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Cyclin-dependent Kinases [CDKs] & Cyclins / Related Products
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ALX-380-102 Revised 03-Apr-08
Borrelidin
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SYNONYMS 2-(7-Cyano-8,16-dihydroxy-9,11,13,15-tetramethyl-18-oxooxacyclooctadeca-4,6-dien-2-yl)cyclopentanecarboxylic acid
Treponemycin
U 78548
C2989
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-102-MC05   0.5 mg 160.00 USD Add To Cart
ALX-380-102-M001   1 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C28H43NO6
MW: 489.7
CAS NUMBER: 7184-60-3
RTECS: ED8750000
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: IRRITANT.

Product Description
Antibiotic. Inhibitor of bacterial and eukaryal threonyl-tRNA synthetase (ThrRS). Inhibitor of cyclin-dependent kinase (CDK). Shows angiogenesis inhibiting and antiviral activity.
Product Specific Literature References
Isolation of a cDNA clone for human threonyl-tRNA synthetase: amplification of the structural gene in borrelidin-resistant cell lines: K.J. Kontis and S.M. Arfin; Mol. Cell. Biol. 9, 1832 (1989) Abstract
Genetic analysis of mutations causing borrelidin resistance by overproduction of threonyl-transfer ribonucleic acid synthetase: J. Frohler, et al.; J. Bacteriol. 143, 1135 (1980) Abstract; Full Text
Increased levels of threonyl-tRNA synthetase in a borrelidin-resistant Chinese hamster ovary cell line: J.S. Gantt, et al.; PNAS 78, 5367 (1981) Abstract; Full Text
Chinese hamster ovary cells resistant to borrelidin overproduce threonyl-tRNA synthetase: S.C. Gerken and S.M. Arfin; J. Biol. Chem. 259, 9202 (1984) Abstract; Full Text
Borrelidin inhibits a cyclin-dependent kinase (CDK), Cdc28/Cln2, of Saccharomyces cerevisiae: E. Tsuchiya, et al.; J. Antibiot. 54, 84 (2001) Abstract
Borrelidin induces the transcription of amino acid biosynthetic enzymes via a GCN4-dependent pathway: E.L. Eastwood and S.E. Schaus; Bioorg. Med. Chem. Lett. 13, 2235 (2003) Abstract
Isolation of vivomycin and borrelidin, two antibiotics with anti-viral activity, from a species of Streptomyces (C2989): M. Lumb, et al.; Nature 206, 263 (1965) Abstract
A unique hydrophobic cluster near the active site contributes to differences in borrelidin inhibition among threonyl-tRNA synthetases: B. Ruan, et al.; J. Biol. Chem. 280, 571 (2005) Abstract; Full Text
Further Categories Containing This Product:
CDK & Cyclin Inhibitors • tRNA / Related Products • Antibiotics - Antiviral / Anti-HIV • Antibiotics for Angiogenesis Research
 
 
ALX-380-206 Revised 19-Aug-08
UCN-02
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Staurosporine / Related Products
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ALX-380-206-MC25   0.25 mg 85.00 USD Add To Cart
ALX-380-206-M001   1 mg 265.00 USD Add To Cart
Product Specification
FORMULA: C28H26N4O4
MW: 482.5
CAS NUMBER: 121569-61-7
RTECS: KC6600000
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5345.
PURITY: ≥98% (HPLC)
APPEARANCE: White to pale yellow solid.
SOLUBILITY: Soluble in ethyl acetate, 100% ethanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of protein kinase C (PKC) and protein kinase A (PKA). Although less selective than its isomer UCN-01 (Prod. No. ALX-380-222), UCN-02 exhibits comparable activity and probably acts by similar mechanisms.
Product Specific Literature References
[1] UCN-01 and UCN-02, new selective inhibitors of protein kinase C. II. Purification, physico-chemical properties, structural determination and biological activities: I. Takahashi, et al.; J. Antibiot. (Tokyo) 42, 571 (1989) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Note: Some interconversion of UCN-02 to UCN-01 may occur under acidic HPLC conditions (see [1]).
Further Categories Containing This Product:
Antitumor Antibiotics • CDK & Cyclin Inhibitors • PKC Inhibitors • Antibiotics for Cell Cycle Research • Antibiotics - Protein Kinase Inhibitors • Alkaloids • Antibiotics - Apoptosis Inducers & Inhibitors • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-380-222 Revised 19-Aug-08
UCN-01
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SYNONYMS 7-Hydroxystaurosporine
Staurosporine, 7-Hydroxy-
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Staurosporine / Related Products
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ALX-380-222-MC25   0.25 mg 85.00 USD Add To Cart
ALX-380-222-M001   1 mg 265.00 USD Add To Cart
Product Specification
FORMULA: C28H26N4O4
MW: 482.5
CAS NUMBER: 112953-11-4
RTECS: KC6600010
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5345.
PURITY: ≥98% (HPLC)
APPEARANCE: Light tan to light yellow solid.
SOLUBILITY: Soluble in methanol, 100% ethanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description

Inhibitor of protein kinase C (PKC) and cyclin-dependent kinases (CDKs) resulting in accumulation of cells in the G1 phase and induction of apoptosis. Enhances the cytotoxicity of other anticancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by these agents.
Product Specific Literature References
[1] UCN-01, a selective inhibitor of protein kinase C from Streptomyces: I. Takahashi, et al.; J. Antibiot. (Tokyo) 40, 1782 (1987) Abstract
[2] UCN-01 and UCN-02, new selective inhibitors of protein kinase C. II. Purification, physico-chemical properties, structural determination and biological activities: I. Takahashi, et al.; J. Antibiot. (Tokyo) 42, 571 (1989) Abstract
[3] UCN-01, 7-hydroxyl-staurosporine, inhibits kinase activity of cyclin-dependent kinases and reduces the phosphorylation of the retinoblastoma susceptibility gene product in A549 human lung cancer cell line: K. Kawakami, et al.; BBRC 219, 778 (1996) Abstract
[4] UCN-01 (7-hydroxystaurosporine) and other indolocarbazole compounds: a new generation of anti-cancer agents for the new century?: S. Akinaga, et al.; Anticancer Drug Des. 15, 43 (2000) Abstract
[5] UCN-01-induced cell cycle arrest requires the transcriptional induction of p21(waf1/cip1) by activation of mitogen-activated protein/extracellular signal-regulated kinase kinase/extracellular signal-regulated kinase pathway: M.M. Facchinetti, et al.; Cancer Res. 64, 3629 (2004) Abstract; Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION Note: Some interconversion of UCN-01 to UCN-02 may occur under acidic HPLC conditions (see [2]).
Further Categories Containing This Product:
Antitumor Antibiotics • CDK & Cyclin Inhibitors • PKC Inhibitors • Antibiotics - Protein Kinase Inhibitors • Antibiotics for Cell Cycle Research • Alkaloids • Antibiotics - Apoptosis Inducers & Inhibitors • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-430-161 Revised 15-Sep-08 New product
Flavopiridol
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SYNONYMS Alvocidib
(-)-2-(2-Chlorophenyl)-5,7-dihydroxy-8-[(3R,4S)-3-hydroxy-1-methyl-4-piperidinyl]-4H-1-benzopyran-4-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-161-M005   5 mg 60.00 USD Add To Cart
ALX-430-161-M025   25 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C21H20ClNO5
MW: 401.8
CAS NUMBER: 146426-40-6
MERCK INDEX: 14: 4094
SOURCE/HOST: Synthetic.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in chloroform; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: HARMFUL.
IDENTITY: Identity determined by 1H-NMR.

Product Description

Potent inhibitor of cyclin-dependent kinases  (CDKs). Induces apoptosis in certain tumor cells. Interacts with multidrug resistance protein 1 (MRP1).
Product Specific Literature References
Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase: W.F. Jr. De Azevedo, et al.; PNAS 93, 2735 (1996) Abstract; Full Text
Flavopiridol induces G1 arrest with inhibition of cyclin-dependent kinase (CDK) 2 and CDK4 in human breast carcinoma cells: B.A. Carlson, et al.; Cancer Res. 56, 2973 (1996) Abstract; Full Text
Flavopiridol: a cytotoxic flavone that induces cell death in noncycling A549 human lung carcinoma cells: K.C. Bible & S.H. Kaufmann; Cancer Res. 56, 4856 (1996) Abstract; Full Text
Flavopiridol (L86-8275): selective antitumor activity in vitro and activity in vivo for prostate carcinoma cells: M. Drees, et al.; Clin. Cancer Res. 3, 273 (1997) Abstract; Full Text
The novel cyclin-dependent kinase inhibitor flavopiridol downregulates Bcl-2 and induces growth arrest and apoptosis in chronic B-cell leukemia lines: A. König, et al.; Blood 90, 4307 (1997) Abstract; Full Text
Flavopiridol induces apoptosis of normal lymphoid cells, causes immunosuppression, and has potent antitumor activity In vivo against human leukemia and lymphoma xenografts: F. Arguello, et al.; Blood 91, 2482 (1998) Abstract; Full Text
Cell cycle-independent induction of apoptosis by the anti-tumor drug Flavopiridol in endothelial cells: S. Brüsselbach, et al.; Int. J. Cancer 77, 146 (1998) Abstract
Flavopiridol induces apoptosis in chronic lymphocytic leukemia cells via activation of caspase-3 without evidence of bcl-2 modulation or dependence on functional p53: J.C. Byrd, et al.; Blood 92, 3804 (1998) Abstract; Full Text
Identification of cytosolic aldehyde dehydrogenase 1 from non-small cell lung carcinomas as a flavopiridol-binding protein: J.B. Schnier, et al.; FEBS Lett. 454, 100 (1999) Abstract
Potent interaction of flavopiridol with MRP1: J.H. Hooijberg, et al.; Br. J. Cancer 81, 269 (1999) Abstract
Flavopiridol: the first cyclin-dependent kinase inhibitor in human clinical trials: A.M. Senderowicz; Invest. New Drugs 17, 313 (1999), (Review) Abstract
Protein kinase inhibitors flavopiridol and 7-hydroxy-staurosporine down-regulate antiapoptosis proteins in B-cell chronic lymphocytic leukemia: S. Kitada, et al.; Blood 96, 393 (2000) Abstract; Full Text
Flavopiridol, a cyclin-dependent kinase inhibitor, enhances radiosensitivity of ovarian carcinoma cells: U. Raju, et al.; Cancer Res. 63, 3263 (2003) Abstract; Full Text
Potential use of pharmacological cyclin-dependent kinase inhibitors as anti-HIV therapeutics: A. Pumrery, et al.; Curr. Pharm. Des. 12, 1949 (2006) Abstract
Flavopiridol synergizes TRAIL cytotoxicity by downregulation of FLIPL: T.E. Fandy, et al.; Cancer Chemother. Pharmacol. 60, 313 (2007) Abstract
Successful treatment of animal models of rheumatoid arthritis with small-molecule cyclin-dependent kinase inhibitors: C. Sekine, et al.; J. Immunol. 180, 1954 (2008) Abstract
Further Categories Containing This Product:
Flavones • Antitumor Agents (Apoptosis Inducers) • MDR Other Products
 
 
ALX-480-050 Revised 17-Jul-07
6-Dimethylaminopurine
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SYNONYMS N6,N6-Dimethyladenine
6-DMAP
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-480-050-M100   100 mg 15.00 USD Add To Cart
Product Specification
FORMULA: C7H9N5
MW: 163.2
CAS NUMBER: 938-55-6
PURITY: ≥97%
APPEARANCE: Crystalline.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Non-selective inhibitor of cdc2 and other kinases.
Product Specific Literature References
Inhibition of cyclin-dependent kinases by purine analogues: J. Vesley, et al.; Eur. J. Biochem. 224, 771 (1994)
 
 
ALX-380-116 Revised 07-Apr-08
Hypothemycin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-116-C250   250 µg 140.00 USD Add To Cart
ALX-380-116-M001   1 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C19H22O8
MW: 378.4
CAS NUMBER: 76958-67-3
SOURCE/HOST: Isolated from Phoma sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or acetone; insoluble in methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Exhibits antifungal and cytotoxic activity against some tumor cell lines partly attributed to inhibition of Ras-inducible genes. Inhibits proliferation of mouse and human T cells and modulates production of cytokines during T cell activation. Facilitates the ubiquitinylation process of cyclin D1. Has been identified as a potent and selective inhibitor of threonine/tyrosine-specific kinase, MEK, and other protein kinases that contain a conserved cysteine residue in the ATP-binding site in both in vitro and in vivo studies.
Product Specific Literature References
Metabolites of pyrenomycetes XIII: Structure of (+) hypothemycin, an antibiotic macrolide from hypomyces trichothecoides: M.S.R. Nair & S.T. Carey; Tetrahedron Lett. 21, 2011 (1980)
Metabolites of pyrenomycetes. XIV: Structure and partial stereochemistry of the antibiotic macrolides hypothemycin and dihydrohypothemycin: M.S.R. Nair, et al.; Tetrahedron 37, 2445 (1981)
Revised structure and stereochemistry of hypothemycin: T. Agatsuma et al.; Chem. Pharm. Bull. 41, 373 (1993)
Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor: H. Tanaka, et al.; Jpn. J. Cancer Res. 90, 1139 (1999) Abstract
Hypothemycin inhibits the proliferative response and modulates the production of cytokines during T cell activation: R. Camacho, et al.; Immunopharmacology 44, 255 (1999) Abstract
Suppression of oncogenic transformation by hypothemycin associated with accelerated cyclin D1 degradation through ubiquitin-proteasome pathway: H. Sonoda, et al.; Life Sci. 65, 381 (1999) Abstract
Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK: A. Zhao, et al.; J. Antibiot. 52, 1086 (1999) Abstract
Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides: A. Schirmer, et al.; PNAS 103, 4234 (2006) Abstract; Full Text
Chemistry and biology of resorcylic acid lactones: N. Winssinger, et al.; Chem. Commun. (Camb). 1, 22 (2007), (Review) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors • Tyrosine Kinase Inhibitors • Antibiotics - Protein Kinase Inhibitors • Antibiotics - Proteasome / Ubiquitin Modulators • Antitumor Antibiotics • Ubiquitination Other Products • CDKs & Cyclins Other Products • Ras Signalling Pathway Other Products • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-153-012 Revised 04-Mar-05
Cyclin-dependent Kinase 2 Inhibitor
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SYNONYMS CDK2/Cyclin Inhibitor
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-153-012-M001   1 mg 120.00 USD Add To Cart
ALX-153-012-M005   5 mg 480.00 USD Add To Cart
Product Specification
SEQUENCE: H-Tyr-Ser-Phe-Val-His-His-Gly-Phe-Phe-Asn-Phe-Arg-Val-Ser-Trp-Arg-Glu-Met-Leu-Ala-OH
FORMULA: C121H164N32O27S
MW: 2530.9
PEPTIDE CONTENT: 75-95%
PURITY: ≥97%
APPEARANCE: White to off-white lyophilized solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry.
Product Description
Inhibitor of cyclin-dependent kinase 2 (CDK2).
Product Specific Literature References
Genetic selection of peptide aptamers that recognize and inhibit cyclin- dependent kinase 2: P. Colas, et al.; Nature 380, 548 (1996) Abstract
Further Categories Containing This Product:
Peptides
 
 
ALX-153-041 Revised 04-Mar-05
Cyclin-dependent Kinase 2 Inhibitory Peptide I
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SYNONYMS CDK2/Cyclin Inhibitory Peptide I
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-153-041-C500   500 µg 145.00 USD Add To Cart
Product Specification
SEQUENCE: H-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Gly-Pro-Val-Lys-Arg-Arg-Leu-Phe-Gly-OH
FORMULA: C111H196N48O23
MW: 2571.1
PURITY: ≥98% (HPLC)
APPEARANCE: Solid.
FORMULATION: Lyophilized. Counter Ion: Trifluoroacetate salt.
SOLUBILITY: Soluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Following reconstitution, aliquot and freeze (-20°C). Product is stable for 2 years as supplied. Stock solutions are stable for 3 months at -20°C.
HANDLING: Hygroscopic.
Product Description
Cell permeable inhibitor of CDK2/cyclin complexes. Blocks phosphorylation of substrates by CDK2/cyclin A and CDK/cyclin E complexes. Preferentially induces apoptosis only in transformed cells and not in non-transformed cells.

Chimeric peptide consisting of the N-terminal sequence of the HIV-TAT protein (directing uptake across the cell membrane) and the consensus sequence PVKRRLFG that serves as the docking site for CDK2/cyclin complexes.
Product Specific Literature References
Selective killing of transformed cells by cyclin/cyclin-dependent kinase 2 antagonists: Y.N. Chen, et al.; PNAS 96, 4325 (1999) Abstract; Full Text
Further Categories Containing This Product:
Peptides • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-153-042 Revised 04-Mar-05
Cyclin-dependent Kinase 2 Inhibitory Peptide II
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SYNONYMS CDK2/Cyclin Inhibitory Peptide II
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-153-042-C500   500 µg 145.00 USD Add To Cart
Product Specification
SEQUENCE: H-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Gly-Pro-Val-Lys-Arg-Arg-Leu-Asp-Leu-OH
FORMULA: C110H200N48O25
MW: 2595.1
PURITY: ≥98%
APPEARANCE: Lyophilized solid.
SOLUBILITY: Soluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Very hygroscopic.
Product Description
Cell permeable inhibitor of CDK2/cyclin complexes. Blocks phosphorylation of substrates by CDK2/cyclin A and CDK/cyclin E complexes. Preferentially induces apoptosis only in transformed cells and not in non-transformed cells.
Product Specific Literature References
Selective killing of transformed cells by cyclin/cyclin-dependent kinase 2 antagonists: Y.N. Chen, et al.; PNAS 96, 4325 (1999) Abstract; Full Text
Further Categories Containing This Product:
Peptides • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-165-018 Revised