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CDK & Cyclin Inhibitors
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ALX-270-386 Revised 24-Feb-05
Aloisine
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SYNONYMS RP106
7-n-Butyl-6-(4-methoxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-386-M001   1 mg 25.00 USD Add To Cart
Product Specification
FORMULA: C17H19N3O
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 (IC50=700nM), CDK5/p25 (IC50=1.5µM), and GSK-3 (IC50=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-270-385 Revised 17-Jul-07
Aloisine A
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SYNONYMS RP107
7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-385-M001   1 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C16H17N3O
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 (IC50=150nM), CDK2/cyclin A (IC50=120nM), CDK2/cyclin E (IC50=400nM), CDK5/p25
(IC50=200nM), CDK5/p35 (IC50=160nM) and GSK-3α (IC50=500nM). Also inhibits GSK-3β (IC50=650nM) and c-Jun N-terminal kinase (JNK) (IC50~3-10µM). Poor inhibitor of CK1, CK2, CDK4/cyclin D1, MAPKK, PKA, PKG, PKCs and c-raf (IC50≥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-270-275 Revised 11-Sep-08
Alsterpaullone
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SYNONYMS 9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5H)-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-275-M001   1 mg 60.00 USD Add To Cart
ALX-270-275-M005   5 mg 270.00 USD Add To Cart
Product Specification
FORMULA: C16H11N3O3
MW: 293.3
CAS NUMBER: 237430-03-4
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow to brown powder.
SOLUBILITY: Soluble in DMSO; insoluble in water or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
IDENTITY: Identity determined by IR, 1H-NMR and 13C-NMR.

Product Description
Potent inhibitor of CDK1/cyclin B (IC50=35nM). Potent and selective inhibitor of CDK2/cyclin A, CDK2/cyclin E (IC50=200nM), CDK5/p25 (IC50=40nM), CDK5/p35 (IC50=40nM) and GSK-3β . Induces apoptosis by activation of caspase-8 and caspase-9 followed by disruption of the mitochondrial potential.

Licensed from NCI.
Product Specific Literature References
ATP-site directed inhibitors of cyclin-dependent kinases: N. Gray, et al.; Curr. Med. Chem. 6, 859 (1999) Abstract
Fused azepinones with antitumor activity: C. Kunick; Curr. Pharm. Des. 5, 181 (1999), (Review) Abstract
Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity: C. Schultz, et al.; J. Med. Chem. 42, 2909 (1999) Abstract
Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases: D.W. Zaharevitz, et al.; Cancer Res. 59, 2566 (1999) Abstract
2-Substituted paullones: CDK1/cyclin B-inhibiting property and in vitro antiproliferative activity: C. Kunick, et al.; Bioorg. Med. Chem. Lett. 10, 567 (2000) Abstract
Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25: M. Leost, et al.; Eur. J. Biochem. 267, 5983 (2000) Abstract
Inhibition of CDKs as a therapeutic modality: E.A. Sausville, et al.; Ann. NY Acad. Sci. 910, 207 (2000) Abstract
A novel, extraneuronal role for cyclin-dependent protein kinase 5 (CDK5): modulation of cAMP-induced apoptosis in rat leukemia cells: T. Sandal, et al.; J. Biol. Chem. 277, 20783 (2002) Abstract; Full Text
Intracellular Targets of Paullones. Identification following affinity purification on immobilized inhibitor: M. Knockaert, et al.; J. Biol. Chem. 277, 25493 (2002) Abstract; Full Text
Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential: T. Lahusen, et al.; Mol Carcinog 36, 183 (2003) Abstract
The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003) Abstract
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products • GSK-3 Inhibitors
 
 
ALX-270-249 Revised 11-Sep-08
Aminopurvalanol A
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SYNONYMS (2R)-2-((6-((3-Amino-5-chlorophenyl)amino)-9-(1-methylethyl)-
9H-purin-2-yl)amino)-3-methyl-1-butanol
NG-97
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-249-M001   1 mg 45.00 USD Add To Cart
ALX-270-249-M005   5 mg 135.00 USD Add To Cart
Product Specification
FORMULA: C19H26N7OCl
MW: 403.9
CAS NUMBER: 220792-57-4
PURITY: ≥97% (1H-NMR)
APPEARANCE: White to brownish solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Packaged under inert gas. Protect from light.
HAZARD: IRRITANT.

Product Description
Cell permeable, reversible and competitive inhibitor of CDK1/cyclin B (IC50=33nM), CDK2/cyclin A (IC50=33nM), CDK2/cyclin E (IC50=28nM) and CDK5/p35 (IC50=20nM).
Product Specific Literature References
Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors: Y.T. Chang, et al.; Chem. Biol. 6, 361 (1999) Abstract
A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts: G.R. Rosania, et al.; PNAS 96, 4797 (1999) Abstract; Full Text
M-phase regulation of the recruitment of mRNAs onto polysomes using the CDK1/cyclin B inhibitor aminopurvalanol: M. Le Breton, et al.; BBRC 306, 880 (2003) Abstract
 
 
ALX-270-387 Revised 18-Jul-07
3-Amino-1H-pyrazolo[3,4-b]quinoxaline
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-387-M001   1 mg 40.00 USD Add To Cart
ALX-270-387-M005   5 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C9H7N5
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 (IC50=600nM), CDK5/p25 (IC50=400nM) and GSK-3β (IC50=1µM). Does not inhibit Cdc25 phosphatase activity (IC50>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-350-375 Revised 22-Jul-08 New product
Arcyriaflavin A
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-375-M001   1 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C20H11N3O2
MW: 325.3
CAS NUMBER: 118458-54-1
SOURCE/HOST: Synthetic. Originally isolated from the marine ascidian Eudistoma sp.
PURITY: ≥95% (HPLC)
APPEARANCE: Orange to red solid.
SOLUBILITY: Soluble in DMSO (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Protect from light. Packaged under inert gas.

Product Description
Potent inhibitor of CDK4 / cyclin D1 (IC50 = 59nM). Inhibits human cytomegalovirus (HCMV) replication in cell culture (IC50 = 200nM).
Product Specific Literature References
Staurosporine aglycone (K252-c) and arcyriaflavin A from the marine ascidian, Eudistoma sp: P.A. Horton, et al.; Experientia 50, 843 (1994) Abstract
Indolocarbazoles: potent, selective inhibitors of human cytomegalovirus replication: M.J. Slater, et al.; Bioorg. Med. Chem. 7, 1067 (1999) Abstract
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors: C. Sanchez-Martinez, et al.; Bioorg. Med. Chem. Lett. 13, 3835 (2003) Abstract
Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors: G. Zhu, et al.; Bioorg. Med. Chem. Lett. 13, 1231 (2003) Abstract
Two indolocarbazole alkaloids with apoptosis activity from a marine-derived actinomycete Z(2)039-2: R. Liu, et al.; Arch. Pharm. Res. 30, 270 (2007) Abstract
Further Categories Containing This Product:
Natural Products for Cell Cycle Research • Antiviral Agents Other Products • Marine Natural Products
 
 
ALX-350-273 Revised 03-Apr-08
3-ATA
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SYNONYMS 3-Amino-9-thio(10H)-acridone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-273-M001   1 mg 60.00 USD Add To Cart
ALX-350-273-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C13H10N2S
MW: 226.3
CAS NUMBER: 12982-10-85
PURITY: ≥95%
APPEARANCE: White solid powder.
SOLUBILITY: Soluble in DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Specific CDK4 inhibitor (IC50=3.1µM) inducing growth inhibition of p16-altered tumors.
Product Specific Literature References
The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4: A. Kubo, et al.; Clin. Cancer Res. 5, 4279 (1999) Abstract
3-Amino thioacridone, a selective cyclin-dependent kinase 4 inhibitor, attenuates kainic acid-induced apoptosis in neurons: E. Verdaguer, et al.; Neuroscience 120, 599 (2003) Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors
 
 
ALX-270-388 Revised 18-Jul-07
Benfluorene
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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
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ALX-270-388-M001   1 mg 70.00 USD Add To Cart
ALX-270-388-M005   5 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C20H15NO4
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 (IC50=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 (IC50>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-350-298 Revised 03-Apr-08
Betulinic acid (~95%)
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SYNONYMS 3β-Hydroxy-20(29)-lupaene-28-oic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-298-M100   100 mg 55.00 USD Add To Cart
ALX-350-298-M500   500 mg 180.00 USD Add To Cart
ALX-350-298-G001   1 g 290.00 USD Add To Cart
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Product Specification
FORMULA: C30H48O3
MW: 456.7
CAS NUMBER: 472-15-1
SOURCE/HOST: Isolated from Platanus acerifolia (plane tree) bark.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator.
Product Specific Literature References
Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids: T. Fujioka, et al.; J. Nat. Prod. 57, 243 (1994) Abstract
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis: E. Pisha, et al.; Nat. Med. 1, 1046 (1995) Abstract
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents: Y. Kashiwada, et al.; J. Med. Chem. 39, 1016 (1996) Abstract
Betulinic acid triggers CD95 (APO-1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors: S. Fulda, et al.; Cancer Res. 57, 4956 (1997) Abstract
Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives: F. Hashimoto, et al.; Bioorg. Med. Chem. 5, 2133 (1997) Abstract
Betulinic acid induces apoptosis in human neuroblastoma cell lines: M.L. Schmidt, et al.; Eur. J. Cancer 33, 2007 (1997) Abstract
Induction of p53 without increase in p21WAF1 in betulinic acid-mediated cell death is preferential for human metastatic melanoma: M. Rieber & M. Strasberg Rieber; DNA Cell Biol. 17, 399 (1998) Abstract
Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid: S. Fulda, et al.; J. Biol. Chem. 273, 33942 (1998) Abstract; Full Text
Betulinic acid inhibits aminopeptidase N activity: M.F. Melzig & H. Bormann; Planta Med. 64, 655 (1998) Abstract
Correspondence re: S. Fulda et al., Betulinic acid triggers CD95 (Apo1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors. Cancer Res., 57: 4956, 1997: M. Rieber & M. Strasberg Rieber; Cancer. Res. 58, 5876 (1998) Abstract
Betulinic acid: a new cytotoxic agent against malignant brain-tumor cells: S. Fulda, et al.; Int. J. Cancer 82, 435 (1999) Abstract
Betulinic acid-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing: W. Wick, et al.; J Pharmacol. Exp. Ther. 289, 1306 (1999) Abstract; Full Text
Effects of betulinic acid alone and in combination with irradiation in human melanoma cells: E. Selzer, et al.; J. Invest. Dermatol. 114, 935 (2000) Abstract
Betulinic acid suppresses carcinogen-induced NF-kappa B activation through inhibition of I kappa B alpha kinase and p65 phosphorylation: abrogation of cyclooxygenase-2 and matrix metalloprotease-9: Y. Takada & B.B. Aggarwal; J. Immunol. 171, 3278 (2003) Abstract
Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection: R.H. Cichewicz & S.A. Kouzi; Med. Res. Rev. 24, 90 (2004), Review Abstract
Betulinic acid-induced apoptosis in leukemia cells: H. Ehrhardt, et al.; Leukemia 18, 1406 (2004) Abstract
Betulinic acid and its derivatives: a review on their biological properties: P. Yogeeswari & D. Sriram; Curr. Med. Chem. 12, 657 (2005), Review Abstract
Betulinic acid decreases expression of bcl-2 and cyclin D1, inhibits proliferation, migration and induces apoptosis in cancer cells: W. Rzeski, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 374, 11 (2006) Abstract
Activation and inhibition of the proteasome by betulinic acid and its derivatives: L. Huang, et al.; FEBS Lett. 581, 4955 (2007) Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors • NF-kB Pathway Inhibitors • Other Natural Products - DNA Regulation / Transcription • Natural Products - NF-kB Pathway Inhibitors • MPTP [Mitochondrial Transition Pore] / Related Products • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Anti-inflammatory Agents • Natural Products - Antiviral / anti-HIV Agents • Ubiquitin & Proteasome Other Products • Antitumor Agents (Apoptosis Inducers) • HIV / AIDS / 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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