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Items 14 of 14
ALX-340-042
Revised 07-Jan-06
Arvanil
SYNONYMS
N-[(4-Hydroxy-3-methoxyphenyl)methyl]-5
Z
,8
Z
,11
Z
,14
Z
-eicosatetraenamide
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
Cannabinoid Receptor Agonists & Antagonists / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-340-042-M005
5 mg
25.00 USD
Product Specification
FORMULA:
C
28
H
41
NO
3
MW:
439.6
CAS NUMBER:
128007-31-8
PURITY:
≥98%
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Keep cool and dry.
Product Description
"Hybrid" activator of CB
1
receptor (CB
1
: K
i
=0.5µM; CB
2
: K
i
=>15µM) and TRPV1 (K
i
=0.3µM). Also inhibits anandamide uptake (IC
50
=3.6µM) and fatty acid amide hydrolase (FAAH) (IC
50
=3µM). Analgesic, vasodilatory and anti-inflammatory
in vivo
. Apoptosis inducer.
Product Specific Literature References
Unsaturated long-chain N-acyl-vanillyl-amides (N-AVAMs): vanilloid receptor ligands that inhibit anandamide-facilitated transport and bind to CB1 cannabinoid receptors:
D. Melck, et al.; BBRC
262
, 275 (1999)
Abstract
Neurobehavioral activity in mice of N-vanillyl-arachidonyl-amide
:
V. Di Marzo, et al.; Eur. J. Pharmacol.
406
, 363 (2000)
Abstract
A structure/activity relationship study on arvanil, an endocannabinoid and vanilloid hybrid
:
V. Di Marzo, et al.; J. Pharmacol. Exp. Ther.
300
, 984 (2002)
Abstract
The CB1/VR1 agonist arvanil induces apoptosis through an FADD/caspase-8-dependent pathway
:
R. Sancho, et al.; Br. J. Pharmacol.
140
, 1035 (2003)
Abstract
Evidence against the presence of an anandamide transporter
:
S.T. Glaser, et al.; PNAS
100
, 4269 (2003)
Abstract
Arvanil, a hybrid endocannabinoid and vanilloid compound, behaves as an antihyperkinetic agent in a rat model of Huntington's disease:
E. de Lago, et al.; Brain Res.
1050
, 210 (2005)
Abstract
Arvanil inhibits T lymphocyte activation and ameliorates autoimmune encephalomyelitis:
A.M. Malfitano, et al.; J. Neuroimmunol.
171
, 110 (2006)
Abstract
Further Categories Containing This Product:
Anandamide Uptake Inhibitors
•
Apoptosis Inducers & Inhibitors Other Products
•
TRPV1 Agonists and Antagonists / Related Products
•
Analgesic / Anti-nociceptive Agents / Related Products
•
Anti-inflammatory Agents Other Products
•
Fatty Acid Amide Hydrolase [FAAH] / Related Products
ALX-270-443
Revised 05-May-08
AS601245
SYNONYMS
1,3-Benzothiazol-2-yl-(2-{[2-(3-pyridinyl)ethyl]amino}-4-pyrimidinyl) acetonitrile
JNK Inhibitor V
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
JNK [SAPK1] / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-443-M001
1 mg
50.00 USD
ALX-270-443-M005
5 mg
150.00 USD
ALX-270-443-M025
25 mg
520.00 USD
Product Specification
FORMULA:
C
20
H
16
N
6
S
MW:
372.5
CAS NUMBER:
345987-15-7
PURITY:
≥95% (HPLC)
APPEARANCE:
White to yellow solid.
PURITY DETAIL:
Sum of two isomers.
SOLUBILITY:
Soluble in DMSO (10mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:
Hygroscopic. Packaged under inert gas. Protect from light.
HAZARD:
HARMFUL.
IDENTITY:
Identity determined by
1
H-NMR.
Product Description
Potent and cell permeable ATP competitive JNK inhibitor (hJNK1: IC
50
=150nM, hJNK2: IC
50
=220nM and hJNK3: IC
50
=70 nM). Displays anti-inflammatory properties and has been shown to reduce TNF-α plasma levels induced by LPS in mice.
Product Specific Literature References
AS601245 (1,3-benzothiazol-2-yl (2-[[2-(3-pyridinyl) ethyl] amino]-4 pyrimidinyl) acetonitrile): a c-Jun NH2-terminal protein kinase inhibitor with neuroprotective properties:
S. Carboni, et al.; J. Pharmacol. Exp. Ther.
310
, 25 (2004)
Abstract
;
Full Text
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase:
P. Gaillard, et al.; J. Med. Chem.
48
, 4596 (2005)
Abstract
Further Categories Containing This Product:
TNF-alpha & TNF Receptors Other Products
•
Anti-inflammatory Agents Other Products
ALX-430-064
Revised 15-Sep-08
Auranofin
PRODUCT LINE
Inflammation
PRODUCT CATEGORY
Lipoxygenases / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-430-064-M025
25 mg
35.00 USD
ALX-430-064-M100
100 mg
68.00 USD
Product Specification
FORMULA:
C
20
H
34
AuO
9
PS
MW:
678.5
CAS NUMBER:
34031-32-8
MERCK INDEX:
14:
878
PURITY:
≥98%
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in DMSO (5mg/ml) or 100% ethanol (4mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+20°C
USE/STABILITY:
Solutions are stable for up to 3 months when stored at -20 °C.
HAZARD:
TOXIC.
Product Description
Gold derivative in clinical use as an anti-arthritic. Acts as an inhibitor of several leukocyte activation pathways. Inhibits release of inflammatory mediators from human macrophages, pulmonary mast cell and basophils. Also inhibits human neutrophil 5-lipoxygenase. Efficient inducer of mitochondrial membrane permeability transition pore in the presence of calcium ions, potentially referable to its inhibition of mitochondrial thioredoxin reductase.
Product Specific Literature References
Antiarthritic gold compounds effectively quench electronically excited singlet oxygen:
E.J. Corey, et al.; Science
236
, 68 (1987)
Abstract
Modulation of mediator release from human basophils and pulmonary mast cells and macrophages by auranofin:
M. Columbo, et al.; Biochem. Pharmacol.
39
, 285 (1990)
Abstract
Auranofin stimulates LTA hydrolase and inhibits 5-lipoxygenase/LTA synthase activity of isolated human neutrophils
:
W.H. Betts, et al.; Biochem. Pharmacol.
39
, 1233 (1990)
Abstract
Auranofin inhibits the activation pathways of polymorphonuclear leukocytes at multiple sites:
R. Rudkowski, et al.; Biochem. Pharmacol.
41
, 1921 (1991)
Abstract
Induction of mitochondrial permeability transition by auranofin, a Gold(I)-phosphine derivative
:
M.P. Rigobello, et al.; Br. J. Pharmacol.
136
, 1162 (2002)
Abstract
General Literature References
Auranofin
:
W.F. Kean, et al.; Br. J. Theumatol.
36
, 560 (1997), (Review)
Abstract
;
Full Text
Further Categories Containing This Product:
MPTP [Mitochondrial Transition Pore] / Related Products
•
TLRs Other Products
•
Anti-inflammatory Agents Other Products
ALX-270-219
Revised 15-May-07
BAY 11-7082
SYNONYMS
(E)-3-(4-Methylphenylsulfonyl)-2-propenenenitrile
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
NF-kB Pathway Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
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ALX-270-219-M010
10 mg
45.00 USD
ALX-270-219-M050
50 mg
190.00 USD
Product Specification
FORMULA:
C
10
H
9
NO
2
S
MW:
207.3
CAS NUMBER:
195462-67-7
PURITY:
≥99%
SOLUBILITY:
Soluble in DMSO, 100% ethanol, methanol or methylene dichloride; insoluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Keep under inert gas.
Product Description
Inhibitor of cytokine induced IκBα phosphorylation resulting thereby in a decreased expression of NF-κB and adhesion molecules. Potential anti-inflammatory agent.
Product Specific Literature References
Novel inhibitor of cytokine-induced IkBa phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo:
J.W. Pierce, et al.; J. Biol. Chem.
272
, 21096 (1997)
Abstract
;
Full Text
Inhibition of NF-kappaB induces apoptosis of KSHV-infected primary effusion lymphoma cells:
S.A. Keller, et al.; Blood
96
, 2537 (2000)
Abstract
Insulin-like growth factor-I protects colon cancer cells from death factor-induced apoptosis by potentiating tumor necrosis factor alpha- induced mitogen-activated protein kinase and nuclear factor kappaB signaling pathways:
M.M. Remacle-Bonnet, et al.; Cancer Res.
60
, 2007 (2000)
Abstract
Up-regulation of multidrug resistance P-glycoprotein via nuclear factor- kappaB activation protects kidney proximal tubule cells from cadmium- and reactive oxygen species-induced apoptosis:
F. Thevenod, et al.; J. Biol. Chem.
275
, 1887 (2000)
Abstract
;
Full Text
Neuronal injury-induced expression and release of apolipoprotein E in mixed neuron/glia co-cultures: nuclear factor kappaB inhibitors reduce basal and lesion-induced secretion of apolipoprotein E:
V. Petegnief, et al.; Neuroscience
104
, 223 (2001)
Abstract
Poly(ADP-ribose) polymerase-1 promotes microglial activation, proliferation, and matrix metalloproteinase-9-mediated neuron death:
T.M. Kauppinen & R.A. Swanson; J. Immunol.
174
, 2288 (2005)
Abstract
;
Full Text
Further Categories Containing This Product:
Anti-inflammatory Agents Other Products
ALX-270-220
Revised 04-Nov-05
BAY 11-7085
SYNONYMS
(E)-3-(
t
-Butylphenylsulfonyl)-2-propenenitrile
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
NF-kB Pathway Inhibitors
Ordering Information
Product Numbers:
Format:
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ALX-270-220-M010
10 mg
60.00 USD
Product Specification
FORMULA:
C
13
H
15
NO
2
S
MW:
249.3
CAS NUMBER:
196309-76-9
PURITY:
≥98%
APPEARANCE:
White to off-white crystalline powder.
SOLUBILITY:
Soluble in DMSO or ethanol; insoluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Keep under inert gas.
Product Description
Has biological properties very similar to those of BAY 11-7082 (Prod. No.
ALX-270-219
). In addition, the product exhibits potent anti-inflammatory properties
in vivo
.
Product Specific Literature References
Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo
:
J.W. Pierce, et al.; J. Biol. Chem.
272
, 21096 (1997)
Abstract
;
Full Text
Pharmacologic interference with NF-kappaB activation attenuates central nervous system complications in experimental Pneumococcal meningitis:
U. Koedel, et al.; J. Infect Dis.
182
, 1437 (2000)
Abstract
Neuronal injury-induced expression and release of apolipoprotein E in mixed neuron/glia co-cultures: nuclear factor kappaB inhibitors reduce basal and lesion-induced secretion of apolipoprotein E:
V. Petegnief, et al.; Neuroscience
104
, 223 (2001)
Abstract
Further Categories Containing This Product:
Anti-inflammatory Agents Other Products
ALX-270-097
Revised 07-Sep-06
Ebselen
SYNONYMS
2-Phenyl-1,2-benzisoselenazol-3-(2
H
)-one
PRODUCT LINE
Oxidative Stress
PRODUCT CATEGORY
Peroxynitrite / Scavengers / Detection
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-097-M001
1 mg
12.00 USD
ALX-270-097-M005
5 mg
20.00 USD
ALX-270-097-M025
25 mg
60.00 USD
Product Specification
FORMULA:
C
13
H
9
NOSe
MW:
274.2
CAS NUMBER:
60940-34-3
PURITY:
≥98% (NMR)
APPEARANCE:
White to off-white crystalline solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Description
Selenium-based inhibitor of protein kinase C, NADPH, 5-lipoxygenase, cyclooxygenase (COX) and NADPH oxidase. Anti-inflammatory antioxidant. Mimics glutathione peroxidase. Inhibits oxidative modifications of low density lipoproteins (LDL).
Product Specific Literature References
A novel biologically active seleno-organic compound--III. Effects of PZ 51 (Ebselen) on glutathione peroxidase and secretory activities of mouse macrophages
:
M.J. Parnham & S. Kindt; Biochem. Pharmacol.
33
, 3247 (1984)
Abstract
Seleno-organic compounds and the therapy of hydroperoxide-linked pathological conditions
:
M.J. Parnham & E. Graf; Biochem. Pharmacol.
36
, 3095 (1987)
Abstract
Kinetic mechanism and substrate specificity of glutathione peroxidase activity of ebselen (PZ51)
:
M. Maiorino, et al.; Biochem. Pharmacol.
37
, 2267 (1988)
Abstract
Studies on the anti-inflammatory activity of ebselen. Ebselen interferes with granulocyte oxidative burst by dual inhibition of NADPH oxidase and protein kinase C?:
I.A. Cotgreave, et al.; Biochem. Pharmacol.
38
, 649 (1989)
Abstract
T. Nikawa, et al.; Biochem. Pharmacol.
47
, 1007 (1994)
Abstract
Effects of ebselen and probucol on oxidative modifications of lipid and protein of low density lipoprotein induced by free radicals:
N. Noguchi, et al.; Biochim. Biophys. Acta
1213
, 176 (1994)
Abstract
Strong inhibition of mammalian lipoxygenases by the antiinflammatory seleno-organic compound ebselen in the absence of glutathione:
C. Schewe, et al.; Biochem. Pharmacol.
48
, 65 (1994)
Abstract
Ebselen: a glutathione peroxidase mimic
:
H. Sies; Meth. Enzymol.
234
, 476 (1994)
Abstract
Molecular actions of ebselen-an antiinflammatory antioxidant
:
T. Schewe; Gen. Pharmacol.
26
, 1153 (1995)
Abstract
Ebselen
:
H. Sies; Meth. Enzymol.
252
, 341 (1995)
Abstract
Ebselen as a glutathione peroxidase mimic and as a scavenger of peroxynitrite
:
H. Sies & H. Masumoto; Adv. Pharmacol.
38
, 229 (1997)
Abstract
Free radical generation by selenium compounds and their prooxidant toxicity
:
J.E. Spallholz; Biomed. Environ. Sci.
10
, 260 (1997)
Abstract
Protection against peroxynitrite by selenoproteins
:
H. Sies, et al.; Z. Naturforsch. [C]
53
, 228 (1998)
Abstract
Ebselen protects mice against T cell-dependent, TNF-mediated apoptotic liver injury
:
G. Tiegs, et al.; J. Pharmacol. Exp. Ther.
287
, 1098 (1998)
Abstract
;
Full Text
Further Categories Containing This Product:
Antioxidants, Flavonoids & Free Radical Scavengers Other Products
•
PKC Inhibitors
•
Malaria / Related Products
•
Lipoxygenases / Related Products
•
Anti-inflammatory Agents Other Products
•
COX Inhibitors
ALX-350-254
Revised 10-Mar-08
Epoxomicin
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antibiotics - Proteasome / Ubiquitin Modulators
Ordering Information
Product Numbers:
Format:
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Unit Price:
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ALX-350-254-C050
50 µg
132.00 USD
Product Specification
FORMULA:
C
28
H
50
N
4
O
7
MW:
554.7
CAS NUMBER:
134381-21-8
MERCK INDEX:
14:
3630
SOURCE/HOST:
Synthetic.
PURITY:
≥95% (HPLC)
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO (15mg/ml); insoluble in water.
ACTIVITY:
k
obs
/[I] = 25’000M
-1
s
-1
versus 20S proteasome.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Avoid freeze/thaw cycles. Protect from light.
IDENTITY:
Identity determined by
1
H-NMR.
Product Description
Cell permeable, potent and selective proteasome inhibitor originally isolated from
Actinomycetes
strain based on its potent
in vivo
antitumor activity. More potent inhibitor of the chymotrypsin-like activity of the proteasome than lactacystin. Effectively inhibits NF-κB activation
in vitro
and potently blocks inflammation
in vivo
in the mouse ear edema assay.
Product Specific Literature References
Epoxomicin, a new antitumor agent of microbial origin:
M. Hanada, et al.; J. Antibiot. (Tokyo)
45
, 1746 (1992)
Abstract
Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency:
K.B. Kim, et al.; Bioorg. Med. Chem. Lett.
9
, 3335 (1999)
Abstract
Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity:
L. Meng, et al.; PNAS
96
, 10403 (1999)
Abstract
Total synthesis of the potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology:
N. Sin, et al.; Bioorg. Med. Chem. Lett.
9
, 2283 (1999)
Abstract
The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses:
K. Schwarz, et al.; J. Immunol.
164
, 6147 (2000)
Abstract
Establishment and some characteristics of epoxomicin (a proteasome inhibitor) resistant variants of the human squamous cell carcinoma cell line, A431:
K. Ohkawa, et al.; Int. J. Oncol.
24
, 425 (2004)
Abstract
Further Categories Containing This Product:
Proteasome / Related Products
•
Anti-inflammatory Agents Other Products
•
Antibiotics for Inflammation Research
•
NF-kB Pathway Inhibitors
•
Antibiotics - NF-kB Inhibitors
•
Antitumor Antibiotics
•
Antitumor Agents (Enzyme Inhibitors)
ALX-380-274
Revised 21-May-08
Erythromycin
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antibiotics for Inflammation Research
Ordering Information
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ALX-380-274-G005
5 g
40.00 USD
Product Specification
FORMULA:
C
37
H
67
NO
13
MW:
733.9
CAS NUMBER:
114-07-8
MERCK INDEX:
14:
3681
RTECS:
KF4375000
SOURCE/HOST:
Isolated from
Streptomyces erythreus
.
PURITY:
≥85% (Assay on dry basis)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water (50mg/ml), 100% ethanol or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HAZARD:
HARMFUL.
Product Description
Macrolide antibiotic. Inhibits protein synthesis (elongation) at the transpeptidation step. Binds to the 23S RNA of the 50S ribosomal subunit. Effective against Gram-negative and Gram-positive bacteria.
Product Specific Literature References
Inducible erythromycin resistance in bacteria:
B. Weisblum; Br. Med. Bull.
40
, 47 (1984)
Abstract
Erythromycin inhibits transcriptional activation of NF-kappaB, but not NFAT, through calcineurin-independent signaling in T cells:
Y. Aoki & P.N. Kao; Antimicrob. Agents Chemother.
43
, 2678 (1999)
Abstract
;
Full Text
Assessment of the potential pharmacokinetic and pharmacodynamic interactions between erythromycin and argatroban:
J.Q. Tran, et al.; J. Clin. Pharmacol.
39
, 513 (1999)
Abstract
Inhibition of the metabolism of brotizolam by erythromycin in humans: in vivo evidence for the involvement of CYP3A4 in brotizolam metabolism:
T. Tokairin, et al.; Br. J. Clin. Pharmacol.
60
, 172 (2005)
Abstract
;
Full Text
Related Products
ALX-380-264
EM574
Further Categories Containing This Product:
NF-kB Pathway Inhibitors
•
Anti-inflammatory Agents Other Products
•
Translation Inhibitors
ALX-270-361
Revised 28-Sep-07
Indirubin
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-361-M001
1 mg
50.00 USD
ALX-270-361-M005
5 mg
200.00 USD
Product Specification
FORMULA:
C
16
H
10
N
2
O
2
MW:
262.3
CAS NUMBER:
479-41-4
SOURCE/HOST:
Synthetic.
PURITY:
≥98% (
1
H-NMR, HPLC)
APPEARANCE:
Purple powder.
SOLUBILITY:
Soluble in DMSO (10mg/ml) or methanol (0.3mg/ml). Sparingly soluble in aqueous buffers (12.5µg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
USE/STAB