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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:
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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:
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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-
SYNONYMS
6-Benzylamino-2-(2-hydroxyethylamino)-9-Isopropylpurine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-397-M001
1 mg
40.00 USD
ALX-270-397-M005
5 mg
120.00 USD
Product Specification
FORMULA:
C
17
H
22
N
6
O
MW:
326.4
CAS NUMBER:
158982-15-1
PURITY:
≥98% (HPLC)
APPEARANCE:
White to off-white crystalline solid.
SOLUBILITY:
Soluble in DMSO or dimethyl formamide; sparingly soluble in methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stock solutions are stable for 3 months when stored at -20°C.
Product Description
Inhibitor of CDK1/cyclin B (IC
50
=2µM) and CDK5/p35 (IC
50
=3µM).
Product Specific Literature References
Inhibition of cyclin-dependent kinases by purine analogues
:
J. Vesely, et al.; Eur. J. Biochem.
224
, 771 (1994)
Abstract
Cassette dosing pharmacokinetics of a library of 2,6,9-trisubstituted purine cyclin-dependent kinase 2 inhibitors prepared by parallel synthesis:
F.I. Raynaud, et al.; Mol. Cancer Ther.
3
, 353 (2004)
Abstract
ALX-270-398
Revised 06-Feb-05
PNU 112455A . hydrochloride
SYNONYMS
N
4
-(6-Aminopyrimidin-4-yl)-sulfanilamide . HCl
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
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ALX-270-398-M001
1 mg
34.00 USD
ALX-270-398-M005
5 mg
135.00 USD
Product Specification
FORMULA:
C
10
H
11
N
5
O
2
S . HCl
MW:
265.3 . 36.5
PURITY:
≥95%
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO or water.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light and moisture. Packaged under inert gas. Hygroscopic.
Product Description
Selective and ATP-competitive inhibitor of CDK2/cyclin E (K
i
=2µM) and CDK5/p25 (K
i
=2µM). Binds to the ATP-binding pocket of CDK2. Does not affect the activities of c-met, IGF-1 receptor tyrosine kinase, cAMP-dependent kinase and ERK2 at concentrations as high as 100µM.
Product Specific Literature References
The cyclin-dependent kinases cdk2 and cdk5 act by a random, anticooperative kinetic mechanism
:
P.M. Clare, et al.; J. Biol. Chem.
276
, 48292 (2001)
Abstract
;
Full Text
ALX-270-400
Revised 31-Mar-05
SU 9516
SYNONYMS
3-[1-(3
H
-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
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ALX-270-400-M005
5 mg
80.00 USD
ALX-270-400-M025
25 mg
320.00 USD
Product Specification
FORMULA:
C
13
H
11
N
3
O
2
MW:
241.3
PURITY:
≥95%
APPEARANCE:
Yellow to orange solid.
SOLUBILITY:
Soluble in DMSO (10mg/ml).
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
+4°C
HANDLING:
Protect from light. Packaged under inert gas.
Product Description
Cell permeable, potent, selective and ATP-competitive inhibitor of CDK2/cyclin A (IC
50
=22nM), CDK1/cyclin B (IC
50
=40nM) and CDK4/cyclin D1 (IC
50
=200nM). Has no effect on the activity of PKC, p38, PDGFRβ and EGFR (IC
50
>10µM). Displays anti-proliferative and pro-apoptotic properties in tumor cells.
Inhibits proliferation of growth factor-stimulated colon carcinoma cells by binding to CDK2 and thus preventing the phosphorylation of pRb and its dissociation from E2F.
Product Specific Literature References
A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells
:
M.E. Lane, et al.; Cancer Res.
61
, 6170 (2001)
Abstract
SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells
:
B. Yu, et al.; Biochem Pharmacol.
64
, 1091 (2002)
Abstract
SU9516: biochemical analysis of cdk inhibition and crystal structure in complex with cdk2
:
D.J. Moshinsky, et al.; BBRC
310
, 1026 (2003)
Abstract
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors
:
X. Li, et al.; Bioorg. Med. Chem. Lett.
13
, 1939 (2003)
Abstract
Further Categories Containing This Product:
Antitumor Agents (Anti-proliferative)
•
Antitumor Agents (Enzyme Inhibitors)
•
Antitumor Agents (Apoptosis Inducers)
ALX-270-403
Revised 12-Jun-08
2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
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ALX-270-403-M001
1 mg
115.00 USD
Product Specification
FORMULA:
C
20
H
10
BrN
3
O
2
MW:
404.2
PURITY:
≥95% (HPLC)
APPEARANCE:
Yellow solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
+4°C
USE/STABILITY:
Stock solutions are stable for up to 2 months if stored at -20°C.
HANDLING:
Packaged under inert gas. Protect from light. After reconstitution, prepare aliquots and store at -20°C.
HAZARD:
TOXIC.
IDENTITY:
Identity determined by NMR.
Product Description
Cell permeable, unsymmetrical compound that displays antiproliferative properties. Potent, selective and ATP-competitive inhibitor of CDK4/cyclin D1 (IC
50
=76nM), CDK2/cyclin E (IC
50
=520nM) and CDK1/cyclin B (IC
50
=2.1µM). Shows little activity towards CaMKII, PKA and GSK-3β (IC
50
>20µM).
Product Specific Literature References
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors
:
G. Zhu, et al.; J. Med. Chem.
46
, 2027 (2003)
Abstract
ALX-270-419
Revised 08-Oct-08
NU6102
SYNONYMS
O
6
-Cyclohexylmethyl-2-(4’-sulfamoylanilino)purine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-419-M001
1 mg
50.00 USD
ALX-270-419-M005
5 mg
145.00 USD
Product Specification
FORMULA:
C
18
H
22
N
6
O
3
S
MW:
402.5
PURITY:
≥95%
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Packaged under inert gas.
HAZARD:
MAY BE CARCINOGENIC. HARMFUL.
Product Description
1,000-fold more potent inhibitor of CDK1/cyclin B (IC
50
=9.5nM) and CDK2/cyclin A3 (IC
50
=5.4nM) than NU2058 (Prod. No.
ALX-270-394
). Selective for CDK1 and CDK2 compared to CDK4/D1 (IC
50
=1.6µM), DYRK1A (IC
50
=0.9µM), PDK1 (IC
50
=0.8µM) and ROCKII (IC
50
=0.6µM).
Product Specific Literature References
Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor
:
T.G. Davies, et al.; Nat. Struct. Biol.
9
, 745 (2002)
Abstract
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2
:
K.L. Sayle, et al.; Bioorg. Med. Chem. Lett.
13
, 3079 (2003)
Abstract
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2
:
I.R. Hardcastle, et al.; J. Med. Chem.
47
, 3710 (2004)
Abstract
Further Categories Containing This Product:
Carcinogens & Tumor Promoters Other Products
ALX-270-424
Revised 13-Feb-07
5-Iodo-indirubin-3'-monoxime
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
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ALX-270-424-M001
1 mg
90.00 USD
Product Specification
FORMULA:
C
16
H
10
IN
3
O
2
MW:
403.2
PURITY:
≥98% (
1
H-NMR)
APPEARANCE:
Dark red solid.
SOLUBILITY:
Soluble in DMSO (1M).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Description
Potent inhibitor of GSK-3β (IC
50
=9nM). Also inhibits CDK1/cyclin B (IC
50
=25nM) and CDK5/p25 (IC
50
=20nM) by binding to the ATP-binding pocket.
Product Specific Literature References
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
Related Products
ALX-270-271
Indirubin-3'-monoxime
ALX-270-361
Indirubin
ALX-270-296
Indirubin-5-sulfonic acid . sodium salt
ALX-430-149
7BIO
ALX-430-156
6BIO
ALX-430-157
Me-7BIO
Further Categories Containing This Product:
GSK-3 Inhibitors
ALX-270-441
Revised 18-Aug-08
NU6140
