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Antibiotics for Cell Cycle Research
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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
 
 
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
 
 
ALX-380-014 Revised 15-May-08
Staurosporine
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SYNONYMS Antibiotic AM-2282
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-380-014-C100   100 µg 47.00 USD Add To Cart
ALX-380-014-C250   250 µg 112.00 USD Add To Cart
ALX-380-014-M001   1 mg 270.00 USD Add To Cart
ALX-380-014-M005   5 mg 790.00 USD Add To Cart
Product Specification
FORMULA: C28H26N4O3
MW: 466.5
CAS NUMBER: 62996-74-1
MERCK INDEX: 14: 8802
RTECS: KC655000
SOURCE/HOST: Isolated from Streptomyces staurosporeus.
PURITY: ≥98%
APPEARANCE: Off-white to green powder.
SOLUBILITY: Soluble in ethyl acetate, DMSO or dimethyl formamide; only slightly soluble in chloroform and methanol. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable for at least 2 years after receipt when stored +4°C.
HANDLING: Protect from light and moisture.
HAZARD: HARMFUL. MAY BE CARCINOGENIC.

Product Description
Model apoptosis inducer. Potent cell-permeable inhibitor of a variety of protein kinases, e.g. protein kinase C (PKC), CDK1/cyclin B (IC50~5nM), CDK2/cyclin A (IC50=7nM), CDK4/cyclin D (IC50=3-10µM), CDK5/p25 (IC50=4nM) and GSK-3β (IC50=15nM).
Product Specific Literature References
A new alkaloid AM-2282 of Streptomyces origin. Taxonomy, fermentation, isolation and preliminary characterization: S. Omura, et al.; J. Antibiot. (Tokyo) 30, 275 (1977) Abstract
A. Furusaki, et al.; J. C. S. Chem. Commun. 800 (1978)
Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase: T. Tamaoki, et al.; BBRC 135, 397 (1986) Abstract
Staurosporine, a potent platelet aggregation inhibitor from a Streptomyces species: S. Oka, et al.; Agric. Biol. Chem. 50, 2723 (1986)
Staurosporine inhibits tyrosine-specific protein kinase activity of Rous sarcoma virus transforming protein p60: N. Nakano, et al.; J. Antibiot. (Tokyo) 40, 706 (1987) Abstract
Contrasting actions of staurosporine, a protein kinase C inhibitor, on human neutrophils and primary mouse epidermal cells: T. Sako, et al.; Cancer Res. 48, 4646 (1988) Abstract
Staurosporine, a protein kinase C inhibitor interferes with proliferation of arterial smooth muscle cells: H. Matsumoto & Y. Sasaki; Biochem. Biophys. Res. Commun. 158, 105 (1989) Abstract
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989), (Review) Abstract
Staurosporine: an effective inhibitor for Ca2+/calmodulin-dependent protein kinase II: N. Yanagihara, et al.; J. Neurochem. 56, 294 (1991) Abstract
Is staurosporine a specific inhibitor of protein kinase C in intact porcine coronary arteries?: M. Kageyama, et al.; J. Pharmacol. Exp. Ther. 259, 1019 (1991) Abstract
Induction of a common pathway of apoptosis by staurosporine: R. Bertrand, et al.; Exp. Cell Res. 211, 314 (1994) Abstract
First total synthesis of Staurosporine and ent-Staurosporine: J.T. Link et al.; J. Am. Chem. Soc. 117, 552 (1995)
Staurosporine induces programmed cell death in embryonic neurons and activation of the ceramide pathway: D.A. Wiesner & G. Dawson; J. Neurochem 66, 1418 (1996) Abstract
Staurosporine and ent-staurosporine: the first total synthesis, prospects for a regioselective approach, and activity profile: J.T. Link et al.; J. Am. Chem. Soc. 118, 2825 (1996)
K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996), Review Abstract
Characterization of the cell death process induced by staurosporine in human neuroblastoma cell lines: J. Boix, et al.; Neuropharmacology 36, 811 (1997) Abstract
Caspase-3-dependent cleavage of Bcl-2 promotes release of cytochrome c: D.G. Kirsch, et al.; J. Biol. Chem. 274, 21155 (1999) Abstract; Full Text
Molecular mechanism of staurosporine-induced apoptosis in osteoblasts: H.J. Chae, et al.; Pharmacol. Res. 42, 373 (2000) Abstract
Glycogen synthase kinase-3beta facilitates staurosporine- and heat shock-induced apoptosis. Protection by lithium: G.N. Bijur, et al.; J. Biol. Chem. 275, 7583 (2000) Abstract; Full Text
Dissociation of staurosporine-induced apoptosis from G2-M arrest in SW620 human colonic carcinoma cells: initiation of the apoptotic cascade is associated with elevation of the mitochondrial membrane potential (deltapsim): B.G. Heerdt, et al.; Cancer Res. 60, 6704 (2000) Abstract
Changes in mitochondrial membrane potential during staurosporine- induced apoptosis in Jurkat cells: J.L. Scarlett, et al.; FEBS Lett. 475, 267 (2000) Abstract
Equivalent death of P-glycoprotein expressing and nonexpressing cells induced by the protein kinase C inhibitor staurosporine: K.M. Tainton, et al.; BBRC 276, 231 (2000) Abstract
Caspase-8 activation and bid cleavage contribute to MCF7 cellular execution in a caspase-3-dependent manner during staurosporine-mediated apoptosis: D. Tang, et al.; J. Biol. Chem. 275, 9303 (2000) Abstract; Full Text
Insulin-stimulated protein kinase B phosphorylation on Ser-473 is independent of its activity and occurs through a staurosporine-insensitive kinase: M.M. Hill, et al.; J. Biol. Chem. 276, 25643 (2001) Abstract; Full Text
Single-cell fluorescence resonance energy transfer analysis demonstrates that caspase activation during apoptosis is a rapid process. Role of caspase-3: M. Rehm, et al.; J. Biol. Chem. 277, 24506 (2002) Abstract; Full Text
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ALX-380-056 Revised 10-May-07
Verruculogen
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-380-056-M001   1 mg 60.00 USD Add To Cart
ALX-380-056-M005   5 mg 225.00 USD Add To Cart
Product Specification
FORMULA: C27H33N3O7
MW: 511.2
CAS NUMBER: 12771-72-1
RTECS: JH4920000
SOURCE/HOST: Isolated from Penicillium verruculosum.
PURITY: ≥96%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in ethyl acetate, DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: VERY TOXIC.

Product Description
Neurotoxin that acts as an inhibitor of the M phase of the mammalian cell cycle. Inhibits Ca2+-activated K+ channels. Decreases GABA levels in CNS.
Product Specific Literature References
Tremorgenic indole alkaloids potently inhibit smooth muscle high- conductance calcium-activated potassium channels: H.H. Knaus, et al.; Biochemistry 33, 5819 (1994) Abstract
Novel mammalian cell cycle inhibitors, tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. II. Physico- chemical properties and structures: C.B. Cui, et al.; J. Antibiot. (Tokyo) 49, 534 (1996) Abstract
Verruculogen production in airborne and clinical isolates of Aspergillus fumigatus Fres.: I. Kosalec, et al.; Acta Pharm. 55, 357 (2005) Abstract
 
 
ALX-380-068 Revised 09-Apr-08
Trichostatin A
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SYNONYMS TSA
[R-(E,E)]-7-[4-(Dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide]
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics - DNA Regulation / Transcription
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ALX-380-068-M001   1 mg 115.00 USD Add To Cart
ALX-380-068-M005   5 mg 385.00 USD Add To Cart
Product Specification
FORMULA: C17H22N2O3
MW: 302.4
CAS NUMBER: 58880-19-6
MERCK INDEX: 14: 9649
SOURCE/HOST: Isolated from Streptomyces hygroscopicus.
PURITY: ≥98% (HPLC)
APPEARANCE: Whitish film adhered to inside of vial.
SOLUBILITY: Soluble in DMSO, dimethyl formamide, acetonitrile, methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Potent, reversible inhibitor of histone deacetylase (HDAC). Mediates the activation of O6-methylguanine-DNA methyltransferase (MGMT). May be involved in cell cycle progression of several cell types. Induces cell growth arrest at both G1 and G2/M phases. May induce apoptosis in some cases. Induces acetylation of histone-3/4 and expression of p300.
Product Specific Literature References
A new antifungal antibiotic, trichostatin: N. Tsuji, et al.; J. Antibiot. 29, 1 (1976) Abstract
Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A: M. Yoshida, et al.; J. Biol. Chem. 265, 17174 (1990) Abstract; Full Text
Trichostatin A induces morphological changes and gelsolin expression by inhibiting histone deacetylase in human carcinoma cell lines: Y. Hoshikawa, et al.; Exp. Cell Res. 214, 189 (1994) Abstract
Trichostatin A inhibits both ras-induced neurite outgrowth of PC12 cells and morphological transformation of NIH3T3 cells: M. Futamura, et al.; Oncogene 10, 1119 (1995) Abstract
Trichostatin A and trapoxin: novel chemical probes for the role of histone acetylation in chromatin structure and function: M. Yoshida, et al.; Bioessays 17, 423 (1995) Abstract
Selective inhibition of IL-2 gene expression by trichostatin A, a potent inhibitor of mammalian histone deacetylase: I. Takahashi, et al.; J. Antibiot. 49, 453 (1996) Abstract
A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p: J. Taunton, et al.; Science 272, 408 (1996) Abstract
Transcriptional activation and chromatin remodeling of the HIV-1 promoter in response to histone acetylation: C. Van Lint, et al.; EMBO J. 15, 1112 (1996) Abstract
Induction of caspase-3 protease activity and apoptosis by butyrate and trichostatin A (inhibitors of histone deacetylase): dependence on protein synthesis and synergy with a mitochondrial/cytochrome c- dependent pathway:: V. Medina, et al.; Cancer Res. 57, 3697 (1997) Abstract
A histone deacetylase inhibitor potentiates retinoid receptor action in embryonal carcinoma cells: S. Minucci, et al.; PNAS 94, 11295 (1997) Abstract; Full Text
Histone deacetylase inhibitor activates the WAF1/Cip1 gene promoter through the Sp1 sites: Y. Sowa, et al.; BBRC 241, 142 (1997) Abstract
Retinoblastoma protein recruits histone deacetylase to repress transcription: A. Brehm, et al.; Nature 391, 597 (1998) Abstract
Effects of cell density and trichostatin A on the expression of HDAC1 and p57Kip2 in Hep 3B cells: S.G. Gray & T.J. Ekstrom; BBRC 245, 423 (1998) Abstract
Regulation of the human O6-methylguanine-DNA methyltransferase gene by transcriptional coactivators cAMP response element-binding protein- binding protein and p300: K.K. Bhakat & S. Mitra; J. Biol. Chem. 275, 34197 (2000) Abstract; Full Text
Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells: P.A. Marks, et al.; J. Natl. Cancer Inst. 92, 1210 (2000) Abstract
Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivo: D.M. Vigushin, et al.; Clin. Cancer Res. 7, 971 (2001) Abstract
Chromatin remodeling agent trichostatin A: a key-factor in the hepatic differentiation of human mesenchymal stem cells derived of adult bone marrow: S. Snykers, et al.; BMC Dev. Biol. 7, 24 (2007) Abstract
Trichostatin A induces myocardial differentiation of monkey ES cells: M. Hosseinkhani, et al.; BBRC 356, 386 (2007) Abstract
 
 
ALX-380-071 Revised 18-Nov-08
Rifampicin
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SYNONYMS Rifampin
3-(4-Methylpiperazinyl-iminomethyl)rifamycin SV
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-380-071-M100   100 mg 18.00 USD Add To Cart
Product Specification
FORMULA: C43H58N4O12
MW: 823.0
CAS NUMBER: 13292-46-1
MERCK INDEX: 14: 8216
RTECS: VJ7000000
SOURCE/HOST: Semisynthetic.
PURITY: ≥95%
APPEARANCE: Orange to brown powder.
SOLUBILITY: Soluble in DMSO (25mg/ml) or methanol (25mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Antibacterial (tuberculostatic). Inhibits DNA-dependent RNA polymerase. Potent inducer of hepatic cytochrome P450 enzymes.
Product Specific Literature References
Rifampicin: a new orally active rifamycin: N. Maggi, et al.; Chemotherapy 11, 285 (1966) Abstract
Rifampicin sensitivity of the components of DNA-dependent RNA polymerase: E. di Mauro, et al.; Nature 222, 533 (1969) Abstract
Chemical and biological properties of rifampicin: S. Furesz; Antibiot. Chemother. 16, 316 (1970) Abstract
On the mechanism of rifampicin inhibition of RNA synthesis: W.R. McClure and C.L. Cech; J. Biol. Chem. 253, 8949 (1978) Abstract
Pharmacokinetic drug interactions with rifampicin: K. Venkatesan; Clin. Pharmacokinet. 22, 47 (1992), Review Abstract
Pharmacokinetic interactions with rifampicin : clinical relevance: M. Niemi, et al.; Clin. Pharmacokinet. 42, 819 (2003), Review Abstract
Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor: J. Chen and K. Raymond; Ann. Clin. Microbiol. Antimicrob. 50, 3 (2006), Review Abstract
 
 
ALX-380-090 Revised 12-Mar-08
Tryprostatin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cytoskeletal Research
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ALX-380-090-C500   500 µg 179.00 USD Add To Cart
Product Specification
FORMULA: C22H27N3O3
MW: 381.5
SOURCE/HOST: Isolated from Aspergillus fumigatus.
PURITY: ≥90%
APPEARANCE: White powder.
SOLUBILITY: Soluble in methanol, 100% ethanol or DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Diketopiperazine. Arrests cell cycle progression at the G2/M phase. Inhibitor of MAP-dependent microtubule assembly. Inhibits the ABC-transporter breast cancer resistance protein (BCRP) and thereby reverses the resistance of cancer cells against antitumor drugs.
Product Specific Literature References
Tryprostatins A and B, novel mammalian cell cycle inhibitors produced by Aspergillus fumigatus: C.B. Cui, et al.; J. Antibiot. 48, 1382 (1995) Abstract
Novel mammalian cell cycle inhibitors, tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. I. Taxonomy, fermentation, isolation and biological properties: C.B. Cui, et al.; J. Antibiot. 49, 527 (1996) Abstract
Novel mammalian cell cycle inhibitors, tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. II. Physico-chemical properties and structures: C.B. Cui, et al.; J. Antibiot. 49, 534 (1996) Abstract
Tryprostatin A, a specific and novel inhibitor of microtubule assembly: T. Usui, et al.; Biochem. J. 333, 543 (1998) Abstract; Full Text
Reversal of breast cancer resistance protein-mediated drug resistance by tryprostatin A: H. Woehlecke, et al.; Int. J. Cancer 107, 721 (2003) Abstract
 
 
ALX-380-092 Revised 03-Jul-08
Radicicol
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SYNONYMS Monorden
1aS-(1aR*,2Z,4E,14*,15aR*)]-8-Chloro-1a,14,15,15a-tetrahydro-9,11-dihydroxy-14-methyl-6H-oxireno[e][2]benzoxacyclotetradecin-6,12(7H)-dione
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-092-M001   1 mg 75.00 USD Add To Cart
ALX-380-092-M005   5 mg 295.00 USD Add To Cart
Product Specification
FORMULA: C18H17ClO6
MW: 364.8
CAS NUMBER: 12772-57-5
MERCK INDEX: 14: 6253
RTECS: RR1105000
SOURCE/HOST: Isolated from Humicola fuscoatra.
PURITY: ≥98% (HPLC)
APPEARANCE: White to light yellow powder.
SOLUBILITY: Soluble in DMSO, methanol or acetone.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Antifungal macrocycl