble to 50 mM in DMSO
Activity: 

 

Antibiotic; inhibits GlcNAc phosphotransferase (GPT). Blocks the formation of N-glycosidic linkages by inhibiting the first step in glycoprotein synthesis. Activity induces ER stress and causes G1 arrest; can be used to induce autophagy. Tunicamycin contains four main components as follows:

  • Homolog A, n=8, C37H60N4O16, molecular weight = 816.90
  • Homolog B, n=9, C38H62N4O16, molecular weight = 830.93
  • Homolog C, n=10, C39H64N4O16, molecular weight = 844.95
  • Homolog D, n=11, C40H66N4O16, molecular weight = 858.99

The composition of this product will vary from batch to batch and can be found on the relevant certificate of analysis.

Use & Storage
Storage: 
Store at +4°C
Literature
References: 

Ding et al (2007) Differential effects of endoplasmic reticulum stress-induced autophagy on cell survival. J.Biol.Chem. 282 4702. PMID: 17135238.

Duriez et al (2008) The hepatitis B virus precore protein is retrotransported from endoplasmic reticulum (ER) to cytosol through the ER-associated pathway. J.Biol.Chem. 283 32352. PMID: 18805786.

Lauer et al (2009) Primary murine airway smooth muscle cells exposed to poly(I:C) or tunicamycin synthesize a leukocyte-adhesive hyaluronan matrix. J.Biol.Chem. 284 5299. PMID: 19088077.

UK Price: 
340
Euro Price: 
160
CHF Price: 
185
SKK Price: 
1390
DKK Price: 
145
NOK Price: 
1240

1138

Thapsigargin

$99.00
Information
MW: 
650.76
Purity: 
>97%
Solubility: 
Soluble to 100 mM in DMSO
Activity: 

Potent inhibitor of sarco-endoplasmic reticulum Ca2+-ATPases. Causes ER stress; can be used to induce autophagy in mammalian cells.

Use & Storage
Storage: 
Desiccate at -20°C
Literature
References: 

 

Davidson and Varhol (1995) Kinetics of thapsigargin-Ca2+-ATPase (sarcoplasmic reticulum) interaction reveals a two-step binding mechanism and picomolar inhibition. J.Biol.Chem. 270 11731. PMID: 7744817.

Treiman et al (1998) A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca2+-ATPases. TiPS 19 131. PMID: 9612087.

Yu et al (1998) Specific substitutions at amino acid 256 of the sarcoplasmic/endoplasmic reticulum Ca2+ transport ATPase mediate resistance to thapsigargin in thapsigargin-resistant hamster cells. J.Biol.Chem. 273 3542. PMID:9452480.

Ding et al (2007) Differential effects of endoplasmic reticulum stress-induced autophagy on cell survival. J.Biol.Chem. 282 4702. PMID: 17135238.

UK Price: 
340
Euro Price: 
110
CHF Price: 
130
SKK Price: 
955
DKK Price: 
800
NOK Price: 
850

1097

Taxol

$125.00
Information
MW: 
853.92
Purity: 
>99%
Solubility: 
Soluble to 25 mM in ethanol and to 100 mM in DMSO
Activity: 

Antitumor agent; promotes and stabilizes tubulin polymerization, causing cell cycle arrest. Induces autocatalytic activation of caspase-10 in CCRF-HSB-2 cells, triggering apoptosis.

Use & Storage
Storage: 
Store at +4°C
Literature
References: 

Merck Index 12 7117.

McGuire et al (1989) Taxol: a unique antineoplastic agent with significant activity in advanced ovarian epithelial neoplasms. Ann.Intern.Med. 111 273. PMID: 2569287.

Rowinsky et al (1990) Taxol: a novel investigational antimicrotubule agent. J.Natl.Cancer Inst. 82 1247. PMID:1973737.

Rao et al (1999) Characterization of the taxol binding site on the microtubule. J.Biol.Chem. 274 37990. PMID:10608867.

Park et al (2004) Taxol induces caspase-10-dependent apoptosis. J.Biol.Chem. 279 51057. PMID: 15452117.

UK Price: 
79 269
Euro Price: 
125 415
CHF Price: 
145 525
SKK Price: 
1090 37-5
DKK Price: 
905 3115
NOK Price: 
960 3215

1370

Sphingosine-1-phosphate

$169.00
Information
MW: 
379.48
Purity: 
>98%
Activity: 

Endogenous second messenger involved in the control of cell proliferation and motility, and Ca2+ mobilization. Acts as an agonist at sphingosine-1-phosphate receptors (S1P1-5) and as an activator of GPR3, GPR6 and GPR12. Effectors regulated include p38 MAP kinase, PLC, adenylyl cyclase, myosin light chain phosphatase and focal adhesion kinase.

Use & Storage
Storage: 
Desiccate at +4°C
Literature
References: 

van Koppen et al (1996) Activation of a high affinity Gi protein-coupled plasma membrane receptor by sphingosine-1-phosphate. J.Biol.Chem. 271 2082. PMID: 8567663.

Pyne and Pyne (2000) Sphingosine 1-phosphate signalling via the endothelial differentiation gene family of G-protein-coupled receptors. Pharmacol.Ther. 88 115. PMID: 11150592.

Essler et al (2002) Sphingosine 1-phosphate dynamically regulates myosin light chain phosphatase activity in human endothelial cells. Cell.Signal. 14 607. PMID: 11955953.

Uhlenbrock et al (2002) Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors. Cell.Signal. 14 941. PMID: 12220620.

UK Price: 
340
Euro Price: 
170
CHF Price: 
195
SKK Price: 
1480
DKK Price: 
1200
NOK Price: 
1275

1418

Resveratrol

$105.00
Information
MW: 
228.25
Purity: 
>98%
Solubility: 
Soluble to 100 mM in ethanol and to 100 mM in DMSO
Activity: 

A phytoestrogen with antitumor, antioxidant, antiplatelet, anti-inflammatory and antifungal effects. Inhibits cytochrome P450 1A1 (IC50 = 23 μM) and displays mixed agonist/antagonist actions at ERα and ERβ estrogen receptors. Converted into the anticancer agent piceatannol (Cat. No. 1554) by cytochrome P450 1B1.

Use & Storage
Storage: 
Desiccate at +4°C
Literature
References: 

Kimura et al (1985) Effects of stilbenes on arachidonate metabolism in leukocytes. Biochim.Biophys.Acta 834 275. PMID: 3922423.

Chun et al (1999) Resveratrol is a selective human cytochrome P450 1A1 inhibitor. Biochem.Biophys.Res.Commun.262 20. PMID: 10448061.

Bowers et al (2000) Resveratrol acts as a mixed agonist/antagonist for estrogen receptors α and β. Endocrinology 141 3657. PMID: 11014220.

Fremont (2000) Biological effects of resveratrol. Life Sci. 66 663. PMID: 10680575.

Baur and Sinclair (2006) Therapeutic potential of resveratrol: the in vivo evidence. Nat.Rev.Drug Discov. 5 493. PMID: 16732220.

UK Price: 
340
Euro Price: 
105
CHF Price: 
115
SKK Price: 
905
DKK Price: 
735
NOK Price: 
805

1292

Rapamycin

$255.00
Information
MW: 
914.18
Purity: 
>98%
Activity: 

Antifungal and immunosuppressant. Specific inhibitor of mTOR (mammalian target of Rapamycin). Complexes with FKBP-12 and binds mTOR inhibiting its activity. Inhibits interleukin-2-induced phosphorylation and activation of p70 S6 kinase. Induces autophagy in yeast and mammalian cell lines.

Use & Storage
Storage: 
Desiccate at -20°C
Literature
References: 

Kuo et al (1992) Rapamycin selectively inhibits interleukin-2 activation of p70 S6 kinase. Nature 358 70. PMID:1614535.

Huang et al (2003) Rapamycins: mechanism of action and cellular resistance. Cancer Biol.Ther. 2 221. PMID:12878853.

Kobayashi et al (2007) Rapamycin, a specific inhibitor of the mammalian target of rapamycin, suppresses lymphangiogenesis and lymphatic metastasis. Cancer Sci. 98 726. PMID: 17425689.

Fleming et al (2011) Chemical modulators of autophagy as biological probes and potential therapeutics. 7 9. PMID:21164513.

UK Price: 
340
Euro Price: 
240
CHF Price: 
305
SKK Price: 
2100
DKK Price: 
1800
NOK Price: 
1865

1391

NF 449

$199.00
Information
MW: 
1505.06
Solubility: 
Soluble to 50 mM in water
Activity: 

 

Potent purinergic receptor antagonist that displays high selectivity for P2X1 (IC50 values are 0.28, 0.69, 120, 1820, 47000 and > 300000 nM for rP2X1, rP2X1+5, rP2X2+3, rP2X3, rP2X2 and P2X4 receptors respectively). Provides antithrombotic protection in vivoAlso acts as a Gsα-selective antagonist.

Use & Storage
Storage: 
Store at RT
Literature
References: 

 

Hohenegger et al (1998) G-selective G protein antagonists. Proc.Natl.Acad.Sci.U.S.A. 95 346. PMID: 9419378.

Hechler et al (2005) Inhibition of platelet functions and thrombosis through selective or non-selective inhibition of the platelet P2 receptors with increasing doses of NF449 [4,4',4",4'"-(carbonylbis(imino-5,1,3-benzenetriylbis-(carbonylimino)))tetrakis-benzene-1,3-disulfonic acid octasodium salt]. J.Pharmacol.Exp.Ther. 314 232. PMID:15792995.

Rettinger et al (2005) Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist. Neuropharmacology. 48 461. PMID: 15721178.

Fleming et al (2011) Chemical modulators of autophagy as biological probes and potential therapeutics. Nat.Chem.Biol. 7 9. PMID: 21164513.

UK Price: 
125 485
Euro Price: 
190 755
CHF Price: 
220 940
SKK Price: 
1635 6650
DKK Price: 
1325 5550
NOK Price: 
1425 5705

1130

LY 294002 hydrochloride

$129.00
Information
MW: 
343.81
Purity: 
>99%
Activity: 

 

A highly selective inhibitor of phosphatidylinositol 3-kinase (IC50 values are 0.31, 0.73, 1.06 and 6.60μM for PI 3-Kβ, PI 3-Kα, PI 3-Kδ and PI 3-Kγ respectively). Inhibits proliferation and induces apoptosis in human colon cancer cells in vitro and in vivoInhibits autophagic sequestration in rat hepatocytes. Negative control LY 303511 (Cat. No. 2418) also available.

Use & Storage
Storage: 
Store at RT
Literature
References: 

 

Vlahos et al (1994) A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY 294002). J.Biol.Chem. 269 5241. PMID: 8106507.

Blommaart et al (1997) The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes. Eur.J.Biochem. 243 240. PMID: 9030745.

Chasserot-Golaz et al (1998) Possible involvement of phosphatidyl-3-kinase in regulated exocytosis: studies in chromaffin cells with inhibitor LY 294002. J.Neurochem. 70 2347. PMID: 9603199.

Ferrandi et al (2007) Phosphoinositide 3-kinase γ inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment. J.Pharmacol.Exp.Ther. 322 923. PMID: 17526805.

UK Price: 
85 309
Euro Price: 
130 470
CHF Price: 
150 585
SKK Price: 
1130 4125
DKK Price: 
925 3455
NOK Price: 
1005 3575

0741

GF 109203X

$185.00
Information
MW: 
412.49
Purity: 
>98%
Solubility: 
Soluble to 25 mM in DMSO
Activity: 

 

Very potent and selective inhibitor of protein kinase C, selective for the α and β1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC50 values are 0.6, 4.6, and 33 μM respectively). Potent antagonist at the 5-HT3receptor (Ki = 29.5 nM). Anti-inflammatory in vivoAlso available as part of the Mixed Kinase Inhibitor Tocriset™.

Use & Storage
Storage: 
Store at RT
Literature
References: 

 

Toullec et al (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J.Biol.Chem. 266 15771. PMID: 1874734.

Martiny-Baron et al (1993) Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976. J.Biol.Chem. 268 9194. PMID: 8486620.

Jacobson et al (1995) Anti-inflammatory properties of Go 6850: a selective inhibitor of protein kinase C. J.Pharmacol.Exp.Ther. 275 995. PMID: 7473193.

Coultrap et al (1999) Competitive antagonism of the mouse 5-hydroxytryptamine3 receptor by bisindolylmaleimide I, a "selective" protein kinase C inhibitor. J.Pharmacol.Exp.Ther. 290 76. PMID: 10381762.

Jiang et al (2011) Heat shock protein 90-mediated inactivation of nuclear factor-κB switches autophagy to apoptosis through becn1 transcriptional inhibition in selenite-indeced NB4 cells. Mol.Biol.Cell. 22 1167. PMID:21346199.

UK Price: 
340
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