Inhibitor

3993

EB 1089

$179.00
Information
MW: 
454.68
Purity: 
>98%
Solubility: 
Soluble in DMSO and in ethanol
Activity: 

 

Vitamin D receptor (VDR) agonist; analog of calcitriol (Cat. No. 2551). Exhibits anti-tumor and anti-proliferative activity with reduced hypercalcemic effects. 60 times more potent in inhibiting MCF-7 cell growth in vitroalso shown to induce autophagy in MCF-7 cells. Reverses the effects of parathyroid hormone-related protein (PTHrP).

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

 

 

Abdaimi et al (1999) Reversal of hypercalcaemia with the vitamin D analogue EB1089 in a human model of squamous cancer. Cancer Res, 59 3325.

Hoyer-Hansen et al (2005) Vitamin D analog EB1089 triggers dramatic lysosomal changes and Beclin 1-mediated autophagic cell death. Cell Death Differ. 12 1297. PMID: 15905882.

Lu et al (2008) Vitamin D3 analogue EB1089 inhibits the proliferation of human laryngeal squamous carcinoma cells via p57. Mol.Cancer Ther. 7 1268. PMID: 18483314.

Ormerod et al (2008) The calcitriol analogue EB1089 impairs alveolarization and induces localized regions of increased fibroblast density in neonatal rat lung. Exp.Lung.Rs. 34 155.

Bhatia et al (2009) EB1089 inhibits the parathyroid hormone-related protein-enhanced bone metastasis and xenograft growth of human prostate cancer cells. Mol.Cancer Ther. 8 1787. PMID: 19584236.

 

UK Price: 
340
Euro Price: 
170
CHF Price: 
210
SKK Price: 
1490
DKK Price: 
1275
NOK Price: 
1350

3093

Dorsomorphin dihydrochloride

$185.00
Information
MW: 
472.41
Purity: 
>98%
Solubility: 
Soluble to 100 mM in water and to 10 mM in DMSO
Activity: 

 

Potent and selective inhibitor of AMP-activated protein kinase (AMPK) (Ki = 109 nM). Displays no significant activity on several structurally related kinases including ZAPK, SYK, PKCθ, PKA and JAK3. Inhibits AMPK activation induced by AICAR (Cat. No. 2840) and metformin (Cat. No. 2864). Also inhibits bone morphogenetic protein (BMP) type I receptors (ALK2, ALK3 and ALK6). Promotes cardiomyogenesis in mouse embryonic stem cells (ESCs) in vitroShown to induce autophagy in cancer cell lines via a mechanism independent of AMPK inhibition.

Use & Storage
Storage: 
Desiccate at RT
Literature
References: 

 

Zhou et al (2001) Role of AMP-activated protein kinase in mechanism of metformin action. J.Clin.Invest. 108 1167. PMID: 11602624.

Hao et al (2008) Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells. PLoS ONE 3 2904. PMID: 18682835.

Yu et al (2008) Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat.Chem.Biol.4 33. PMID: 18026094.

Vucicevic et al (2011) Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway. Autophagy 7 40. PMID: 20980833.

UK Price: 
115 455
Euro Price: 
175 695
CHF Price: 
220 870
SKK Price: 
1550 6155
DKK Price: 
1300 5140
NOK Price: 
1395 5285

The CCAAT box-binding transcription factor NF-Y regulates basal expression of human proteasome genes.

Xu, H. et al. (2012) "The CCAAT box-binding transcription factor NF-Y regulates basal expression of human proteasome genes." Biochim. Biophys. Acta 1823(4): 818–825.

PubMed ID: 
22285817
Product(s) Referenced: 
MG132, Suc-Leu-Leu-Val-Tyr-AMC pep- tide substrate

Structural and molecular characterization of iron-sensing hemerythrin-like domain within F-box and leucine-rich repeat protein 5 (FBXL5).

Thompson, J.W. et al. (2012) "Structural and molecular characterization of iron-sensing hemerythrin-like domain within F-box and leucine-rich repeat protein 5 (FBXL5)." J. Biol. Chem. 287(10): 7357–7365.

PubMed ID: 
22253436
Product(s) Referenced: 
MG132

The ubiquitin-activating enzyme (E1) of the early-branching eukaryote Giardia intestinalis shows unusual proteolytic modifications and play important roles during encystation.

Niño, C.A. et al. (2012) "The ubiquitin-activating enzyme (E1) of the early-branching eukaryote Giardia intestinalis shows unusual proteolytic modifications and play important roles during encystation." Acta tropica. 2012 Apr 4.

PubMed ID: 
22498829
Product(s) Referenced: 
ubiquitin-aldehyde

Inhibitor Mediated Protein Degradation.

Long, M.J.C. et al. (2012) "Inhibitor Mediated Protein Degradation." Chemistry & Biology 19(5): 629–637.

PubMed ID: 
22633414
Product(s) Referenced: 
immunoproteasome from mouse spleen, Purified 20S proteasome from HeLa, IU1

Chalcone-based small-molecule inhibitors attenuate malignant phenotype via targeting deubiquitinating enzymes.

Issaenko, O.A. and Amerik, A.Y. (2012) "Chalcone-based small-molecule inhibitors attenuate malignant phenotype via targeting deubiquitinating enzymes." Cell cycle (Georgetown, Tex.) 11(9).

PubMed ID: 
22510564
Product(s) Referenced: 
Ubiquitin aldehyde (Ubal), 20S Human proteasome

Ubiquitination of BST-2 Protein by HIV-1 Vpu Protein Does Not Require Lysine, Serine, or Threonine Residues within the BST-2 Cytoplasmic Domain.

Gustin, J.K. et al. (2012) "Ubiquitination of BST-2 Protein by HIV-1 Vpu Protein Does Not Require Lysine, Serine, or Threonine Residues within the BST-2 Cytoplasmic Domain." J. Biol. Chem. 287(18): 14837–14850.

PubMed ID: 
22383521
Product(s) Referenced: 
MG132

Herpes virus deneddylases interrupt the cullin-RING ligase neddylation cycle by inhibiting the binding of CAND1.

Gastaldello, S. et al. (2012) "Herpes virus deneddylases interrupt the cullin-RING ligase neddylation cycle by inhibiting the binding of CAND1." Journal of molecular cell biology. 2012 Apr 3;

PubMed ID: 
22474075
Product(s) Referenced: 
Ub-VS

The ubiquitin-activating enzyme (E1) of the early-branching eukaryote Giardia intestinalis shows unusual proteolytic modifications and play important roles during encystation.

Niño, C.A. et al. (2012) "The ubiquitin-activating enzyme (E1) of the early-branching eukaryote Giardia intestinalis shows unusual proteolytic modifications and play important roles during encystation." Acta tropica. 2012 Apr 4.

PubMed ID: 
22498829
Product(s) Referenced: 
MG132
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