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Cell Cycle
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ALX-270-439 Revised 18-Sep-06
Trans-24
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SYNONYMS (5R,11aS)-2-Benzyl-5-(3-hydroxyphenyl)-6H-1,2,3,5,11,11a-hexahydroimidazo[1,5-b]-β-carboline-1,3-dione
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY Cell Cycle Blockers & Inhibitors / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-439-M001   1 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C26H21N3O3
MW: 423.5
CAS NUMBER: 869304-55-2
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 6 months when stored at -20°C in the dark.
HANDLING: Protect from light.
HAZARD: HARMFUL.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Potent, cell permeable non-tubulin-interacting mitosis inhibitor. Blocks mitosis (IC50=650nM) by binding to the mitotic kinesin Eg5.
Product Specific Literature References
Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5: N. Sunder-Plassmann, et al.; Bioorg. Med. Chem. 13, 6094 (2005) Abstract
Further Categories Containing This Product:
Kinesin & Kinesin-like Proteins / Related Products
 
 
ALX-270-441 Revised 18-Aug-08
NU6140
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SYNONYMS 4-(6-Cyclohexylmethoxy-9H-purin-2-ylamino)-N,N-diethylbenzamide
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-441-M005   5 mg 185.00 USD Add To Cart
Product Specification
FORMULA: C23H30N6O2
MW: 422.5
CAS NUMBER: 444723-13-1
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (10mg/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: Packaged under inert gas. Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.
IDENTITY: Identity determined by NMR.

Product Description
Highly cell permeable purine compound that acts as a selective and ATP-competitive inhibitor of CDKs (IC50=6.6µM, 0.41µM, 5.5µM, 15µM and 3.9µM for CDK1/cyclin B, CDK2/cyclin A, CDK4/cyclin D, CDK5/p25 and CDK7/cyclin H) and displays anticancer properties. Causes cell cycle arrest at the G2/M phase and induces apoptosis by activating caspases and downregulating survivin.
Product Specific Literature References
Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation: M. Pennati, et al.; Mol. Cancer Ther. 4, 1328 (2005) Abstract
Further Categories Containing This Product:
Survivin [TIAP] • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-270-442 Revised 21-Oct-08
CDK1/2 Inhibitor III
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SYNONYMS 5-Amino-3-((4-(aminosulfonyl)phenyl)amino)-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-442-M001   1 mg 118.00 USD Add To Cart
Product Specification
FORMULA: C15H13F2N7O2S2
MW: 425.4
CAS NUMBER: 443798-55-8
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (10mg/ml), tetrahydro-furan or acetone.
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.
HAZARD: HARMFUL.
IDENTITY: Identity determined by NMR.

Product Description
Cell permeable triazolo-diamine compound that displays anti-proliferative properties in various human cancer cells (IC50=20nM, 35nM and 92nM in HCT-116, HeLa, and A375 cells). Acts as a highly potent, ATP-competitive inhibitor of CDK1/cyclin B and CDK2/cyclin A (IC50=600pM and 500pM) with selectivity over VEGF-R2 and GSK-3β (IC50=32nM and 140nM).
Product Specific Literature References
1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities: R. Lin, et al.; J. Med. Chem. 48, 4208 (2005) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • GSK-3 Inhibitors • VEGFs & VEGF-Rs Other Products • Antitumor Agents (Anti-proliferative)
 
 
ALX-270-463 Revised 22-Apr-08
RO-3306
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SYNONYMS (5Z)-2-((Thiophen-2-yl)methylamino)-5-((quinolin-6-yl)methylene)thiazol-4(5H)-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-463-M001   1 mg 50.00 USD Add To Cart
ALX-270-463-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C18H13N3OS2
MW: 351.4
CAS NUMBER: 872573-93-8
PURITY: ≥95% (1H-NMR)
APPEARANCE: Brown solid.
SOLUBILITY: Soluble in DMSO (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 6 months after receipt when stored at -20°C in the dark.
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Inhibitor of CDK1/cyclin B1 and CDK1/cyclin A. Reversibly arrests human cells at the G2/M border of the cell cycle. Allows for effective cell synchronisation in early mitosis.
Product Specific Literature References
Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1: L.T. Vassilev, et al.; PNAS 103, 10660 (2006) Abstract; Full Text
Cell cycle synchronization at the G2/M phase border by reversible inhibition of CDK1: L.T. Vassilev; Cell Cycle 5, 2555 (2006) Abstract; Full Text
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-270-487 Revised 16-Sep-08 New product
BML-259
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SYNONYMS N-(5-Isopropylthiazol-2-yl)phenylacetamide
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-487-M005   5 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C14H16N2OS
MW: 260.4
CAS NUMBER: 267654-00-2
PURITY: ≥98% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: 30mg/ml soluble in DMSO or dimethyl formamide, 0.25mg/ml soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.

Product Description
Potent inhibitor of CDK5 (IC50 = 64nM) and CDK2 / cyclin E (IC50 = 98nM).
Product Specific Literature References
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer’s disease: C.J. Helal, et al.; Bioorg. Med. Chem. Lett. 14, 5521 (2004) Abstract
 
 
ALX-303-003 Revised 29-Jan-05
D-erythro-Sphingosine, N-Hexanoyl-
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SYNONYMS N-Hexanoyl-D-erythro-sphingosine
C6-Ceramide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Ceramides / Cerebrosides / Sphingolipids / Related Products
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ALX-303-003-M001   1 mg 38.00 USD Add To Cart
ALX-303-003-M005   5 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C24H47NO3
MW: 397.6
CAS NUMBER: 124753-97-5
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Cell permeable, biologically active, nonphysical ceramide analog. Activates protein phosphatase 2A and MAP kinase (MAPK/ERK). Induces an arrest at the G0/G1 transition of the cell cycle. Inhibits diacylglycerol accumulation and phospholipase D activation in fibroblasts. Induces apoptosis.
Product Specific Literature References
Ceramide stimulates a cytosolic protein phosphatase: R.T. Dobrowsky & Y.A. Hannun; J. Biol. Chem. 267, 5048 (1992) Abstract; Full Text
Sphingomyelinase and ceramide activate mitogen-activated protein kinase in myeloid HL-60 cells: M. A. Raines, et al.; J. Biol. Chem. 268, 14572 (1993) Abstract; Full Text
Ceramide activates heterotrimeric protein phosphatase 2A: R.T. Dobrowsky, et al.; J. Biol. Chem. 268, 15523 (1993) Abstract; Full Text
Induction of apoptotic DNA damage and cell death by activation of the sphingomyelin pathway: W.D. Jarvis, et al.; PNAS 91, 73 (1994) Abstract; Full Text
Identification of a defect in the phospholipase D/diacylglycerol pathway in cellular senescence: M.E. Venable, et al.; J. Biol. Chem. 269, 26040 (1994) Abstract; Full Text
Role for ceramide in cell cycle arrest: S. Jayadev, et al.; J. Biol. Chem. 270, 2047 (1995) Abstract; Full Text
Further Categories Containing This Product:
Phospholipase D / Related Products • MAPK Pathway Activators • Apoptosis Inducers & Inhibitors Other Products • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-340-047 Revised 08-Jul-08
Prostaglandin A2
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SYNONYMS Medullin
Prosta-5,10,13-trien-1-oic acid, 15-hydroxy-9-oxo-, (5Z,13E,15S)-
PRODUCT LINE Inflammation
PRODUCT CATEGORY Prostaglandins & Prostaglandin Analogs
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ALX-340-047-M001   1 mg 33.00 USD Add To Cart
ALX-340-047-M005   5 mg 147.00 USD Add To Cart
Product Specification
FORMULA: C20H30O4
MW: 334.5
CAS NUMBER: 13345-50-1
PURITY: ≥98%
FORMULATION: Liquid. Solution in methyl acetate.
SOLUBILITY: Soluble in 100% ethanol (100mg/ml), DMSO (50mg/ml) or dimethyl formamide (75mg/ml); slightly soluble in PBS, pH 7.2 (2.4mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. PGA2 will be degraded to PGB2 in basic solutions (pH > 7.4). We do not recommend storing aqueous solutions for more than one day.

Product Description
Blocks cell cycle at the G1 and G2/M phase [1] by inhibiting G1 phase cyclin dependent kinases [2] downregulating cyclin D1 [3]. Modulates all three aspects of the glutathione-mediated biotransformation system, i.e. GSH levels, glutathione S-transferase activity and transport of GSH conjugates [4].
Product Specific Literature References
[1] Prostaglandin A2 blocks the activation of G1 phase cyclin-dependent kinase without altering mitogen-activated protein kinase stimulation: M. Hitomi, et al.; J. Biol. Chem. 271, 9376 (1996) Abstract; Full Text
[2] p21Waf1 inhibits the activity of cyclin dependent kinase 2 by preventing its activating phosphorylation: M. Hitomi, et al.; Oncogene 17, 959 (1998) Abstract
[3] Down-regulation of cyclin D1 expression by prostaglandin A(2) is mediated by enhanced cyclin D1 mRNA turnover: S. Lin, et al.; Mol. Cell. Biol. 20, 7903 (2000) Abstract; Full Text
[4] Interactions of prostaglandin A2 with the glutathione-mediated biotransformation system: M.L. van Iersel, et al.; Biochem. Pharmacol. 57, 1383 (1999) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the methyl acetate under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-350-006 Revised 05-Apr-08
Genistein (synthetic)
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SYNONYMS 4',5,7-Trihydroxyisoflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-006-M010   10 mg 25.00 USD Add To Cart
ALX-350-006-M025   25 mg 50.00 USD Add To Cart
ALX-350-006-M050   50 mg 90.00 USD Add To Cart
ALX-350-006-M100   100 mg 150.00 USD Add To Cart
ALX-350-006-G001   1 g 480.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 446-72-0
MERCK INDEX: 14: 4391
RTECS: NR2392000
SOURCE/HOST: Synthetic.
PURITY: ≥99% (HPLC)
APPEARANCE: White to yellow crystalline powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Tyrosine protein kinase inhibitor. Inhibits phosphorylation of EGFR kinase. Inhibits tumor cell proliferation and induces tumor cell differentiation. Inhibits topoisomerase II activity in vivo. Produces cell cycle arrest and apoptosis. Direct inhibitor of insulin-induced glucose uptake in adipocytes (IC50=20µM).
Product Specific Literature References
Genistein, a specific inhibitor of tyrosine-specific protein kinases: T. Akiyama, et al.; J. Biol. Chem. 262, 5592 (1987) Abstract; Full Text
Erbstatin blocks platelet activating factor-induced protein-tyrosine phosphorylation, polyphosphoinositide hydrolysis, protein kinase C activation, serotonin secretion and aggregation of rabbit platelets: H. Salari, et al.; FEBS Lett. 263, 104 (1990) Abstract
Mechanisms of cancer chemoprevention by soy isoflavone genistein: F.H. Sarkar & Y. Li; Cancer Metastasis Rev. 21, 265 (2002) Abstract
Soy isoflavone phyto-pharmaceuticals in interleukin-6 affections. Multi-purpose nutraceuticals at the crossroad of hormone replacement, anti-cancer and anti-inflammatory therapy: N. Dijsselbloem, et al.; Biochem. Pharmacol. 68, 1171 (2004), Review Abstract
Genistein affects testosterone secretion by Leydig cells in roosters (Gallus gallus domesticus): M. Opalka, et al.; Reprod. Biol. 4, 185 (2004) Abstract
Genistein directly inhibits GLUT4-mediated glucose uptake in 3T3-L1 adipocytes: M. Bazuine, et al.; BBRC 325, 511 (2005) Abstract
Decreased circulating levels of tumor necrosis factor-alpha in postmenopausal women during consumption of soy-containing isoflavones: Y. Huang, et al.; J. Clin. Endocrinol. Metab. 90, 3956 (2005) Abstract
Phytoestrogens and lipoproteins in women: C.N. Bairey Merz, et al.; J. Clin. Endocrinol. Metab. 91, 2209 (2006) Abstract
Clinical review: a critical evaluation of the role of soy protein and isoflavone supplementation in the control of plasma cholesterol concentrations: A. Dewell, et al.; J. Clin. Endocrinol. Metab. 91, 772 (2006), Review Abstract
The role of genistein and synthetic derivatives of isoflavone in cancer prevention and therapy: F.H. Sarkar, et al.; Mini Rev. Med. Chem. 6, 401 (2006), Review Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • TNF-alpha & TNF Receptors Other Products • Cell Cycle Blockers & Inhibitors / Related Products • EGFR Kinase Inhibitors • Natural Products - Topoisomerase Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Natural Products - Antitumor Reagents • Active Substances from Fruit and Vegetables • Antitumor Agents (Apoptosis Inducers) • Natural Products for Cell Cycle Research • Natural Products for Angiogenesis Research • Natural Products - Apoptosis Inducers & Inhibitors • Isoflavones • Antitumor Agents (Anti-proliferative)
 
 
ALX-350-013 Revised 23-Oct-07
Olomoucine (high purity)
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SYNONYMS 6-Benzylamino-2-(2-hydroxyethylamino)-9-methylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-013-M005   5 mg 65.00 USD Add To Cart
ALX-350-013-M025   25 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C15H18N6O
MW: 298.4
CAS NUMBER: 101622-51-9
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent and very selective inhibitor of cdc2, CDK and other cyclin-related kinases by competing for the ATP-binding domain of the kinase. Inhibits CDK1/cyclin B (IC50=7µM), CDK2 (IC50=7µM) and CDK5/p35 (IC50=3µM). Also inhibits DNA synthesis in interleukin-2 stimulated T lymphocytes and triggers G1 arrest similar to that observed in interleukin-2 deprived cells. Can be used to synchronize cells in G1. Triggers apoptosis in target tumor cells in vitro and in vivo and in maturing cerebellar granule neurons.
Product Specific Literature References
Inhibition of cyclin-dependent kinases by purine analogues: J. Vesely, et al.; Eur. J. Biochem. 224, 771 (1994) Abstract
Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases: R.T. Abraham, et al.; Biol. Cell 83, 105 (1995) Abstract
Mitotic disassembly of the Golgi apparatus in vivo: T. Mistelli & G. Warren; J. Cell Sci. 108, 2715 (1995) Abstract
Chemical inhibitors of cyclin-dependent kinases: L. Meijer, et al.; Meth. Enzymol. 283, 113 (1997) Abstract
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
The cyclin-dependent kinase inhibit