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ALX-350-236 Revised 04-Sep-08
Homoharringtonine
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Immunomodulators
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ALX-350-236-M001   1 mg 45.00 USD Add To Cart
ALX-350-236-M005   5 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C29H39NO9
MW: 545.6
CAS NUMBER: 26833-87-4
RTECS: FK0260000
SOURCE/HOST: Isolated from Cephalotaxus hainanensis.
PURITY: ≥96%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: VERY TOXIC.

Product Description
Cephalotaxine alkaloid. Inhibits the formation of diphenylalanine and acetylphenylalanyl-puromycin in liver ribosomes. Has promising activity in hematologic malignancies. Lowers the levels of telomerase. Induces apoptosis.
Product Specific Literature References
Different effects of L-histidinol and homoharringtonine on 5- fluorouracil and bis-chloroethylnitrosourea activity in a murine model: R.C. Warrington & W.D. Fang; Anticancer Res. 11, 1879 (1991) Abstract
Selective inhibition of the polypeptide chain elongation in eukaryotic cells: R.M. Tujebajeva, et al.; Biochim. Biophys. Acta 1129, 177 (1992) Abstract
Homoharringtonine is safe and effective for patients with acute myelogenous leukemia: E. Feldman, et al.; Leukemia 6, 1185 (1992) Abstract
Homoharringtonine: history, current research, and future direction: H.M. Kantarjian, et al.; Cancer 92, 1591 (2001), Review Abstract
Homoharringtonine: a new treatment option for myeloid leukemia: C.Y. Luo, et al.; Hematology 9, 259 (2004), Review Abstract
Homoharringtonine-induced apoptosis of human leukemia HL-60 cells is associated with down-regulation of telomerase: W.Z. Xie, et al.; Am. J. Chin. Med. 34, 233 (2006) Abstract
 
 
ALX-350-250 Revised 22-Jul-08 New product
Butyrolactone I
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-250-C200   200 µg 135.00 USD Add To Cart
Product Specification
FORMULA: C24H24O7
MW: 424.5
CAS NUMBER: 87414-49-1
PURITY: ≥99% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: 25mg/ml soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Cell permeable and selective inhibitor of the cyclin-dependent kinases CDK1/cyclin B, CDK2 and CDK5. Inhibits cell cycle progression at the G1/S and G2/M transitions. Blocks Fas-induced apoptosis. Displays antitumor activity.
Product Specific Literature References
Butyrolactone I, a selective inhibitor of cdk2 and cdc2 kinase: M. Kitagawa, et al.; Oncogene 8, 2425 (1993) Abstract
Inhibition of cell cycle oscillation of DNA replication by a selective inhibitor of the cdc2 kinase family, butyrolactone I, in Xenopus egg extracts: A. Someya, et al.; BBRC 198, 536 (1994) Abstract
A cyclin-dependent kinase inhibitor, butyrolactone I, inhibits phosphorylation of RB protein and cell cycle progression: M. Kitagawa, et al.; Oncogene 9, 2549 (1994) Abstract
Evidence for cdk5 as a major activity phosphorylating tau protein in porcine brain extract: T. Hosoi, et al.; J. Biochem. 117, 741 (1995) Abstract
Transcriptional activation of the cdc2 gene is associated with Fas- induced apoptosis of human hematopoietic cells: Y. Furukawa, et al.; J. Biol. Chem. 271, 28469 (1996) Abstract; Full Text
Antitumor effects of butyrolactone I, a selective cdc2 kinase inhibitor, on human lung cancer cell lines: K. Nishio, et al.; Anticancer Res. 16, 3387 (1996) Abstract
An exogenous cdk inhibitor, butyrolactone-I, induces apoptosis with increased Bax/Bcl-2 ratio in p53-mutated pancreatic cancer cells: M. Wada, et al.; Anticancer Res. 18, 2559 (1998) Abstract
Effects of cyclin-dependent kinase inhibitors on transcription and ocular circadian rhythm of Aplysia: N. Sankrithi and A. Eskin; J. Neurochem. 72, 605 (1999) Abstract
Butyrolactone I induces cyclin B1 and causes G2/M arrest and skipping of mitosis in human prostate cell lines: M. Suzuki, et al.; Cancer Lett. 138, 121 (1999) Abstract
Butyrolactone I reversibly inhibits meiotic maturation of bovine oocytes, without influencing chromosome condensation activity: M. Kubelka, et al.; Biol. Reprod. 62, 292 (2000) Abstract; Full Text
Involvement of Cdk5/p25 in digoxin-triggered prostate cancer cell apoptosis: H. Lin, et al.; J. Biol. Chem. 279, 29302 (2004) Abstract; Full Text
Regulation of mitotic function of Chk1 through phosphorylation at novel sites by cyclin-dependent kinase 1 (Cdk1): T. Shiromizu, et al.; Genes Cells 11, 477 (2006) Abstract
 
 
ALX-350-251 Revised 23-Oct-07
(R)-Roscovitine
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SYNONYMS 6-Benzylamino-2-(R)-[(1-ethyl)-2-hydroxyethylamino]-9-isopropylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-251-M001   1 mg 30.00 USD Add To Cart
ALX-350-251-M005   5 mg 110.00 USD Add To Cart
ALX-350-251-M050   50 mg 450.00 USD Add To Cart
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Product Specification
FORMULA: C19H26N6O
MW: 354.5
CAS NUMBER: 186692-46-6
PURITY: ≥97%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in chloroform, DMSO or methanol; moderately soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent and selective inhibitor of CDKs. Selective for CDK1/cyclin B kinase (IC50=450nM) [2], CDK2 (IC50=700nM) [4] and CDK5/p35 (IC50=160nM) [4,5]. More potent than olomoucine (Prod. No. ALX-350-013). Inhibits M phase promoting factor (MPF) kinase activity. Has effects on calcium channel gating.
Product Specific Literature References
[1] Activation of cyclin-dependent kinases by Myc mediates induction of cyclin A, but not apoptosis: B. Rudolph, et al.; EMBO J. 15, 3065 (1996) Abstract
[2] Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine: W.F. De Azvedo, et al.; Eur. J. Biochem. 243, 518 (1997) Abstract
[3] 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
[4] Chemical inhibitors of cyclin-dependent kinases: L. Meijer and S.H. Kim; Meth. Enzymol. 283, 113 (1997) Abstract
[5] Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5: L. Meijer, et al.; Eur. J. Biochem. 243, 527 (1997) Abstract
[6] Direct in vivo inhibition of the nuclear cell cycle cascade in experimental mesangial proliferative glomerulonephritis with Roscovitine, a novel cyclin-dependent kinase antagonist: J.W. Pippin, et al.; J. Clin. Invest. 100, 2512 (1997) Abstract
[7] Early inhibition of DNA synthesis in the developing rat cerebral cortex by the purine analogues olomoucine and roscovitine: J.S. Yakisich, et al.; BBRC 243, 674 (1998) Abstract
[8] The cyclin-dependent kinase inhibitors olomoucine and roscovitine arrest human fibroblasts in G1 phase by specific inhibition of CDK2 kinase activity: F. Alessi, et al.; Exp. Cell Res. 245, 8 (1998) Abstract
[9] Effects of cyclin-dependent kinase inhibitors on transcription and ocular circadian rhythm of Aplysia: N. Sankrithi & A. Eskin; J. Neurochem. 72, 605 (1999) Abstract
[10] Transcription of herpes simplex virus immediate-early and early genes is inhibited by roscovitine, an inhibitor specific for cellular cyclin- dependent kinases: L.M. Schang, et al.; J. Virol. 73, 2161 (1999) Abstract
[11] Roscovitine and other purines as kinase inhibitors. From starfish oocytes to clinical trials: L. Meijer & E. Raymond; Acc. Chem. Res. 36, 417 (2003), (Review) Abstract
[12] The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003) Abstract
[13] Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 67, 1947 (2004) Abstract
[14] Roscovitine targets, protein kinases and pyridoxal kinase: S. Bach, et al.; J. Biol. Chem. 280, 31208 (2005) Abstract
[15] The effects of presynaptic calcium channel modulation by roscovitine on transmitter release at the adult frog neuromuscular junction: S. Cho & S.D. Meriney; Eur. J. Neurosci. 23, 3200 (2006) Abstract
[16] Roscovitine differentially affects CaV2 and Kv channels by binding to the open state: Z. Buraei, et al.; Neuropharmacology 52, 883 (2007) Abstract
Further Categories Containing This Product:
Ion Channels & Transporters Other Products
 
 
ALX-350-257 Revised 08-Oct-08
Vinblastine . sulfate
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SYNONYMS Vincaleukoblastine . sulfate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-257-M005   5 mg 45.00 USD Add To Cart
ALX-350-257-M025   25 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C46H58N4O9 . H2SO4
MW: 811.0 . 98.1
CAS NUMBER: 143-67-9
MERCK INDEX: 14: 9982
SOURCE/HOST: Semisynthetic from catharanthine or vindoline.
PURITY: ≥98%
APPEARANCE: White powder.
SOLUBILITY: Soluble in DMSO, methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Plant alkaloid that arrests the cell cycle in G2/M phase by blocking mitotic spindle formation. Depolymerizes microtubules and blocks binding of tubulin to microtubule proteins. Induces apoptosis. Triggers Raf-1 activation, phosphorylation of Bcl-2 family proteins and induction of p53 expression.
Product Specific Literature References
Microtubule antagonists activate programmed cell death (apoptosis) in cultured rat hepatocytes: K. Tsukidate, et al.; Am. J. Pathol. 143, 918 (1993) Abstract
Resistance of Ehrlich tumor cells to apoptosis can be due to accumulation of heat shock proteins: V.L. Gabai, et al.; FEBS Lett. 375, 21 (1995) Abstract
The interaction of taxol and vinblastine with radiation induction of p53 and p21 WAF1/CIP1: R.B. Tishler & D.M. Lamppu; Br. J. Cancer. Suppl. 27, S82 (1996) Abstract
Raf-1/bcl-2 phosphorylation: a step from microtubule damage to cell death: M.V. Blagosklonny, et al.; Cancer Res. 57, 130 (1997) Abstract
Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle: A. Jordan, et al.; Med. Res. Rev. 18, 259 (1998) Abstract
The C terminus of beta-tubulin regulates vinblastine-induced tubulin polymerization: S.S. Rai & J. Wolff; PNAS 95, 4253 (1998) Abstract; Full Text
Caspase-3 activation is not responsible for vinblastine-induced Bcl-2 phosphorylation and G2/M arrest in human small cell lung carcinoma Ms-1 cells: E. Tashiro, et al.; Jpn. J. Cancer Res. 89, 940 (1998) Abstract
Use of drugs to study role of microtubule assembly dynamics in living cells: A. Jordan & L. Wilson; Meth. Enzymol. 298, 252 (1998) Abstract
Vinblastine-induced phosphorylation of Bcl-2 and Bcl-XL is mediated by JNK and occurs in parallel with inactivation of the Raf-1/MEK/ERK cascade: M. Fan, et al.; J. Biol. Chem. 275, 29980 (2000) Abstract; Full Text
Vinblastine, a chemotherapeutic drug, inhibits palmitoylation of tubulin in human leukemic lymphocytes: J.M. Caron & M. Herwood; Chemotherapy 53, 51 (2007) Abstract
 
 
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-350-289 Revised 05-Apr-08
10Z-Hymenialdisine
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SYNONYMS 4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-289-C500   500 µg 190.00 USD Add To Cart
Product Specification
FORMULA: C11H10BrN5O2
MW: 324.1
CAS NUMBER: 82005-12-7
SOURCE/HOST: Isolated from sponge Axinella damicornis (Stylissa damicornis).
PURITY: ≥97%
APPEARANCE: Yellow needles.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Originally isolated from the sponges Axinella verrucosa and Acantella aurantiaca. Potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC50=6nM). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-β (GSK-3β) and CDK5/p35 in Alzheimer’s disease. Inhibitor of DNA damage checkpoint at G2 phase (IC50=6µM), cyclin-dependent kinases CDK1/cyclin B (IC50=22nM), CDK2/cyclin A (IC50=70nM), CDK2/cyclin E (IC50=40nM), CDK4/cyclin D1 (IC50=600nM), CDK5/p25 (IC50=28nM), GSK-3β (IC50=10nM), and casein kinase 1 (CK1) (IC50=35nM). Inhibitor of NF-κB activation and of various pro-inflammatory cytokines such as IL-1, IL-2 (IC50=2.4µM), IL-6, IL-8, TNF-α (IC50=1.4µM) and nitric oxide (NO) (IC50=0.8µM) in a variety of cell lines.
Product Specific Literature References
Isolation and x-ray crystal structure of a novel bromo-compound from two marine sponges: G. Cimino, et al.; Tetrahedron Lett. 23, 767 (1982)
Bioactive alkaloids from the tropical marine sponge Axinella carteri: A. Supriyono, et al.; Z. Naturforsch. [C] 50, 669 (1995) Abstract
The natural product hymenialdisine inhibits interleukin-8 production in U937 cells by inhibition of nuclear factor-kappaB: J.J. Breton & M.C. Chabot-Fletcher; J. Pharmacol. Exp. Ther. 282, 459 (1997) Abstract; Full Text
Inhibition of NFkappaB-mediated interleukin-1beta-stimulated prostaglandin E2 formation by the marine natural product hymenialdisine: A. Roshak, et al.; J. Pharmacol. Exp. Ther. 283, 955 (1997) Abstract; Full Text
Inhibition of interleukin-1-induced proteoglycan degradation and nitric oxide production in bovine articular cartilage/chondrocyte cultures by the natural product, hymenialdisine: A.M. Badger, et al.; J. Pharmacol. Exp. Ther. 290, 587 (1999) Abstract; Full Text
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent: L. Meijer, et al.; Chem. Biol. 7, 51 (2000) Abstract
Inhibition of the G2 DNA damage checkpoint and of protein kinases Chk1 and Chk2 by the marine sponge alkaloid debromohymenialdisine: D. Curman, et al.; J. Biol. Chem. 276, 17914 (2001) Abstract; Full Text
An investigation of cell proliferation and soluble mediators induced by interleukin 1beta in human synovial fibroblasts: comparative response in osteoarthritis and rheumatoid arthritis: H. Inoue, et al.; Inflamm. Res. 50, 65 (2001) Abstract
Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1): D. Tasdemir, et al.; J. Med. Chem. 45, 529 (2002) Abstract
Inhibition of cytokine production by hymenialdisine derivatives: V. Sharma, et al.; J. Med. Chem. 47, 3700 (2004) Abstract
 
 
ALX-350-290 Revised 19-Oct-07
Debromohymenialdisine
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SYNONYMS DBH
4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-290-C100   100 µg 90.00 USD Add To Cart
Product Specification
FORMULA: C11H11N5O2
MW: 245.2
CAS NUMBER: 125118-55-0
SOURCE/HOST: Isolated from sponge Stylotella aurantium.
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Inhibitor of G2 DNA damage checkpoint (IC50=8µM) and check point kinases 1 (Chk1) (IC50=3µM) and 2 (Chk2) (IC50=3.5µM) [1,3]. Unlike other checkpoint inhibitors DBH does not inhibit ataxia-telangiectasia mutated (ATM) or ATM-Rad3-related protein. Also inhibits MAP kinase kinase 1 (MEK-1) (IC50=881nM) but is not as potent as 10Z-hymenialdisine (Prod. No. ALX-350-289) (IC50=6nM) [2].
Product Specific Literature References
[1] Inhibition of the G2 DNA damage checkpoint and of protein kinases Chk1 and Chk2 by the marine sponge alkaloid debromohymenialdisine: D. Curman, et al.; J. Biol. Chem. 276, 17914 (2001) Abstract; Full Text
[2] Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1): D. Tasdemir, et al.; J. Med. Chem. 45, 529 (2002) Abstract
[3] G2 checkpoint abrogators as anticancer drugs: T. Kawabe; Mol. Cancer Ther. 3, 513 (2004) Abstract
 
 
ALX-350-291 Revised 19-Oct-07
Hymenidin
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SYNONYMS 2-Debromooroidin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-291-M001   1 mg 230.00 USD Add To Cart
Product Specification
FORMULA: C11H12BrN5O
MW: 310.2
CAS NUMBER: 107019-95-4
SOURCE/HOST: Isolated from Hymeniacidon sp.
PURITY: ≥95%
APPEARANCE: Amorphous solid.
SOLUBILITY: Soluble in DMSO or 100 % ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC. CYTOTOXIC.

Product Description
Antagonist of serotonergic receptors. Inhibitor of CDK5/p25 (IC50=4µM) and GSK-3β (IC50=12µM). 
Product Specific Literature References
A novel antagonist of serotonergic receptors, hymenidin, isolated from the Okinawan marine sponge Hymeniacidon sp: J. Kobayashi, et al.; Experientia 42, 1176 (1986) Abstract
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent: L. Meijer, et al.; Chem. Biol. 7, 51 (2000)
Brominated pyrrole alkaloids from marine Agelas sponges reduce depolarization-induced cellular calcium elevation: U. Bickmeyer, et al.; Toxicon. 44, 45 (2004) Abstract
Marine compounds for the therapeutic treatment of neurological disorders: D. Alonso, et al.; Expert Opininon on Therapeutic Patents 15, 1377 (2005)
 
 
ALX-350-293 Revised 19-Oct-07
(S)-Roscovitine