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Cell Cycle Blockers & Inhibitors / Related Products
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ALX-105-011 Revised 18-Sep-06
S-Trityl-L-cysteine
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SYNONYMS NSC 83265
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY Cell Cycle Blockers & Inhibitors / Related Products
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ALX-105-011-M100   100 mg 20.00 USD Add To Cart
ALX-105-011-M500   500 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C22H21NO2S
MW: 363.5
CAS NUMBER: 2799-07-7
RTECS: AY7710000
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or acetic acid
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Potent, cell permeable cysteine thioether displaying anti-mitotic and anti-tumor properties. Inhibits mitosis by blocking basal and microtubule-activated ATPase activities of the mitotic kinesin Eg5 (IC50=1µM and 140nm). Induces mitotic arrest in HeLa cells (IC50=700nM) and inhibits the growth of NCI tumor cell line panel (GI50=1.31µM).
Product Specific Literature References
In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities: S. DeBonis, et al.; Mol. Cancer Ther. 3, 1079 (2004) Abstract; Full Text
S-trityl-l-cysteine is a reversible, tight-binding inhibitor of the human kinesin eg5 that specifically blocks mitotic progression: D.A. Skoufias, et al.; J. Biol. Chem. 281, 17559 (2006) Abstract; Full Text
Further Categories Containing This Product:
Kinesin & Kinesin-like Proteins / Related Products • Antitumor Agents (Anti-proliferative)
 
 
ALX-270-143 Revised 20-Feb-08
Tyrphostin AG 494
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SYNONYMS Tyrphostin B48
N-Phenyl-3,4-dihydroxybenzylidenecyanoacetamide
α-Cyano-(3,4-dihydroxy)-N-phenylcinnamamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
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ALX-270-143-M005   5 mg 25.00 USD Add To Cart
ALX-270-143-M025   25 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C16H12N2O3
MW: 280.3
CAS NUMBER: 133550-35-3
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Blocks CDK2 activation and causes cells to arrest at late G1 and during S phase.
Product Specific Literature References
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases: A. Gazit, et al.; J. Med. Chem. 34, 1896 (1991) Abstract
Tyrphostin AG 494 blocks Cdk2 activation: N. Osherov & A. Levitzki; FEBS Lett. 410, 187 (1997) Abstract
Inhibition of Cdk2 activation by selected tyrphostins causes cell cycle arrest at late G1 and S phase: N. Kleinberger-Doron, et al.; Exp. Cell Res. 241, 340 (1998) Abstract
Further Categories Containing This Product:
EGFR Kinase Inhibitors • Tyrosine Kinase Inhibitors • CDK & Cyclin Inhibitors • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-270-168 Revised 18-May-06
Tyrphostin AG 490
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SYNONYMS Tyrphostin B42
N-Benzyl-3,4-dihydroxy-benzylidenecyanoacetamide
α-Cyano-(3,4-dihydroxy)-]N-benzylcinnamamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
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ALX-270-168-M005   5 mg 45.00 USD Add To Cart
ALX-270-168-M025   25 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C17H14N2O3
MW: 294.3
CAS NUMBER: 133550-30-8
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO and acetone; slightly soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selectively inhibits CDK2 activation leading to a potent cell cycle arrest at late G1 and S phase. Cell permeable inhibitor of JAK-2 tyrosine kinase. Does not significantly inhibit other kinases, such as Lck, Lyn, Btk, Syk or Src. Blocks IL-7 induced JAK kinase activity in T cells (JAK-1, JAK-3) and the consequent phosphorylation of PI-3 kinase. Valuable tool for studying the cellular role of JAK kinases in signal transduction.
Product Specific Literature References
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors: A. Gazit, et al.; J. Med. Chem. 32, 2344 (1989) Abstract
Tyrosine phosphorylation is an obligatory event in IL-2 secretion [published erratum appears in J Immunol 1991 May 1;146(9):3260]: A. Levitzki; Biochem. Pharmacol. 40, 913 (1990) Abstract
Activation of phosphatidylinositol-3 kinase by ligation of the interleukin-7 receptor is dependent on protein tyrosine kinase activity: H. Dadi, et al.; Blood 84, 1579 (1994) Abstract; Full Text
JAK3 protein tyrosine kinase mediates interleukin-7-induced activation of phosphatidylinositol-3’ kinase: N. Sharfe, et al.; Blood 86, 2077 (1995) Abstract; Full Text
Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor: N. Meydan, et al.; Nature 379, 645 (1996) Abstract
Tyrphostin AG-490 inhibits cytokine-mediated JAK3/STAT5a/b signal transduction and cellular proliferation of antigen-activated human T cells: R.A. Kirken, et al.; J. Leukoc. Biol. 65, 891 (1999) Abstract
JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response: L.H. Wang, et al.; J. Immunol. 162, 3897 (1999) Abstract
JAK2 tyrosine kinase inhibitor tyrphostin AG490 downregulates the mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STAT) pathways and induces apoptosis in myeloma cells: J. De Vos, et al.; Br. J. Haematol. 109, 823 (2000) Abstract
Further Categories Containing This Product:
Janus Kinases [JAKs] / Related Products • Tyrosine Kinase Inhibitors • CDK & Cyclin Inhibitors • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-270-271 Revised 17-Jul-07
Indirubin-3'-monoxime
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-271-M001   1 mg 50.00 USD Add To Cart
ALX-270-271-M005   5 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C16H11N3O2
MW: 277.3
PURITY: ≥98% (1H-NMR)
APPEARANCE: Dark red powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Selective and strong inhibitor of cyclin-dependent kinases (CDKs). Inhibits CDK1/cyclin B (IC50=180nM), CDK2/cyclin A (IC50~500nM), CDK2/cyclin E (IC50=250nM), CDK4/cyclin D1 (IC50=3.3µM) and CDK5/p35 (IC50=100nM).  Inhibits the proliferation of a large range of cells, mainly through arresting the cells in the G2/M phase of the cell cycle. Powerful inhibitor of GSK-3β (IC50~100nM) and tau phosphorylation in vitro and in vivo at Alzheimer’s disease-specific sites.
Product Specific Literature References
Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases: R. Hoessel, et al.; Nature Cell Biol. 1, 60 (1999) Abstract; Full Text
Anti-mitotic properties of indirubin-3'-monoxime, a CDK/GSK-3 inhibitor: induction of endoreplication following prophase arrest: E. Damiens, et al.; Oncogene 20, 3786 (2001) Abstract; Full Text
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
Inhibition of cyclin-dependent kinase 1 (CDK1) by indirubin derivatives in human tumour cells: D. Marko, et al.; Br. J. Cancer 84, 283 (2001) Abstract; Full Text
Related Products
Further Categories Containing This Product:
GSK-3 Inhibitors • Tau / Related Products • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-270-346 Revised 28-May-08
Ratjadone A (synthetic)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-270-346-C002   2 µg 150.00 USD Add To Cart
Product Specification
FORMULA: C28H40O5
MW: 456.6
CAS NUMBER: 163564-92-9
SOURCE/HOST: Synthetic.
PURITY: ≥95%
FORMULATION: Liquid. Solution in methanol.
SOLUBILITY: Soluble in methanol (20mg/ml) or aqueous buffers (<100µM).
SHIPPING: SHIPPED ON DRY ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Sensitive to acids and bases. Unstable in acidic buffer systems (pH<6). Stable in substance as oil and in solution in methanol at -20°C.
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Represents a new class of natural compounds, which inhibit proliferation in eukaryotes by blocking nuclear export. As potent as leptomycin B (Prod. No. ALX-380-100) and specific for G1/S checkpoint. Cytotoxic secondary metabolite (IC50=50pg/ml in mouse cell line L929) that arrests tumor cells in the G1 phase at remarkably low concentrations (50pg/ml in HeLa cell line KB3.1). Inhibits the binding between the nuclear export signal (NES) of proteins and the chromosome maintenance region protein (CRM1). Anticancer compound. Belongs to the family of orphan ligands which include polyketides like leptomycin B, callystatin A and other related compounds.
Product Specific Literature References
Antibiotics from gliding bacteria, LXIII. Ratjadone: a new antifungal metabolite from Sorangium cellulosum: D. Schummer, et al.; Liebigs Ann. 685 (1995)
Ratjadon: a new antifungal compound from Sorangium cellulosum (myxobacteria) production, physio-chemical and biological properties: J. Gerth, et al.; J. Antibiot. 48, 973 (1995) Abstract
The chemistry and biology of ratjadone: M. Kalesse, et al.; ChemBioChem. 9, 709 (2001) Abstract
The chemistry and biology of the leptomycin family: M. Kalesse & M. Christmann; Synthesis 8, 981 (2002) Abstract
Ratjadone and leptomycin B block CRM1-dependent nuclear export by identical mechanisms: T. Meissner, et al.; FEBS Lett. 576, 27 (2004)
Nuclear targeting of adenovirus type 2 requires CRM1-mediated nuclear export: S. Strunze, et al.; Mol. Biol. Cell 16, 2999 (2005) Abstract
Further Categories Containing This Product:
Nuclear Envelope & Nuclear Transport • Antitumor Antibiotics • Antitumor Agents (Anti-proliferative) • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-270-369 Revised 28-May-08
Ratjadone C (native)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-270-369-C005   5 µg 180.00 USD Add To Cart
Product Specification
FORMULA: C28H40O5
MW: 456.6
SOURCE/HOST: Isolated from Sorangium cellulosum.
PURITY: ≥95%
FORMULATION: Liquid. Solution in methanol (5µg in 1ml).
SOLUBILITY: Soluble in methanol (>50mg/ml). Sparingly soluble in aqueous buffers (up to 10µg/ml in PBS).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Acid and base sensitive. Unstable in acidic and alkaline buffer systems (pH <6 or >7). Stable in methanolic solution at -20°C.
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Cytotoxic secondary metabolite that inhibits cell growth of mammalian cell lines in the picomolar range (IC50=0.2ng/ml with L929 mouse cells) including multidrug resistant (MDR) HeLa cells (IC50=0.1ng/ml with KB-V1). Like leptomycin B (Prod. No. ALX-380-100), ratjadone C binds covalently to the nuclear export protein CRM1. It inhibits cargo protein binding to the leucine-rich nuclear export sequence and thereby blocks nuclear export.
Product Specific Literature References
Antibiotics from gliding bacteria, LXIII. Ratjadone: a new antifungal metabolite from Sorangium cellulosum: D. Schummer, et al.; Liebigs Ann. 685 (1995)
Ratjadon: a new antifungal compound from Sorangium cellulosum (myxobacteria) production, physico-chemical and biological properties: K. Gerth, et al.; J. Antibiot. (Tokyo) 48, 973 (1995) Abstract
The chemistry and biology of the leptomycin family: M. Kalesse & M. Christmann; Synthesis 8, 981 (2002) Abstract
Ratjadones inhibit nuclear export by blocking CRM1/exportin 1: M. Koster, et al.; Exp. Cell. Res. 286, 321 (2003) Abstract
Further Categories Containing This Product:
Nuclear Envelope & Nuclear Transport • Antitumor Agents (Anti-proliferative) • Antitumor Antibiotics • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-270-373 Revised 11-Aug-06
trans-HR22C16
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY Cell Cycle Blockers & Inhibitors / Related Products
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ALX-270-373-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C23H23N3O3
MW: 389.5
CAS NUMBER: 462630-41-7
PURITY: ≥95%
APPEARANCE: Yellow to ocher solid.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description

Cell permeable non-tubulin-interacting mitosis inhibitor. Blocks mitosis (IC50=800nM) by binding to the mitotic kinesin Eg5.
Product Specific Literature References
HR22C16: A Potent Small-Molecule Probe for the Dynamics of Cell Division: S. Hotha, et al.; Angew. Chem. Int. Ed. Engl. 42, 2379 (2003) Abstract
Further Categories Containing This Product:
Kinesin & Kinesin-like Proteins / 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-270-386 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-270-390 Revised 09-Jan-08
Bohemine
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SYNONYMS 6-Benzylamino-2-(3-hydroxypropylamino)-9-isopropylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-390-M001   1 mg 40.00 USD Add To Cart
ALX-270-390-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C18H24N6O
MW: 340.4
CAS NUMBER: 189232-42-6