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ALX-270-387
Revised 18-Jul-07
3-Amino-1H-pyrazolo[3,4-b]quinoxaline
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-387-M001
1 mg
40.00 USD
ALX-270-387-M005
5 mg
160.00 USD
Product Specification
FORMULA:
C
9
H
7
N
5
MW:
185.2
CAS NUMBER:
40254-90-8
PURITY:
≥98% (HPLC)
APPEARANCE:
Red solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
+4°C
HANDLING:
Protect from light. Packaged under inert gas.
Product Description
Selective inhibitor of CDK1/cyclin B (IC
50
=600nM), CDK5/p25 (IC
50
=400nM) and GSK-3β (IC
50
=1µM). Does not inhibit Cdc25 phosphatase activity (IC
50
>10µM).
Product Specific Literature References
Pyrazolo[3,4-b]quinoxalines. A new class of cyclin-dependent kinases inhibitors
:
M.A. Ortega, et al.; Bioorg. Med. Chem.
10
, 2177 (2002)
Abstract
Further Categories Containing This Product:
GSK-3 Inhibitors
ALX-270-388
Revised 18-Jul-07
Benfluorene
SYNONYMS
Ethyl-(6-hydroxy-4-phenylbenzo[4,5]furo[2,3-
b
])pyridine-3-carboxylate
1-Aza-9-oxafluorene 5a
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-388-M001
1 mg
70.00 USD
ALX-270-388-M005
5 mg
280.00 USD
Product Specification
FORMULA:
C
20
H
15
NO
4
MW:
333.3
PURITY:
≥95% (HPLC)
APPEARANCE:
Brownish powder.
SOLUBILITY:
Soluble in DMSO or 100% ethanol. Insoluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
Product Description
Selective inhibitor of CDK1 (IC
50
=28.8µM) with P-glycoprotein-modulating properties (inhibitory activity ratio 9.5 at 7µM). Weakly inhibits CDK5 (6% inhibition at 10µM) with no effect on CDK2 and CDK4 (IC
50
>100µM).
Product Specific Literature References
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties
:
K. Brachwitz, et al.; J. Med. Chem.
46
, 876 (2003)
Abstract
ALX-270-389
Revised 17-Jul-07
Elbfluorene
SYNONYMS
3-Acetyl-6-hydroxy-4-phenylbenzo[4,5]furo[2,3-
b
]pyridine
1-Aza-9-oxafluorene 5b
PRODUCT LINE
DNA Regulation / Transcription
PRODUCT CATEGORY
DNA Repair Other Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-389-M001
1 mg
75.00 USD
ALX-270-389-M005
5 mg
300.00 USD
Product Specification
FORMULA:
C
19
H
13
NO
3
MW:
303.3
PURITY:
≥95% (HPLC)
APPEARANCE:
Off-white to brownish powder.
SOLUBILITY:
Soluble in DMSO. Insoluble in water or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
Product Description
Selective inhibitor of CDK1/cyclin B (IC
50
=4.2µM) with some P-glycoprotein-modulating properties (inhibitory activity ratio 1.26 at 7µM). Weakly inhibits CDK5/p25 (6% inhibition at 10µM) with no effect on CDK2/cyclin E and CDK4/cyclin D1 (IC
50
>100µM).
Product Specific Literature References
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties
:
K. Brachwitz, et al.; J. Med. Chem.
46
, 876 (2003)
Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors
ALX-270-390
Revised 09-Jan-08
Bohemine
SYNONYMS
6-Benzylamino-2-(3-hydroxypropylamino)-9-isopropylpurine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-390-M001
1 mg
40.00 USD
ALX-270-390-M005
5 mg
120.00 USD
Product Specification
FORMULA:
C
18
H
24
N
6
O
MW:
340.4
CAS NUMBER:
189232-42-6
PURITY:
≥97% (HPLC)
APPEARANCE:
White to off-white crystalline solid.
SOLUBILITY:
Soluble in DMSO, dimethyl formamide, 100% ethanol or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from moisture.
Product Description
Cell permeable inhibitor of CDK1 (IC
50
=1.1µM) and CD2 (IC
50
=600nM). Arrests cell cycle in the G
1
/S boundary and activates mature bovine oocytes.
Product Specific Literature References
Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds
:
L. Havlicek, et al.; J. Med. Chem.
40
, 408 (1997)
Abstract
Treatment of Vicia faba root tip cells with specific inhibitors to cyclin-dependent kinases leads to abnormal spindle formation
:
P. Binarova, et al.; Plant J.
16
, 697 (1998)
Abstract
Activation of bovine oocytes by specific inhibition of cyclin-dependent kinases
:
R. Alberio, et al.; Mol. Reprod. Dev.
55
, 422 (2000)
Abstract
Proteomics approach in classifying the biochemical basis of the anticancer activity of the new olomoucine-derived synthetic cyclin-dependent kinase inhibitor, bohemine
:
H. Kovarova, et al.; Electrophoresis
21
, 3757 (2000)
Abstract
In vivo metabolism of 2,6,9-trisubstituted purine-derived cyclin-dependent kinase inhibitor bohemine in mice: glucosidation as the principal metabolic route
:
Z. Chmela, et al.; Drug. Metab. Dispos.
29
, 326 (2001)
Abstract
;
Full Text
Antiproliferative effect of plant cytokinin analogues with an inhibitory activity on cyclin-dependent kinases:
K. Vermeulen, et al.; Leukemia
16
, 299 (2002)
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors/Related Products
ALX-270-391
Revised 18-Jul-07
CGP 74514A
SYNONYMS
N-(
cis
-
2-Aminocyclohexyl)-N-(3-chlorophenyl)-9-ethyl-9
H
-purine-2,6-diamine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-391-M001
1 mg
35.00 USD
ALX-270-391-M005
5 mg
70.00 USD
ALX-270-391-M025
25 mg
280.00 USD
Product Specification
FORMULA:
C
19
H
24
ClN
7
MW:
385.9
PURITY:
≥95%
APPEARANCE:
White to yellow solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Packaged under inert gas.
Product Description
Cell permeable, potent and selective inhibitor of CDK1/cyclin B (IC
50
=25nM). Reported to affect the activities of other kinases only at much higher concentrations: PKCα (IC
50
=6.1µM), PKA (IC
50
=125µM) and EGFR (IC
50
>10µM). Induces mitochondrial damage and apoptosis in several human leukemia cell lines (>3µM).
Product Specific Literature References
2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors
:
P. Imbach, et al.; Bioorg. Med. Chem. Lett.
9
, 91 (1999)
Abstract
The lethal effects of pharmacological cyclin-dependent kinase inhibitors in human leukemia cells proceed through a phosphatidylinositol 3-kinase/Akt-dependent process
:
C. Yu, et al.; Cancer Res.
63
, 1822 (2003)
Abstract
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
ALX-270-392
Revised 08-Dec-04
3-(2-Chloro-3-indolylmethylene)-1,3-dihydroindol-2-one
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-392-M001
1 mg
35.00 USD
ALX-270-392-M005
5 mg
130.00 USD
Product Specification
FORMULA:
C
17
H
11
ClN
2
O
MW:
294.7
PURITY:
≥95% (HPLC)
APPEARANCE:
Yellow to orange solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
+4°C
USE/STABILITY:
Stable for 3 years after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:
Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C. Protect from light.
Product Description
Selective, ATP-competitive inhibitor of CDK1/cyclin B (IC
50
=5.8µM) and CDK5 (IC
50
=25µM). Does not inhibit GSK-3β (IC
50
>100µM). Exhibits potent antiproliferative properties (IC
50
=2µM in HeLa cells).
Product Specific Literature References
Potential antitumor agents. 25 [1]. Synthesis and cytotoxic activity of 3-(2-chloro-3-indolylmethylene)1,3-dihydroindol-2-ones
:
A. Andreani, et al.; Anticancer Res.
16
, 3585 (1996)
Abstract
Imidazo[2,1 -b]thiazolylmethylene- and indolylmethylene-2-indolinones: a new class of cyclin-dependent kinase inhibitors. Design, synthesis, and CDK1/cyclin B inhibition
:
A. Andreani, et al.; Anticancer Drug Des.
15
, 447 (2000)
Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors)
•
Antitumor Agents (Anti-proliferative)
ALX-270-393
Revised 17-Jul-07
CVT-313
SYNONYMS
6-(4-Methoxybenzylamino)-2-[
bis
(2-hydroxyethylamino)]-9-isopropylpurine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-393-M001
1 mg
60.00 USD
ALX-270-393-M005
5 mg
240.00 USD
Product Specification
FORMULA:
C
20
H
28
N
6
O
3
MW:
400.5
PURITY:
≥98% (HPLC)
APPEARANCE:
White crystalline solid.
SOLUBILITY:
Soluble in DMSO, dimethyl formamide or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from moisture.
Product Description
Specific inhibitor of CDK2/cyclin A (IC
50
=500nM) and CDK2/cyclin E (IC
50
=500nM). Also inhibits CDK1/cyclin B (IC
50
=4.2µM) and CDK4/cyclin D1 (IC
50
=215µM).
Product Specific Literature References
CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation
:
E.E. Brooks, et al.; J. Biol. Chem.
272
, 29207 (1997)
Abstract
;
Full Text
Histone H1 phosphorylation by Cdk2 selectively modulates mouse mammary tumor virus transcription through chromatin remodeling
:
R.N. Bhattacharjee, et al.; Mol. Cell. Biol.
21
, 5417 (2001)
Abstract
;
Full Text
ALX-270-394
Revised 21-Sep-05
NU2058
SYNONYMS
O
6
-Cyclohexylmethylguanine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-394-M005
5 mg
80.00 USD
ALX-270-394-M025
25 mg
290.00 USD
Product Specification
FORMULA:
C
12
H
17
N
5
O
MW:
247.3
CAS NUMBER:
161058-83-9
SOLUBILITY:
Soluble in water or DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HAZARD:
IRRITANT.
Product Description
Competitive inhibitor of CDK1/cyclin B (IC
50
=5µM) and CDK2/cyclin A (IC
50
=12µM). Pharmacologically distinct from the relative specific inhibitor of CDK1/2 roscovitine (Prod. No.
ALX-350-251
).
Product Specific Literature References
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles:
C.E. Arris, et al.; J. Med. Chem.
43
, 2797 (2000)
Abstract
The development of a CDK2-docking site peptide that inhibits p53 and sensitizes cells to death:
M. Ferguson, et al.; Cell Cycle
3
, 80 (2004)
Abstract
ALX-270-395
Revised 08-Dec-04
2-Hydroxybohemine
SYNONYMS
6-(2-Hydroxybenzylamino)-2-(3-hydroxypropylamino)-9-isopropylpurine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-395-M001
1 mg
60.00 USD
ALX-270-395-M005
5 mg
240.00 USD
Product Specification
FORMULA:
C
18
H
24
N
6
O
2
MW:
356.4
PURITY:
≥95%
FORMULATION:
Off-white solid.
SOLUBILITY:
100µM soluble in DMSO, dimethyl formamide or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Description
Inhibitor of CDK1 (IC
50
=100nM) and CDK2 (IC
50
=80nM).
Product Specific Literature References
Antiproliferative effect of plant cytokinin analogues with an inhibitory activity on cyclin-dependent kinases
:
K. Vermeulen, et al.; Leukemia
16
, 299 (2002)
Abstract
ALX-270-396
Revised 07-Mar-08
Olomoucine II
SYNONYMS
6-(2-Hydroxybenzylamino)-2(R)-[[1-hydroxymethyl)propyl]amino]-9-isopropylpurine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-396-M001
1 mg
42.00 USD
ALX-270-396-M005
5 mg
145.00 USD
Product Specification
FORMULA:
C
19
H
26
N
6
O
2
MW:
370.5
CAS NUMBER:
500735-47-7
PURITY:
≥98%
APPEARANCE:
White to off-white crystalline solid.
SOLUBILITY:
Soluble in DMSO, dimethyl formamide or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Selective inhibitor of CDK1/cyclin B (IC
50
=20nM). Potent cytotoxin in tumor cells: IC
50
=5.3µM against MCF7 cells, IC
50
=11.1µM against K562 cells, IC
50
=3.0µM against CEM cells, IC
50
=6.3µM against HOS cells, and IC
50
=6.3µM against G361 cells.
Product Specific Literature References
Synthesis and biological activity of olomoucine II
:
V. Krystof, et al.; Bioorg. Med. Chem. Lett.
12
, 3283 (2002)
Abstract
Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor:
V. Krystof, et al.; Cell Mol. Life Sci.
62
, 1763 (2005)
Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors)
•
Antitumor Agents (Apoptosis Inducers)
ALX-270-397
Revised 09-Jan-08
Olomoucine, N9-Isopropyl-
