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ALX-151-026
Revised 20-Jun-08
N-Acetyl-Asp-Tyr(2-malonyl)-Val-Pro-Met-Leu-NH2
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Tyrosine Kinase Inhibitors
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ALX-151-026-M001
1 mg
90.00 USD
Product Specification
FORMULA:
C
39
H
57
N
7
O
14
S
MW:
880.0
PURITY:
≥96% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water (1mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Peptide is very unstable.
Product Description
Peptide containing a phosphotyrosyl mimetic. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides:
B. Ye, et al.; J. Med. Chem.
38
, 4270 (1995)
Abstract
Further Categories Containing This Product:
Phosphoinositide 3-kinase [PI(3)K] / Related Products
•
Peptides
ALX-151-027
Revised 17-Jan-05
N-Acetyl-Asp-Tyr(PO3H2)-Val-Pro-Met-Leu-NH2
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Tyrosine Kinase Inhibitors
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ALX-151-027-M001
1 mg
90.00 USD
Product Specification
FORMULA:
C
36
H
57
N
7
O
13
SP
MW:
858.9
PURITY:
≥96%
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Phosphotyrosine containing peptide. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides:
B. Ye, et al.; J. Med. Chem.
38
, 4270 (1995)
Abstract
Further Categories Containing This Product:
Phosphoinositide 3-kinase [PI(3)K] / Related Products
•
Peptides
ALX-270-465
Revised 22-May-07
AS-252424
SYNONYMS
5-[5-(4-Fluoro-2-hydroxyphenyl)-furan-2-ylmethylene)]-thiazolidine-2,4-dione
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
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Format:
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ALX-270-465-M001
1 mg
30.00 USD
ALX-270-465-M005
5 mg
120.00 USD
ALX-270-465-M025
25 mg
480.00 USD
Product Specification
FORMULA:
C
14
H
8
FNO
4
S
MW:
305.3
CAS NUMBER:
900515-16-4
PURITY:
≥98% (
1
H-NMR)
APPEARANCE:
Yellow to brown crystalline solid.
SOLUBILITY:
Soluble in 100% ethanol (10mg/ml), DMSO (20mg/ml) or dimethyl formamide; also soluble in a 1:1 solution of DMSO:PBS, pH 7.4, (0.5mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stable for at least 2 years after receip when stored at -20°C.
Product Description
Potent and selective phosphoinositide 3-kinase (PI(3)K) p110γ inhibitor shown to be selective for class IB PI(3)K-mediated cellular effects.
Product Specific Literature References
Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils:
A.M. Condliffe, et al.; Blood
106
, 1432 (2005)
Abstract
;
Full Text
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma:
V. Pomel, et al.; J. Med. Chem.
49
, 3857 (2006)
Abstract
;
Full Text
ALX-270-461
Revised 25-May-07
AS-604850
SYNONYMS
5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
Ordering Information
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Format:
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ALX-270-461-M001
1 mg
35.00 USD
ALX-270-461-M005
5 mg
130.00 USD
ALX-270-461-M025
25 mg
520.00 USD
Product Specification
FORMULA:
C
11
H
5
F
2
NO
4
S
MW:
285.2
PURITY:
≥98% (HPLC)
APPEARANCE:
Off-white to yellow solid.
SOLUBILITY:
Soluble in acetonitrile (6mg/ml), DMSO (50mg/ml), methanol (9mg/ml) or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
HAZARD:
IRRITANT.
MELTINGPOINT:
200-202°C
Product Description
Potent, cell permeable and ATP-competitive inhibitor of phosphoinositide 3-kinase γ (PI(3)Kγ). Exhibits selectivity over other PI(3)K isoforms.
Product Specific Literature References
Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis:
M. Camps, et al.; Nat. Med.
11
, 936 (2005)
Abstract
Key role of the p110delta isoform of PI3K in B-cell antigen and IL-4 receptor signaling: comparative analysis of genetic and pharmacologic interference with p110delta function in B cells:
A. Bilancio, et al.; Blood
107
, 642 (2006)
Abstract
;
Full Text
ALX-270-462
Revised 09-Oct-07
AS-605240
SYNONYMS
5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-270-462-M001
1 mg
25.00 USD
ALX-270-462-M005
5 mg
80.00 USD
ALX-270-462-M025
25 mg
320.00 USD
Product Specification
FORMULA:
C
12
H
7
N
3
O
2
S
MW:
257.3
PURITY:
≥95% (
1
H-NMR)
APPEARANCE:
Pink to reddish brown solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Packaged under inert gas.
Product Description
Potent, cell permeable and ATP-competitive inhibitor of phosphoinositide 3-kinase γ (PI(3)Kγ). Exhibits selectivity over other PI(3)K isoforms.
Product Specific Literature References
Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis:
M. Camps, et al.; Nat. Med.
11
, 936 (2005)
Abstract
PI3Kgamma inhibition blocks glomerulonephritis and extends lifespan in a mouse model of systemic lupus:
D.F. Barber, et al.; Nat. Med.
11
, 933 (2005)
Abstract
ALX-270-455
Revised 18-Dec-06
Compound 15e
SYNONYMS
3-[4-(4-Morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-phenol
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-270-455-M001
1 mg
50.00 USD
ALX-270-455-M005
5 mg
190.00 USD
Product Specification
FORMULA:
C
16
H
15
N
3
O
2
S
MW:
313.4
CAS NUMBER:
371943-05-4
PURITY:
≥99% (HPLC)
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO or dioxane.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Potent and specific inhibitor of phosphoinositide 3-kinase p110α isoform. Inhibits proliferation of A375 melanoma cells (IC
50
=0.58µM).
Product Specific Literature References
Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110alpha inhibitors:
M. Hayakawa, et al.; Bioorg. Med. Chem.
14
, 6847 (2006)
Abstract
Further Categories Containing This Product:
Antitumor Agents (Anti-proliferative)
ALX-350-118
Revised 22-Sep-08
Deguelin
SYNONYMS
[-]-Deguelin
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-118-M005
5 mg
60.00 USD
ALX-350-118-M025
25 mg
240.00 USD
Product Specification
FORMULA:
C
23
H
22
O
6
MW:
394.4
CAS NUMBER:
522-17-8
MERCK INDEX:
14:
2863
RTECS:
DX1500000
PURITY:
≥95%
APPEARANCE:
Yellow powder.
SOLUBILITY:
Soluble in acetone, acetonitrile or DMSO. Slightly soluble in 100% ethanol. Insoluble in methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
Product Description
Inhibitor of Akt (protein kinase B; PKB) in an
in vitro
lung carcinogenesis progression model. Inhibits cell proliferation - cells accumulate in the G2-M phase of the cell cycle. Induces apoptosis. Exhibits a marked inhibitory effect on mouse skin tumor promotion in an
in vivo
two-stage carcinogenesis test. Inhibits cyclooxygenase-2 (COX-2) expression.
Product Specific Literature References
Deguelin inhibits the growth of colon cancer cells through the induction of apoptosis and cell cycle arrest:
G. Murillo, et al.; Eur. J. Cancer
38
, 2446 (2002)
Abstract
Effects of deguelin on the phosphatidylinositol 3-kinase/Akt pathway and apoptosis in premalignant human bronchial epithelial cells
:
K.H. Chun, et al.; J. Natl. Cancer Inst.
95
, 291 (2003)
Abstract
;
Full Text
Cancer Chemopreventive Activity of Rotenoids from Derris trifoliata
:
C. Ito, et al.; Planta Med.
70
, 8 (2004)
Abstract
Apoptosis induction by the natural product cancer chemopreventive agent deguelin is mediated through the inhibition of mitochondrial bioenergetics.
:
N. Hail, et al.; Apoptosis
9
, 437 (2004)
Abstract
Deguelin-induced inhibition of cyclooxygenase-2 expression in human bronchial epithelial cells:
H.Y. Lee, et al.; Clin. Cancer Res.
10
, 1074 (2004)
Abstract
Further Categories Containing This Product:
Phosphoinositide 3-kinase [PI(3)K] / Related Products
•
Antitumor Agents (Enzyme Inhibitors)
•
Antitumor Agents (Anti-proliferative)
•
COX Inhibitors
•
Natural Products - Antitumor Reagents
•
Antitumor Agents (Apoptosis Inducers)
•
Natural Products - Apoptosis Inducers & Inhibitors
ALX-270-292
Revised 09-Feb-05
1L-6-Hydroxymethyl-chiro-inositol-2-[(R)-2-O-methyl-3-O-octadecylcarbonate]
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
Ordering Information
Product Numbers:
Format:
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ALX-270-292-M001
1 mg
85.00 USD
ALX-270-292-M005
5 mg
330.00 USD
Product Specification
FORMULA:
C
30
H
58
O
10
MW:
578.8
PURITY:
>98%
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in DMSO or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Keep cool and dry.
Product Description
Potent inhibitor of Akt (PKB) (IC
50
=2.0µM). Weak inhibitor of PI(3)K (phosphoinositide 3-kinase) (IC
50
=83µM). Has been shown to inhibit the growth of the following cancer cell lines: HeLa (IC
50
=2.5µM), HT-29 (IC
50
=10µM), MCF-7 (IC
50
=1.2µM) and PC-3 (IC
50
=2.0µM).
Product Specific Literature References
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth:
Y. Hu, et al.; J. Med. Chem.
43
, 3045 (2000)
Abstract
Further Categories Containing This Product:
Akt [PKB] / Related Products
•
Protein Kinase Inhibitors Other Products
•
Antitumor Agents (Enzyme Inhibitors)
ALX-385-007
Revised 07-Oct-08
Luteolin
SYNONYMS
3',4',5,7-Tetrahydroxyflavone
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Flavones
Ordering Information
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ALX-385-007-M010
10 mg
15.00 USD
ALX-385-007-M050
50 mg
45.00 USD
Product Specification
FORMULA:
C
15
H
10
O
6
MW:
286.2
CAS NUMBER:
491-70-3
MERCK INDEX:
14:
5614
RTECS:
LK9275210
PURITY:
≥90%
APPEARANCE:
Yellow powder.
SOLUBILITY:
Soluble in methanol, alkaline solutions; slightly soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+20°C
Product Description
Antioxidant flavonoid. Inhibits VEGF-induced angiogenesis. Inhibitor of phosphoinositide 3-kinase (PI(3)K). Inhibitor of fatty acid synthase (FAS). Apoptosis inducer.
Product Specific Literature References
Structure-antioxidant activity relationships of flavonoids and phenolic acids:
C.A. Rice-Evans, et al.; Free Radical Biol. & Med.
20
, 933 (1996), (Review)
Abstract
Luteolin inhibits vascular endothelial growth factor-induced angiogenesis; inhibition of endothelial cell survival and proliferation by targeting phosphatidylinositol 3'-kinase activity
:
E. Bagli, et al.; Cancer Res.
64
, 7936 (2004)
Dietary flavonoids: bioavailability, metabolic effects, and safety:
J.A. Ross & C.M. Kasum; Annu. Rev. Nutr.
221
, 19 (2002), (Review)
Abstract
Pharmacological inhibitors of Fatty Acid Synthase (FASN)--catalyzed endogenous fatty acid biogenesis: a new family of anti-cancer agents?:
R. Lupu & J. A. Menendez; Curr. Pharm. Biotechnol.
7
, 483 (2006), (Review)
Abstract
Further Categories Containing This Product:
Natural Products - Other Signal Transduction Pathway Modulators
•
Fatty Acid Synthase [FAS] / Related Products
•
Free Radical Scavengers
•
Phosphoinositide 3-kinase [PI(3)K] / Related Products
•
Natural Products for Angiogenesis Research
•
Natural Products - Apoptosis Inducers & Inhibitors
•
Natural Products - Antioxidants
ALX-270-038
Revised 03-Jan-08
LY-294,002
SYNONYMS
2-(4-Morpholinyl)-8-phenyl-4
H
-1-benzopyran-4-one
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-038-M001
1 mg
30.00 USD
ALX-270-038-M005
5 mg
50.00 USD
ALX-270-038-M025
25 mg
245.00 USD
Product Specification
FORMULA:
C
19
H
17
NO
3
MW:
307.4
CAS NUMBER:
154447-36-6
PURITY:
≥99%
APPEARANCE:
White to off-white crystalline solid.
SOLUBILITY:
Soluble in DMSO, 100% ethanol or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
Product Description
Potent, cell permeable, highly specific inhibitor of PI(3)K (phosphoinositide 3-kinase) that acts on the ATP-binding site of the enzyme. Sensitizes tumor cells to drug-induced apoptosis independent of its PI3K inhibitory activity. For a negative control see LY-303,511 (Prod. No.
ALX-270-410
).
Product Specific Literature References
A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4- morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002):
C.J. Vlahos, et al.; J. Biol. Chem.
269
, 5241 (1994)
Abstract
;
Full Text
Investigation of neutrophil signal transduction using a specific inhibitor of phosphatidylinositol 3-kinase:
C.J. Vlahos, et al.; J. Immunol.
154
, 2413 (1995)
Abstract
LY294002 and LY303511 Sensitize Tumor Cells to Drug-Induced Apoptosis via Intracellular Hydrogen Peroxide Production Independent of
