Inhibitor

I-444

Apcin (Anaphase Promoting Complex Inhibitor) is a cell-permeable compound capable of slowing APC-dependent proteolysis.  Apcin functions by inhibiting substrate binding to Cdc20, the mitotic activator of the ubiquitin ligase activity of the anaphase-promoting complex/cyclosome (APC/C).  The mechanism of action is distinct from that of another APC/C inhibitor, proTAME (I-440), which binds

Apcin

$155.00
Information
Stock: 

Lyophilized powder

FW: 
438.65
Structure (deprecated): 

C13H14Cl3N7O4     

Purity: 
> 95% by LC/MS and NMR data
Solubility: 
Soluble in DMSO to ≥ 20 mM
Use & Storage
Use: 

Optimal dose for each cell line needs to be established empirically, however we do not recommend the use of apcin as a single agent in most experimental designs.  HeLa and hTERT-RPE1 cells are strongly arrested in mitosis when treated with a combination of proTAME (3-12 µM) and apcin (25-50 µM).

Storage: 

Store at -20°C.   Avoid multiple freeze/thaw cycles.

Purity: 
> 95% by LC/MS and NMR data
Literature
References: 

 

Sackton K.L., et al. (2014)  Nature  doi:10.1038/nature13660

Zeng X., et al.  (2010)  Cancer Cell  18: 382-395

Zeng X. and King R.W.  (2012) Nature Chemical Biology 8: 383-392

UK Price: 
120
Euro Price: 
185
CHF Price: 
200
SKK Price: 
1830
DKK Price: 
1377
NOK Price: 
1675
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1190

Biological Activity

Irreversible inhibitor of aspartic proteases. Inhibits lysosomal proteases and interferes with autolysosomal digestion when used in combination with E 64d (Cat. No. 4545).

Pepstatin A

$105.00
Information
MW: 
685.89
Solubility: 
Soluble to 1 mg/ml in ethanol with gentle warming
Use & Storage
Storage: 
Desiccate at -20°C
Literature
References: 

Merck Index 12 7290.

Marciniszyn et al (1976) Mode of inhibition of acid proteases by pepstatin. J.Biol.Chem. 251 7088. PMID: 993206.

Sato et al (2007) Autophagy is activated in colorectal cancer cells and contributes to the tolerance to nutrient deprivation. Cancer Res. 67 9677. PMID: 17942897.

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

1544

Chemical Name: 1,4-Dihydro-2,6-dimethyl-5-nitro-4-­[2-(trifluoromethyl)phenyl]-3-pyridinecarboxylic acid, methyl ester

(±)-Bay K 8644

$165.00
Information
MW: 
356.3
Purity: 
>99%
Solubility: 
Soluble to 100 mM in ethanol
Use & Storage
Storage: 
Store at +4°C
Literature
References: 

Greenberg et al (1984) Calcium channel 'agonist' BAY K 8644 inhibits calcium antagonist binding to brain and PC12 cell membranes. Brain Res. 305 365. PMID: 6204725.

Bourson et al (1989) Central and peripheral effects of the dihydropyridine calcium channel activator BAY K 8644 in the rat. Eur.J.Pharmacol. 160 339. PMID: 2469593.

Shi et al (2008) Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 3 568. PMID: 18983970.

Sarkar et al (2009) Rapamycin and mTOR-independent autophagy inducers ameliorate toxicity of polyglutamine-expanded huntingtin and related proteinopathies. Cell Death Differ. 16 46. PMID: 18636076.

 

UK Price: 
109 415
Euro Price: 
170 630
CHF Price: 
195 785
SKK Price: 
1480 5545
DKK Price: 
1200 4650
NOK Price: 
1275 4770

1334

Chemical Name: (3Z,5E,7R,8S,9S,11E,13E,15S,16R)-8-­Hydroxy-16-[(1S,2R,3S)-2-hydroxy-1-methyl-3-[(2R,4­R,5S,6R)-tetrahydro-2,4-dihydroxy-5-methyl-6-(1-me­thylethyl)-2H-pyran-2-yl]butyl]-3,15-dimethoxy-5,7­,9,11-tetramethyloxacyclohexadeca-3,5,11,13-tetrae­n-2-one

Bafilomycin A1

$129.00
Information
MW: 
622.84
Purity: 
>98%
Solubility: 
Soluble in DMSO
Use & Storage
Storage: 
Desiccate at -20°C
Literature
References: 

Yamamoto et al (1998) Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells. Cell Struct.Funct. 23 33. PMID: 9639028.

Gagliardi et al (1999) Chemistry and stucture activity relationships of bafilomycin A1, a potent and selective inhibitor of the vacuolar H+-ATPase. Curr.Med.Chem. 6 1197. PMID: 10519916.

Fass et al (2006) Microtubules support production of starvation-induced autophagosomes but not their targeting and fusion with lysosomes. J.Biol.Chem. 281 36303. PMID: 16963441.

UK Price: 
340
Euro Price: 
130
CHF Price: 
150
SKK Price: 
1130
DKK Price: 
925
NOK Price: 
1005

4247

Chemical Name: 1-[4-[4-(1-Oxopropyl)-1-piperazinyl­]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)-benz­o[h]-1,6-naphthyridin-2(1H)-one

Biological Activity

Potent and selective mTOR inhibitor (IC50 = 2 - 10 nM for mTORC1 and mTORC2). Displays 200-fold selectivity for mTOR over DNA-PK, ATM and hVps34. Induces autophagy in HeLa cells.

Torin 1

$245.00
Information
MW: 
607.62
Purity: 
>98%
Solubility: 
Soluble to 1 mM in DMSO
Use & Storage
Storage: 
Store at +4°C
Literature
References: 

Guertin and Sabatini (2009) The pharmacology of mTOR inhibition. Sci.Signal. 2 pe24. PMID: 19383975.

Thoreen et al (2009) An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J.Biol.Chem. 284 8023. PMID: 19150980.

Liu et al (2010) Discovery of 1-(4(-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J.Med.Chem. 53 7146. PMID: 20860370.

Peterson et al (2011) mTOR complex 1 regulates lipin 1 localization to control the SREBP pathway. Cell. 146 408. PMID: 21816276.

UK Price: 
149 605
Euro Price: 
230 925
CHF Price: 
295 1185
SKK Price: 
2015 8215
DKK Price: 
1725 6890
NOK Price: 
1790 7015

2706

Alternative Names: NSC 362856, CCRG 81045

Chemical Name: 3,4-Dihydro-3-methyl-4-oxoimidazo[5­,1-d]-1,2,3,5-tetrazine-8-carboxamide

Biological Activity

DNA methylating, chemotherapeutic agent. Displays antitumor activity against a board spectrum of tumors, including leukemias, lymphomas and solid tumors (IC50 = 5.0 μM for cytotoxicity against mouse TLX5 lymphoma cells). Induces autophagy in malignant glioma cells.

Temozolomide

$89.00
Information
MW: 
194.15
Purity: 
>99%
Solubility: 
Soluble to 50 mM in DMSO
Use & Storage
Storage: 
Store at RT
Literature
References: 

Plowman et al (1994) Preclinical antitumor activity of temozolomide in mice: efficacy against human brain tumor xenografts and synergism with 1,3-bis(2-chloroethyl)-1-nitrosourea. Cancer Res. 54 3793. PMID: 8033099.

Clark et al (1995) Antitumor imidazotetraazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide. J.Med.Chem. 38 1493. PMID: 7739008.

Bodell et al (2003) Formation of DNA adducts and induction of lacI mutations in big blue rat-2 cells treated with temozolomide: implications for the treatment of low-grade adult and pediatric tumors. Cancer Epidemiol.Biomarkers Prevent. 12 545.

Kanzawa et al (2004) Role of autophagy in temozolomide-induced cytotoxicity for malignant glioma cells. Cell Death Differ. 11 448. PMID: 14713959.

UK Price: 
65 225
Euro Price: 
105 345
CHF Price: 
115 435
SKK Price: 
905 3060
DKK Price: 
735 2590
NOK Price: 
805 2670
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