BIOMOL Online January 2008

In this issue			January 2008
:: Ion channel modulators :: Geldanamycin-FITC :: BML-267, PTP1B inhibitor			:: Clioquinol, neuroprotective agent :: Protease reagents

FEATURED PRODUCTS

Ion Channel Modulators

21 New Ion Channel Modulators

Calcium channel modulators Calciseptine (Cat. # CA-502 ) – L-type Ca²⁺ channel blocker Cilnidipine (Cat. # CA-237 ) – Dual L- / N-type calcium channel blocker Felodipine (Cat. # CA-236 ) – L-type Ca²⁺ channel blocker SNX-482 (Cat. # CA-501 ) – Cav2.3 (alpha1E, R-type) channel blocker Kurtoxin (Cat. # CA-500 ) – T-type Ca²⁺ channel blocker	Cilnidipine (CA-237)
Potassium channel modulators Charybdotoxin (Cat. # KC-168 ) – Ca²⁺ activated K⁺ channel blocker α-Dendrotoxin (Cat. # KC-167 ) – Kv1.1 and Kv1.2 channel blocker Dendrotoxin-I (Cat. # KC-163 ) – Kv1.1 and Kv1.2 channel blocker Dendrotoxin-K (Cat. # KC-164 ) – Kv1.1 and Kv1.2 channel blocker Iberiotoxin (Cat. # KC-162 ) – Ca²⁺-activated K⁺ channel blocker Margatoxin (Cat. # KC-166 ) – Kv1.3 channel blocker Nicorandil (Cat. # KC-152 ) – ATP-sensitive K⁺ channel activator Stromatoxin-1 (Cat. # KC-165 ) – Kv2 blocker TRAM-34 (Cat. # KC-161 ) – Ca²⁺ activated K⁺ channel blocker	Nicorandil (KC-152)
Sodium channel modulators ATX II (Cat. # NA-106 ) – TTX-sens. and insens. Na⁺ channel activator Batrachotoxin (Cat. # NA-141 ) – Na⁺ channel activator Bupivacaine (Cat. # NA-139 ) – Na⁺ channel blocker Lamotrigine (Cat. # NA-137 ) – Voltage-gated Na⁺ channel blocker PD-85639 (Cat. # NA-140) – Na⁺ channel blocker Riluzole (Cat. # NA-138 ) – Voltage-dependent Na⁺ channel blocker	Batrachotoxin (NA-141)
TRP channel modulators 2-APB (Cat. # CA-238 ) – Activates TRPVs 1-3. Inhibits TRPC 5 & 6 and TRPMs 3 & 8	2-APB (CA-238)
related ion channel modulators ion channels \| calcium channels \| chloride channels \| potassium channels \| sodium channels \| TRP channels

Visit
www.biomol.com/ionchannels
for a complete listing of ion channel antibodies

2-Pore domain potassium channels	NMDA receptors
GABA receptors	Sodium/calcium exchangers
Glycine receptors	TRP channels
HCN channels	Voltage-gated potassium channels

NEW PRODUCTS

Geldanamycin Derivative

Geldanamycin-FITC (Cat. # EI-361)
A novel geldanamycin fluorescent probe that may be used in a fluorescence polarization assay for Hsp90 inhibitors. May also be used for detection of cell surface Hsp90.

related products
geldanamycin | 17-AAG | 17-DMAG | geldanamycin-biotin | 17-GMB-APA-GA

PTP1B Inhibitor
BML-267 (Cat. # PR-121) Potent and selective protein tyrosine phosphatase 1B (PTP1B) inhibitor (IC₅₀=11 microM)

related products
PTP1B assay | PTP1B enzyme | PTP1B substrate | PTP1B inhibitors

PTP1B Drug Discovery Kit (Cat. # AK-822)

A colorimetric, non-radioactive assay designed to measure the phosphatase activity of purified PTP1B. The kit includes human, recombinant PTP1B (residues 1-322), expressed in E. coli. The detection of free-phosphate released is based on the classic Malachite green assay.

The components and assay protocol for the PTP1B Drug Discovery Kit have recently been completely reworked to improve enzyme stability and to permit more effective inhibitor and modulator screening conditions.

Neuroprotective Agent
Clioquinol (Cat. # N-158) A metal chelating ligand which displays protective effects in various neurodegenerative states. It modulates amyloid beta-peptide accumulation via upregulation of metalloprotease activity. When co-administered with vitamin B12 it totally rescues lead-induced impairments of synaptic plasticity in an animal model.
related products neurotrophic agents \| markers of neurological disease \| neuroscience
Protease Reagents
ACE2 (human, recombinant) (Cat. # SE-520) ACE2 extracellular domain (residues 1-740), expressed in mammalian cells. ACE2 is a cell membrane-inserted zinc carboxypeptidase involved in processing of neuropeptides.
Aminopeptidase N (rat kidney) (Cat. # SE-513) Isolated from rat kidney. A zinc-dependent membrane aminopeptidase whose targets include bradykinin and enkephalin.
BACE-1 (human, recombinant) (Cat. # SE-531) Active soluble BACE-1 expressed in E. coli. BACE-1 is an aspartic protease involved in Alzheimer’s disease and cancer.
Cathepsin K Proenzyme (human, recombinant) (Cat. # SE-367) Purified as full-length proenzyme. Unlike mature cathepsin K, procathepsin K is stable, and can be activated in one step.
FAP (human, recombinant) (Cat. # SE-409) Active recombinant human FAP, residues Ser29-Asp760, representing a naturally-occurring cleaved (soluble) form. FAP is a homodimeric serine prolyl peptidase that digests gelatin, collagen, and α2-antiplasmin.
Furin (human, recombinant) (Cat. # SE-536) Active soluble (truncated at amino acid 595) furin. Furin is a proprotein convertase with many targets, such as insulin proreceptor and other pro-hormones and growth factors, proMMPs, plasma pro-factors, and viral and bacterial proteins.
Proteinase 3 (human neutrophil) (Cat. # SE-498) Derived from human sputum neutrophils. Proteinase 3 is a neutral serine protease located in neutrophil azurophil granules.
TIMP-1 (human, purified) (Cat. # SE-530) Purified from human neutrophils. TIMP-1 inhibits most MMPs and ADAMs, displaying K_i’s in the low nanomolar range.
TIMP-2 (human, purified) (Cat. # SE-469) Purified from human fibroblasts. TIMP-2 inhibits most MMPs, particularly MMP-2. It can also inhibit ADAMs such as ADAMTS. TIMP-2 is also required for activation of pro-MMP-2 by MT1-MMP and MT2-MMP.
Apstatin (Cat. # PI-145) Apstatin is a potent and selective inhibitor of aminopeptidase P (APP), K_i=2.6 microM.

Protease Inhibitor Library (Cat. # 2832)

The Screen-Well Protease Inhibitor Library includes 53 known protease inhibitors on a single 96-well plate. Inhibitors are supplied dissolved in DMSO at 10 mM and aliquoted into deep-well plates at either 100 or 500 microliters per well. The library is a convenient and cost-effective way to purchase a panel of protease inhibitors for chemical genomics, assay development, and other applications. Inquire for a list of compounds and pricing.

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