AdipoGen eTOPIX: Small Molecules - Highlights - June 2016

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eTOPIX

Rapid Apoptosis Inducer, Anticancer Kinase Inhibitors, IDO1 Inhibitors & Acidic Organelle Dyes



 



HIGHLIGHT Rapid Apoptosis Inducer
 
Raptinal AG-CR1-2902


Rapid apoptosis inducer that initiates intrinsic pathway caspase-dependent apoptosis within minutes in multiple cell lines and in vivo systems. Exerts anticancer activity in vivo. Induces cell death in various cancer and non-cancerous cell lines with 24 hour IC50 values between 0.7-3.4μM.

LIT: R. Palchaudhuri, et al.; Cell Rep. 13, 2027 (2015)
 

Raptinal
 
 

HIGHLIGHT Dual Class I PI3K & mTOR Inhibitor
 
NVP-BEZ235 AG-CR1-3633


Potent dual ATP-competitive pan class I PI3K and mTOR inhibitor (p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4nM, 5nM, 7nM, 75nM and 6nM, respectively). Subsequently induces G1 phase arrest in biological cell growth and viability assays.

LIT: S.M. Maira, et al.; Mol. Cancer Ther. 7, 1851 (2008)

 

NVP-BEZ235
 
 

HIGHLIGHT Potent LIMK Inhibitor
 
BMS-3 AG-CR1-2901


Potent LIMK (Lim kinase) inhibitor with IC50 values of 5nM and 6nM for LIMK1 and LIMK2, respectively. LIMK inhibition with 1μM BMS-3 damages the microtubule-organizing center (MTOC) protein localisation to spindle poles, undermined the formation and positioning of functional MTOC and thus disrupted spindle formation and chromosome alignment.

LIT: P. Ross-Macdonald, et al.; Mol. Cancer Ther. 7, 3490 (2008)

BMS-3
 
 

HIGHLIGHT Selective IDO1 Inhibitors
 
Epacadostat AG-CR1-3634


Potent and selective competitive IDO1 (indoleamine 2,3-dioxygenase 1) inhibitor (in enzymatic (IC50=72nM) and in cellular tests (IC50=7.1nM)).

LIT: H.K. Koblish, et al.; Mol. Cancer Ther. 9, 489 (2010)




 

Epacadostat
  
NEW IDO1 Inhibitor: MMG-0358 AG-CR1-3630
 
 

HIGHLIGHT Selective Class IIb HDAC6 Inhibitor
 
ACY-775 AG-CR1-3903


Cell permeable, potent and selective class IIb HDAC6 inhibitor (IC50=7.5nM). Displays high selectivity over HDAC1-9 (IC50=1-10µM). Shows improved brain bioavailability compared to tubastatin A (Prod. No. AG-CR1-3900).

LIT: S. Mithraprabhu, et al.; Br. J. Haematol. 162, 559 (2013)

ACY-775
 
 

HIGHLIGHT Fluorescent Dye for Live Imaging
 
Ageladine A AG-CMA-1001


Cell/membrane permeable, non-toxic, pH-sensitive fluorescent dye (blue-green range) for live imaging of pH alteration in acidic organelles, such as lysosomes, autophagolysosomes or vesicles and even in small, transparent whole animals.

Wavelength Max: λex = 370 nm | λem = 415nm


LIT: U. Bickmeyer, et al.; BBRC 373, 419 (2008)
 

Ageladine A
 
Also available Dye: LysoGlow84™ AG-CMA-1005
 
 
Brochure "Small Molecules Highlights 2016"
 
Focus:

Synthetic Small Molecules
Unique Natural Products
Rare Antibiotics

Includes Products from:

AdipoGen Life Sciences
BioViotica
Chemodex
Innaxon

 

Download Product Brochure


Small Molecule Brochure 2016

 
Key Research Areas:
INFLAMMASOMES | INFLAMMATION
CANCER | OBESITY & DIABETES 
IMMUNITY | STEM CELL BIOLOGY
IMMUNO-ONCOLOGY
   Product Groups:
    ELISA KITS | ANTIBODIES
    PROTEINS | SMALL MOLECULES
    FLUORESCENT DYES & PROBES

 
 
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Products are for research use only. Not for diagnostic use.