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Nuclear Envelope & Nuclear Transport
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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
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors / Related Products • Nuclear Envelope & Nuclear Transport • Antitumor Antibiotics • Antibiotics - Antifungal • Antitumor Agents (Anti-proliferative)
 
 
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:
Cell Cycle Blockers & Inhibitors / Related Products • Nuclear Envelope & Nuclear Transport • Antitumor Antibiotics • Antibiotics - Antifungal • Antitumor Agents (Anti-proliferative)
 
 
ALX-350-004 Revised 08-Apr-08
Thapsigargin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Tumor Promoters
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ALX-350-004-M001   1 mg 50.00 USD Add To Cart
ALX-350-004-M005   5 mg 200.00 USD Add To Cart
ALX-350-004-M010   10 mg 350.00 USD Add To Cart
ALX-350-004-M025   25 mg 690.00 USD Add To Cart
Product Specification
FORMULA: C34H50O12
MW: 650.8
CAS NUMBER: 67526-95-8
MERCK INDEX: 14: 9272
PURITY: ≥95% (HPLC)
APPEARANCE: Clear colorless film.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light and oxygen.
HAZARD: HIGHLY IRRITANT. HARMFUL.

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Product Description
Cell permeable tumor promoter by specific inhibition of the (sarco)endoplasmatic reticulum Ca2+-ATPase (SERCA). Inhibition of SERCA reveals a significant change in intracellular Ca2+ homeostasis and pH regulation in tumor cells. Does not increase inositol phosphates. Shows no effect on protein kinase C (PKC). Increases Ca2+-dependent Na+ influx in human platelets in a dose-dependent manner. Induces apoptosis. Stimulates nitric oxide (NO) production, contributing to hepatocyte apoptosis.
Product Specific Literature References
Brefeldin A, thapsigargin, and AIF4- stimulate the accumulation of GRP78 mRNA in a cycloheximide dependent manner, whilst induction by hypoxia is independent of protein synthesis: B.D. Price, et al.; J. Cell. Physiol. 152, 545 (1992) Abstract
Thapsigargin, a Ca(2+)-ATPase inhibitor, depletes the intracellular Ca2+ pool and induces apoptosis in human hepatoma cells: A. Tsukamoto & Y. Kaneko; Cell Biol. Int. 17, 969 (1993) Abstract
The role of calcium, pH, and cell proliferation in the programmed (apoptotic) death of androgen-independent prostatic cancer cells induced by thapsigargin: Y. Furuya, et al.; Cancer Res. 54, 6167 (1994) Abstract
Intracellular Ca2+ signals activate apoptosis in thymocytes: studies using the Ca(2+)-ATPase inhibitor thapsigargin: S. Jiang, et al.; Exp. Cell Res. 212, 84 (1994) Abstract
Role of EGR-1 in thapsigargin-inducible apoptosis in the melanoma cell line A375-C6: S. Muthukkumar, et al.; Mol. Cell. Biol. 15, 6262 (1995) Abstract; Full Text
Baculovirus p35 and Z-VAD-fmk inhibit thapsigargin-induced apoptosis of breast cancer cells: X.M. Qi, et al.; Oncogene 15, 1207 (1997) Abstract
Signal transduction of thapsigargin-induced apoptosis in osteoblast: H.J. Chae, et al.; Bone 25, 453 (1999) Abstract
Nitric oxide is involved in apoptosis induced by thapsigargin in rat mesangial cells: A.M. Rodriguez-Lopez, et al.; Cell Physiol. Biochem. 9, 285 (1999) Abstract
Thapsigargin induces apoptosis in cultured human aortic smooth muscle cells: C. Peiro, et al.; J. Cardiovasc. Pharmacol. 36, 676 (2000) Abstract
Thapsigargin induces a calmodulin/calcineurin-dependent apoptotic cascade responsible for the death of prostatic cancer cells: B. Tombal, et al.; Prostate 43, 303 (2000) Abstract
Changes in intracellular Ca2+ and pH in response to thapsigargin in human glioblastoma cells and normal astrocytes: G.G. Kovacs, et al.; Am. J. Physiol. Cell. Physiol. 289, C361 (2005) Abstract
Thapsigargin, a selective inhibitor of sarco-endoplasmic reticulum Ca2+ -ATPases, modulates nitric oxide production and cell death of primary rat hepatocytes in culture: N.K. Canova, et al.; Cell Biol. Toxicol. 23, 337 (2007) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Dissolving of 0.65mg Thapsigargin in 1ml gives a stock solution of 1mM.
General Literature References
Role of Ca2(+)-ATPases in regulation of cellular Ca2+ signalling, as studied with the selective microsomal Ca2(+)-ATPase inhibitor, thapsigargin: O. Thastrup; Agents Actions 29, 8 (1990), (Review) Abstract
Thapsigargin, a high affinity and global inhibitor of intracellular Ca2+ transport ATPases: G. Inesi and Y. Sagara; Arch. Biochem. Biophys. 298, 313 (1992), (Review) Abstract
Use of thapsigargin to study Ca2+ homeostasis in cardiac cells: T.B. Rogers, et al.; Biosci. Rep. 15, 341 (1995), (Review) Abstract
The sarcoplasmic reticulum Ca2+ pump: inhibition by thapsigargin and enhancement by adenovirus-mediated gene transfer: G. Inesi, et al.; Ann. NY Acad. Sci. 853, 195 (1998), (Review) Abstract; Full Text
A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca(2+)-ATPases: M. Treiman, et al.; TIPS 19, 131 (1998), (Review) Abstract
Further Categories Containing This Product:
Ca2+-ATPase / Related Products • Autophagy Other Products • Other Natural Products - DNA Regulation / Transcription • Nuclear Envelope & Nuclear Transport • Endoplasmatic Reticulum Stress • Carcinogens & Tumor Promoters Other Products • Natural Products - Nitric Oxide Pathway Modulators • Natural Products - ATPase Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-380-100 Revised 14-Mar-08
Leptomycin B
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SYNONYMS LMB
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-100-C100   100 µg 95.00 USD Add To Cart
Product Specification
FORMULA: C33H48O6
MW: 540.7
CAS NUMBER: 87081-35-4
SOURCE/HOST: Isolated from Streptomyces sp.
CONCENTRATION: 0.2mg/ml
PURITY: ≥98% (HPLC)
FORMULATION: Liquid. In 100% ethanol.
SOLUBILITY: Soluble in methanol or 100% ethanol; insoluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Packaged under inert gas.
HAZARD: TOXIC. FLAMMABLE.

Product Description
Antifungal antibiotic that acts as an inhibitor of nuclear export by interacting with CRM1/exportin-1. Inhibits nucleo-cytoplasmic translocation of molecules such as the HIV-1 Rev protein and Rev-dependent export of mRNA. Other proteins that are influenced by leptomycin B are actin, c-Abl, cyclin B1, MDM2/p53, Iκb, MPF and PKA.
Product Specific Literature References
Leptomycins A and B, new antifungal antibiotics. I. Taxonomy of the producing strain and their fermentation, purification and characterization: T. Hamamoto, et al.; J. Antibiot. (Tokyo) 36, 639 (1983) Abstract
Ratjadone and leptomycin B block CRM1-dependent nuclear export by identical mechanisms: T. Meissner, et al.; FEBS Lett. 576, 27 (2004) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Please also see our Product Flyer "LEPTOMYCIN A+B, Inhibitors of Nuclear-Cytoplasmic Transport".
Further Categories Containing This Product:
CDK & Cyclin Inhibitors • Nuclear Envelope & Nuclear Transport • Antibiotics for Cell Cycle Research
 
 
ALX-380-101 Revised 12-Oct-07
Leptomycin A
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SYNONYMS ATS1287 A
LMA
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-101-C050   50 µg 75.00 USD Add To Cart
ALX-380-101-C100   100 µg 120.00 USD Add To Cart
Product Specification
FORMULA: C32H46O6
MW: 526.7
CAS NUMBER: 87081-36-5
SOURCE/HOST: Isolated from Streptomyces sp.
CONCENTRATION: 0.1mg/ml
PURITY: ≥95% (HPLC)
APPEARANCE: Liquid. In 100% ethanol.
SOLUBILITY: Soluble in methanol or 100% ethanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Packaged under inert gas.
HAZARD: FLAMMABLE. TOXIC.

Product Description
Antifungal antibiotic that acts as an inhibitor of nuclear export by interacting with CRM1/exportin-1. Inhibits nucleo-cytoplasmic translocation of molecules such as the HIV-1 Rev protein and Rev-dependent export of mRNA.
Product Specific Literature References
Leptomycins A and B, new antifungal antibiotics. I. Taxonomy of the producing strain and their fermentation, purification and characterization: T. Hamamoto, et al.; J Antibiot (Tokyo) 36, 639 (1983) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Please also see our Product Flyer "LEPTOMYCIN A+B, Inhibitors of Nuclear-Cytoplasmic Transport".
Further Categories Containing This Product:
Antibiotics for Cell Cycle Research • Nuclear Envelope & Nuclear Transport
 
 
ALX-450-013 Revised 22-Feb-08
BAPTA . tetrapotassium salt
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SYNONYMS 1,2-bis(2-Aminophenoxy)ethane-N,N,N',N'-tetraacetic acid . 4K
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calcium Chelators / Caged Calcium Chelators
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ALX-450-013-G001   1 g 98.00 USD Add To Cart
Product Specification
FORMULA: C22H20N2O10 . 4K
MW: 472.4 . 156.4
CAS NUMBER: 73630-08-7
PURITY: ≥97% (as anhydride)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light and moisture.

Product Description
Highly selective Ca2+ chelating agent.
Product Specific Literature References
New calcium indicators and buffers with high selectivity against magnesium and protons: design, synthesis, and properties of prototype structures: R.Y. Tsien; Biochemistry 19, 2396 (1980) Abstract
Calcium-independent increase of transmitter release at frog end-plate by trinitrobenzene sulphonic acid: H. Kijima & T. Tanabe; J. Physiol. 403, 135 (1988) Abstract
Transmitter release at frog end-plate loaded with a Ca2+-chelator, BAPTA: hypertonicity and erythrosin B augment the release independently of internal Ca2+: N. Tanabe & H. Kijima; Neurosci. Lett. 92, 52 (1988) Abstract
Properties of neuroprotective cell-permeant Ca2+ chelators: effects on [Ca2+]i and glutamate neurotoxicity in vitro: M. Tymianski, et al.; J. Neurophysiol. 72, 1973 (1994) Abstract
Chelation of intracellular Ca2+ inhibits murine keratinocyte differentiation in vitro: L. Li, et al.; J. Cell Physiol. 163, 105 (1995) Abstract
Further Categories Containing This Product:
Dyes / Stains / Fluorescent Probes / Fluorescent Labels • Nuclear Envelope & Nuclear Transport
 
 
ALX-450-014 Revised 22-Feb-08
BAPTA/AM
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SYNONYMS 1,2-bis(2-Aminophenoxy)ethane-N,N,N',N'-tetraacetic acid tetrakis(acetoxymethyl) ester
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calcium Chelators / Caged Calcium Chelators
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ALX-450-014-M010   10 mg 48.00 USD Add To Cart
ALX-450-014-M050   50 mg 195.00 USD Add To Cart
Product Specification
FORMULA: C34H40N2O18
MW: 764.7
CAS NUMBER: 126150-97-8
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Packaged under inert gas. Protect from light and moisture.
HAZARD: IRRITANT.
IDENTITY: Determined by 1H-NMR.

Product Description
Cell permeable acetoxymethyl ester derivative of BAPTA (Prod. No. ALX-450-013). Useful for controlling intracellular Ca2+ concentration. Induces inactivation of protein kinase C. Also inhibits thapsigargin-induced apoptosis in rat thymocytes.
Product Specific Literature References
Physiological [Ca2+]i level and pump-leak turnover in intact red cells measured using an incorporated Ca chelator: V.L. Lew, et al.; Nature 298, 478 (1982) Abstract
BAPTA induces a decrease of intracellular free calcium and a translocation and inactivation of protein kinase C in macrophages: P. Dieter, et al.; Biol. Chem. Hoppe-Seyler 374, 171 (1993) Abstract
Intracellular calcium chelator, BAPTA-AM, prevents cocaine-induced ventricular fibrillation: G.E. Billman; Am. J. Physiol. 265, H1529 (1993) Abstract
Intracellular Ca2+ signals activate apoptosis in thymocytes: studies using the Ca(2+)-ATPase inhibitor thapsigargin: S. Jiang, et al.; Exp. Cell. Res. 212, 84 (1994) Abstract
Stimulation of the ERK pathway by GTP-loaded Rap1 requires the concomitant activation of Ras, protein kinase C, and protein kinase A in neuronal cells: T. Bouschet, et al.; J. Biol. Chem. 278, 4778 (2003) Abstract; Full Text
Further Categories Containing This Product:
PKC Inhibitors • Apoptosis Inducers & Inhibitors Other Products • Nuclear Envelope & Nuclear Transport
 
 
ALX-167-024 Revised 17-May-06
SN50
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY NF-kB Pathway Inhibitors
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ALX-167-024-C500   500 µg 125.00 USD Add To Cart
Product Specification
SEQUENCE: H-Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Val-Gln-Arg-Lys-Arg-Gln-Lys-Leu-Met-Pro-OH
FORMULA: C129H230N36O29S
MW: 2781.5
PEPTIDE CONTENT: 50-75%
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white solid.
FORMULATION: Counter Ion: Trifluoroacetate salt.
SOLUBILITY: Soluble in distilled water, 100% ethanol or ethanol:water 1:1.
RECONSTITUTION: Reconstitute in sterile distilled water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Peptides in solution have limited stability.
HANDLING: Avoid freeze/thaw cycles. After reconstitution, prepare aliquots and store at -20°C.
Product Description
Inhibits translocation of the NF-κB active complex into the nucleus. In mouse endothelial LE-II cells induced with LPS, inhibition of NF-κB nuclear translocation was 88% at 50µg/ml (18µM). In human monocytic THP-1 cells induced by LPS or TNF-α there was 85% inhibition at 100µg/ml. For control peptide, see SN50M (Prod. No. ALX-167-025).
Product Specific Literature References
Inhibition of nuclear translocation of transcription factor NF-kappa B by a synthetic peptide containing a cell membrane-permeable motif and nuclear localization sequence: Y.Z. Lin, et al.; J. Biol. Chem. 270, 14255 (1995) Abstract; Full Text
p38 MAP kinase and MKK-1 co-operate in the generation of GM-CSF from LPS-stimulated human monocytes by an NF-kappa B-independent mechanism: K.K. Meja, et al.; Br. J. Pharmacol. 131, 1143 (2000) Abstract
Nuclear factor-kappaB activates dual inhibition sites in the regulation of tumor necrosis factor-alpha-induced neutrophil apoptosis: M. Niwa, et al.; Eur. J. Pharmacol 407, 211 (2000) Abstract
Activation of nuclear factor kappaB and induction of apoptosis by tumor necrosis factor-alpha in the mouse uterine epithelial WEG-1 cell line: S. Pampfer, et al.; Biol. Reprod. 63, 879 (2000) Abstract
Interruption of the NF-kappaB pathway by Bay 11-7082 promotes UCN-01-mediated mitochondrial dysfunction and apoptosis in human multiple myeloma cells: Y. Dai, et al.; Blood 103, 2761 (2004) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Nuclear localization sequence (NLS) aa 360-369 (AAVALLPAVLLALLAPVQRKRQKLMP) of the transcription factor NF-κB p50 linked to a peptide cell-permeablization sequence, the hydrophobic region (h-region) of the signal peptide of Kaposi fibroblast growth factor (K-FGF).
Further Categories Containing This Product:
Nuclear Envelope & Nuclear Transport • Peptides
 
 
ALX-167-025 Revised 17-May-06
SN50M Control Peptide
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY NF-kB Pathway Inhibitors
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ALX-167-025-C500 &nbs