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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-270-385
Revised 07-Jan-09
Aloisine A
SYNONYMS
RP107
7-
n
-Butyl-6-(4-hydroxyphenyl)[5
H
]pyrrolo[2,3-
b
]pyrazine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-385-M001
1 mg
30.00 USD
Product Specification
FORMULA:
C
16
H
17
N
3
O
MW:
267.3
PURITY:
≥95%
APPEARANCE:
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, selective, reversible and ATP-competitive inhibitor of CDK1/cyclin B (IC
50
=150nM), CDK2/cyclin A (IC
50
=120nM), CDK2/cyclin E (IC
50
=400nM), CDK5/p25
(IC
50
=200nM), CDK5/p35 (IC
50
=160nM) and GSK-3α (IC
50
=500nM). Also inhibits GSK-3β (IC
50
=650nM) and c-Jun N-terminal kinase (JNK) (IC
50
~3-10µM). Poor inhibitor of CK1, CK2, CDK4/cyclin D1, MAPKK, PKA, PKG, PKCs and c-raf (IC
50
≥100µM). Blocks cell cycle in both G1 and G2 phase.
Product Specific Literature References
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects
:
Y. Mettey, et al.; J. Med. Chem.
46
, 222 (2003)
Abstract
Further Categories Containing This Product:
GSK-3 Inhibitors
JNK [SAPK1] / Related Products
Cell Cycle Blockers & Inhibitors / Related Products
ALX-270-386
Revised 24-Feb-05
Aloisine
SYNONYMS
RP106
7-
n
-Butyl-6-(4-methoxyphenyl)[5
H
]pyrrolo[2,3-
b
]pyrazine
PRODUCT LINE
Cell Cycle
PRODUCT CATEGORY
CDK & Cyclin Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-386-M001
1 mg
25.00 USD
Product Specification
FORMULA:
C
17
H
19
N
3
O
MW:
281.4
PURITY:
≥95%
APPEARANCE:
Off-white solid.
SOLUBILITY:
Soluble in DMSO or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Protect from light. Packaged under inert gas.
Product Description
Potent, cell permeable, selective ATP-competitive inhibitor of CDK1/cyclin B (IC
50
=700nM), CDK5/p25 (IC
50
=1.5µM), and GSK-3 (IC
50
=920nM).
Product Specific Literature References
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects
:
Y. Mettey, et al.; J. Med. Chem.
46
, 222 (2003)
Abstract
Further Categories Containing This Product:
GSK-3 Inhibitors
Cell Cycle Blockers & Inhibitors / Related Products
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:
Add To Cart
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:
Add To Cart
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 11-Sep-08
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:
Add To Cart
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
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes:
B. Voigt, et al.; Bioorg. Med. Chem. Lett.
15
, 823 (2005)
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:
Add To Cart
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-08
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:
Add To Cart
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
CAS NUMBER:
220749-41-7
PURITY:
≥95% (HPLC)
APPEARANCE:
Yellow to orange solid.
SOLUBILITY:
Soluble in DMSO (200mg/ml).
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. Protect from light. After reconstitution, prepare aliquots and store at -20°C.
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 (Anti-proliferative)
Antitumor Agents (Enzyme Inhibitors)
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:
