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ALX-260-092
Revised 05-Jun-08
MG-132
SYNONYMS
Z-LLL-CHO
Z-Leu-Leu-Leu-CHO
PRODUCT LINE
Ubiquitin & Proteasome
PRODUCT CATEGORY
Proteasome / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-260-092-M001
1 mg
25.00 USD
ALX-260-092-M005
5 mg
60.00 USD
Product Specification
SEQUENCE:
Z-Leu-Leu-Leu-CHO
FORMULA:
C
26
H
41
N
3
O
5
MW:
475.6
CAS NUMBER:
133407-82-6
PURITY:
≥95% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
IDENTITY:
Identity determined by MS.
Product Description
Potent, reversible and cell permeable proteasome inhibitor. Inhibits NF-κB activation.
Product Specific Literature References
Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules:
K.L. Rock, et al.; Cell
78
, 761 (1994)
Abstract
Multiple proteolytic systems, including the proteasome, contribute to CFTR processing:
T.J. Jensen, et al.; Cell
83
, 129 (1995)
Abstract
The proteasome pathway is required for cytokine-induced endothelial-leukocyte adhesion molecule expression:
M.A. Read, et al.; Immunity
2
, 493 (1995)
Abstract
Selective inhibitors of the proteasome-dependent and vacuolar pathways of protein degradation in
Saccharomyces cerevisiae
:
D.H. Lee and A.L. Goldberg; J. Biol. Chem.
271
, 27280 (1996)
Abstract
;
Full Text
The human cytomegalovirus US11 gene product dislocates MHC class I heavy chains from the endoplasmic reticulum to the cytosol:
E.J. Wiertz, et al.; Cell
84
, 769 (1996)
Abstract
Proteasome inhibitors activate stress kinases and induce Hsp72. Diverse effects on apoptosis:
A.B. Meriin, et al.; J. Biol. Chem.
273
, 6373 (1998)
Abstract
;
Full Text
Role of proteasomal degradation in the cell cycle-dependent regulation of DNA topoisomerase IIalpha expression:
L. Salmena, et al.; Biochem. Pharmacol.
61
, 795 (2001)
Abstract
Further Categories Containing This Product:
NF-kB Pathway Inhibitors
ALX-340-020
Revised 01-Apr-05
Prostaglandin F2α
SYNONYMS
Dinoprost
9α,11α,15S-Trihydroxy-prosta-5Z,13E-dien-1-oic acid
PRODUCT LINE
Inflammation
PRODUCT CATEGORY
Prostaglandins & Prostaglandin Analogs
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-340-020-M001
1 mg
36.00 USD
ALX-340-020-M005
5 mg
162.00 USD
Product Specification
FORMULA:
C
20
H
34
O
5
MW:
354.5
CAS NUMBER:
551-11-1
PURITY:
≥99%
APPEARANCE:
White crystalline solid.
SOLUBILITY:
Soluble in 100% ethanol, DMSO or dimethyl formamide; also soluble in aqueous buffers.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stable for at least 2 years after receipt when stored at –20°C.
Product Description
Widely distributed prostaglandin occurring in many species.
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:
Add To Cart
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/STABILITY:
Stable for at least 2 years when stored at +4°C in the dark. Stock solutions should be stored in the dark and used within 1 month.
HANDLING:
Keep cool and dry. Protect from light.
IDENTITY:
Identity determined by
1
H-NMR,
13
C-NMR, IR, ESI-MS and UV.
Product Description
Inhibitor of cyclin-dependent kinases (CDK1/cyclin B (IC
50
=10µM), CDK2/cyclin A (IC
50
=2.2µM), CDK2/cyclin E (IC
50
=7.5µM), CDK4/cyclin D1 (IC
50
=12µM), CDK5/p35 (IC
50
=5.5µM)) [1] and of GSK-3β (IC
50
=600nM) [2]. Inhibits inflammatory reaction in delayed-type hypersensitivity in mice [3]. Ligand of human aryl hydrocarbon receptor [4]. Exhibits anti-cancer activity [5] [6].
Product Specific Literature References
[1]
Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases
:
R. Hoessel, et al.; Nature Cell Biol.
1
, 60 (1999)
Abstract
[2]
Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer’s disease. A property common to most cyclin-dependent kinase inhibitors?:
S. Leclerc, et al.; J. Biol. Chem.
276
, 251 (2001)
Abstract
;
Full Text
[3]
Indirubin inhibits inflammatory reactions in delayed-type hypersensitivity
:
T. Kunikata, et al.; Eur. J. Pharmacol.
410
, 93 (2000)
Abstract
[4]
Indirubin and indigo are potent aryl hydrocarbon receptor ligands present in human urine
:
J. Adachi, et al.; J. Biol. Chem.
276
, 31475 (2001)
Abstract
;
Full Text
[5]
Molecular mechanisms of indirubin and its derivatives: novel anticancer molecules with their origin in traditional Chinese phytomedicine:
G. Eisenbrand, et al.; J. Cancer Res. Clin. Oncol.
130
, 627 (2004)
Abstract
[6]
Indirubin enhances tumor necrosis factor-induced apoptosis through modulation of nuclear factor-kappa B signaling pathway:
G. Sethi, et al.; J. Biol. Chem.
281
, 23425 (2006)
Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION
Indirubin is derived from various natural sources, such as
Indigofera indica, Isatis tinctoria
and
I. indigotica
by fermentation, oxidation and the presence of light as a by product of indigo formation. Indirubin is also present in human urine and fetal bovine serum [4]. Preclinical studies of indirubin its confirmed anti-tumor activity. Efficacy against chronic myelocytic leukemia was demonstrated in clinical trials in China [2].
Related Products
ALX-270-271
Indirubin-3'-monoxime
ALX-270-296
Indirubin-5-sulfonic acid . sodium salt
ALX-270-424
5-Iodo-indirubin-3'-monoxime
ALX-430-149
7BIO
ALX-430-157
Me-7BIO
ALX-430-156
6BIO
Further Categories Containing This Product:
GSK-3 Inhibitors
•
Antitumor Reagents Other Products
•
Anti-inflammatory Agents Other Products
ALX-270-360
Revised 21-May-08
Tryptanthrin
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Other Natural Products for Inflammation Research
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-360-M001
1 mg
50.00 USD
ALX-270-360-M005
5 mg
200.00 USD
Product Specification
FORMULA:
C
15
H
8
N
2
O
2
MW:
248.2
CAS NUMBER:
13220-57-0
SOURCE/HOST:
Synthetic.
PURITY:
≥98% (
1
H-NMR, HPLC)
APPEARANCE:
Yellow needles.
SOLUBILITY:
Soluble in DMSO (8mg/ml) or methanol (0.3mg/ml); sparingly soluble in water (2.5µg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
USE/STABILITY:
Stable for at least 2 years after receipt when stored at +4°C in the dark. Stock solutions made in DMSO must be stored in the dark no longer than one month.
HANDLING:
Protect from light and moisture.
IDENTITY:
Identity determined by
1
H-NMR,
13
C-NMR, IR, MS and UV.
Product Description
Potent inhibitor of prostaglandin and leukotriene synthesis in various cell lines. Selective inhibitor of cyclooxygenase 2 (COX-2). Inhibitor of inducible nitric oxide synsthase (iNOS; NOS II) expression. Inhibits the production of IFN-γ and IL-2 after stimulation of Peyer’s patch lymphocytes with
staphylococcal
enterotoxin B (SEB). Inhibits P-glycoprotein (Pgp) (expressed by the MDR1 gene) and reverses doxorubicin (Prod. No.
ALX-380-042
) resistance on breast cancer cells.
Product Specific Literature References
H. Danz, et al.; Arch. Pharm. Suppl. I
333
, 11 (2000)
Identification and isolation of the cyclooxygenase-2 inhibitory principle in Isatis tinctoria:
H. Danz, et al.; Planta Med.
67
, 411 (2001)
Abstract
Inhibitory activity of tryptanthrin on prostaglandin and leukotriene synthesis:
H. Danz, et al.; Planta Med.
68
, 875 (2002)
Abstract
Tryptanthrin inhibits nitric oxide and prostaglandin E(2) synthesis by murine macrophages:
T. Ishihara, et al.; Eur. J. Pharmacol.
407
, 197 (2000)
Abstract
Tryptanthrin inhibits interferon-gamma production by Peyer’s patch lymphocytes derived from mice that had been orally administered staphylococcal enterotoxin
:
Y. Takei, et al.; Biol. Pharm. Bull.
26
, 365 (2003)
Abstract
Tryptanthrin inhibits MDR1 and reverses doxorubicin resistance in breast cancer cells:
S.T. Yu, et al.; BBRC
358
, 79 (2007)
Abstract
General Information
Tryptanthrin occurs as a natural product in various plants, including
Isatis tinctoria, I. indigotica, Polygonum tinctorium, Couroupita guianensis, Wrightia tinctoria
and
Calanthe discolor.
Further Categories Containing This Product:
Leukotrienes Other Products
•
NOS Inhibitors (NOS Induction & Enzyme Activity)
•
Natural Products - Nitric Oxide Pathway Modulators
•
Prostaglandins Other Products
•
COX Inhibitors
ALX-350-109
Revised 29-Nov-07
Panepoxydone
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Natural Products - NF-kB Pathway Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-350-109-MC05
0.5 mg
390.00 USD
Product Specification
FORMULA:
C
11
H
14
O
4
MW:
210.2
SOURCE/HOST:
Isolated from
Lentinus crinitus
.
PURITY:
>95% (HPLC)
FORMULATION:
Yellow oil
SOLUBILITY:
Soluble in DMSO, 100% ethanol or methanol.
SHIPPING:
SHIPPED ON BLUE ICE
SHORT TERM STORAGE:
+4°C
LONG TERM STORAGE:
-20°C
HANDLING:
After reconstitution, prepare aliquots and store at -20°C. Protect from light. Keep cool and dry.
HAZARD:
TOXIC.
Product Description
Antibiotic. Inhibitor of NF-κB activation by preventing the phosphorylation of IκB protein and thereby interrupts the signalling pathway. Strongly inhibits the expression of several NF-κB dependent pro-inflammatory genes.
Product Specific Literature References
Inhibition of NF-kappa B activation by panepoxydone
:
G. Erkel, et al.; BBRC
226
, 214 (1996)
Abstract
Cytokine induction of NO synthase II in human DLD-1 cells: roles of the JAK-STAT, AP-1 and NF-kappaB-signaling pathways
:
H. Kleinert, et al.; Br. J. Pharmacol.
125
, 193 (1998)
Abstract
Naturally occurring and synthetic inhibitors of NF-kappaB functions
:
K. Umezawa, et al.; Anticancer Drug Des.
15
, 239 (2000)
Abstract
Inhibitors of NF-kappaB signaling: design and synthesis of a biotinylated isopanepoxydone affinity reagent
:
J.B. Shotwell, et al.; Bioorg. Med. Chem. Lett.
12
, 3463 (2002)
Abstract
Molecular design and biological activities of NF-kappaB inhibitors
:
K. Umezawa & C. Chaicharoenpong; Mol. Cells
14
, 163 (2002)
Abstract
Influence of the fungal NF-kappaB inhibitor panepoxydone on inflammatory gene expression in MonoMac6 cells:
G. Erkel, et al.; Int. Immunopharmacol.
7
, 612 (2007)
Abstract
Further Categories Containing This Product:
NF-kB Pathway Inhibitors
•
Natural Products - Anti-inflammatory Agents
•
Natural Products with Antibiotic Activity
ALX-260-095
Revised 04-Mar-05
α-MAPI
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Proteases Other Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-260-095-M001
1 mg
80.00 USD
ALX-260-095-M005
5 mg
240.00 USD
Product Specification
FORMULA:
C
30
H
41
N
7
O
6
MW:
595.7
SOURCE/HOST:
Synthetic.
PURITY:
≥95%
APPEARANCE:
White powder.
SOLUBILITY:
Soluble in methanol; soluble in water (2mg/ml) after sonification.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Microbial alkaline proteinase inhibitor (α-MAPI) binds strongly to the active site of the HIV protease.
Product Specific Literature References
Structural elucidation of alpha-MAPI, a novel microbial alkaline proteinase inhibitor, produced by Streptomyces nigrescens:
T. Watanabe, et al.; THL
7
, 625 (1979)
A high throughput assay for inhibitors of HIV-1 protease. Screening of microbial metabolites:
E. Sarubbi, et al.; FEBS Lett.
279
, 265 (1991)
Abstract
First efficient synthesis of alpha-MAPI:
R.J. Broadbridge, et al.; Chem. Commun.
1998
, 1449
ALX-420-036
Revised 21-Jul-05
DICA
SYNONYMS
2-(2,4-Dichlorophenoxy)-
N
-(2-mercaptoethyl)acetamide
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Caspase Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-420-036-M005
5 mg
40.00 USD
ALX-420-036-M025
25 mg
160.00 USD
Product Specification
FORMULA:
C
10
H
11
Cl
2
NO
2
S
MW:
280.2
CAS NUMBER:
613665-26-2
PURITY:
≥98% (TLC)
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in methanol or DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Do not store DMSO solutions for more than 1 day.
HANDLING:
Keep under inert gas. Protect from oxygen.
Product Description
Inhibitor of caspase-3 and caspase-7 binding to an allosteric site and not to the active site.
Product Specific Literature References
Discovery of an allosteric site in the caspases:
J.A. Hardy, et al.; PNAS
101
, 12461 (2004)
Abstract
;
Full Text
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
ALX-420-030
Revised 12-Dec-06
BAY 41-2272
SYNONYMS
3-(4-Amino-5-cyclopropylpyrimidine-2-yl)-1-(2-fluorobenzyl)-1
H
-pyrazolo[3,4-b]pyridine
PRODUCT LINE
Nitric Oxide Pathway
PRODUCT CATEGORY
Guanylyl Cyclases, Guanosine Phosphate Metabolism / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-420-030-M005
5 mg
92.00 USD
ALX-420-030-M025
25 mg
358.00 USD
Product Specification
FORMULA:
C
20
H
17
FN
6
MW:
360.4
PURITY:
≥98%
APPEARANCE:
White to off-white needles.
SOLUBILITY:
Soluble in DMSO, dichloromethane, 100% ethanol or 2-pyrrolidone. Practically insoluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
Product Description
NO-independent activator of soluble guanylyl cyclase (sGC) [1,2]. Activates both isoforms α
1
β
1
and α
1
β
2
of sGC [3]. While the related compound YC-1 (Prod. No.
ALX-420-025
) also acts as a non-specific phosphodiesterase inhibitor, BAY 41-2272 has no effect on phosphodiesterases. Stimulation of sGC is not blocked by high concentrations of NO scavengers (e.g. PTIO, Prod. No.
ALX-430-007
) and the combination of BAY 41-2272 with the NO donor DEA NONOate (Prod. No.
ALX-430-034
) potentiates the activation of sGC. Although BAY 41-2272 alone is not as strong a stimulator of sGC as NO, concentrations as low as 10-100nM stimulate sGC to a level that would be expected to cause biologically important increases in cGMP [1]. ODQ (Prod. No.
ALX-270-034
), a potent and selective inhibitor of sGC, completely inhibited the effect of BAY 41-2272 [1]. The activity of BAY 41-2272 is described in selected literature references [4-6].
Product Specific Literature References
[1]
NO-independent regulatory site on soluble guanylate cyclase
:
J.P. Stasch, et al.; Nature
410
, 212 (2001)
Abstract
[2]
NO-independent regulatory site of direct sGC stimulators like YC-1 and BAY 41-2272
:
E.M. Becker, et al.; BMC Pharmacol.
1
, 13 (2001)
Abstract
;
Full Text
NO-independent stimulators of soluble guanylate cyclase:
A. Straub, et al.; Bioorg. Med. Chem. Lett.
11
, 781 (2001)
Abstract
[3]
BAY 41-2272 activates two isoforms of nitric oxide-sensitive guanylyl cyclase
:
M. Koglin, et al.; BBRC
292
, 1057 (2002)
Abstract
[4]
Cardiorenal and humoral properties of a novel direct soluble guanylate cyclase stimulator BAY 41-2272 in experimental congestive heart failure:
G. Boerrigter, et al.; Circulation
107
, 686 (2003)
Abstract
[5]
BAY 41-2272: a stimulator of soluble guanylyl cyclase induces nitric oxide-dependent penile erection in vivo
:
E. Bischoff, et al.; Urology
61
, 464 (2003)
Abstract
[6]
Macrophage endothelial nitric oxide synthase auto-regulates cellular activation and pro-inflammatory protein expression
:
L. Connelly, et al.; J. Biol. Chem
278
, 26480 (2003)
Abstract
;
Full Text
Antiinflammatory activity of soluble guanylate cyclase: cGMP-dependent down-regulation of P-selectin expression and leukocyte recruitment:
A. Ahluwalia, et al.; PNAS
101
, 1386 (2004)
Abstract
;
Full Text
Identification of residues crucially involved in soluble guanylate cyclase activation:
C. Rothkegel, et al.; FEBS Lett.
580
, 4205 (2006)
Abstract
ALX-270-477
Revised 19-Aug-08
STO-609
SYNONYMS
7-Oxo-7H-benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic acid acetic acid
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
CAM Kinase Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-477-M001
1 mg
45.00 USD
Product Specification
FORMULA:
C
19
H
10
N
2
O
3
· CH
3
COOH
MW:
314.3 . 60.1
CAS NUMBER:
52029-86-4
PURITY:
≥95% (HPLC)
APPEARANCE:
Yellow to orange solid.
SOLUBILITY:
Soluble in DMSO (10mg/ml; warm) or 100mM sodium hydroxide (20mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING:
Protect from light. Hygroscopic.
IDENTITY:
Identity determined by
1
H-NMR.
Product Description