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Signal Transduction Enzymes / Related Products
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ALX-270-374 Revised 08-Dec-04
5-[(S)-(-)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin
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SYNONYMS Caspase-7 Inhibitor
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Caspase Inhibitors
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ALX-270-374-M001   1 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C14H16N2O5S
MW: 324.4
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or methanol.
HANDLING: Packaged under inert gas. Protect from light.

Product Description
Potent, reversible, non-peptide inhibitor of caspase-3 (Ki=60nm), caspase-7 (Ki=170nM) and caspase-9 (Ki=3.1µM).
Product Specific Literature References
Potent and selective nonpeptide inhibitors of caspases 3 and 7: D. Lee, et al.; J. Med. Chem. 44, 2015 (2001) Abstract
Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality: D. Lee, et al.; J. Biol. Chem. 275, 16007 (2000) Abstract
 
 
ALX-420-036 Revised 21-Jul-05
DICA
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SYNONYMS 2-(2,4-Dichlorophenoxy)-N-(2-mercaptoethyl)acetamide
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Caspase Inhibitors
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ALX-420-036-M005   5 mg 40.00 USD Add To Cart
ALX-420-036-M025   25 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C10H11Cl2NO2S
MW: 280.2
CAS NUMBER: 613665-26-2
PURITY: ≥98% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Do not store DMSO solutions for more than 1 day.
HANDLING: Keep under inert gas. Protect from oxygen.

Product Description
Inhibitor of caspase-3 and caspase-7 binding to an allosteric site and not to the active site.
Product Specific Literature References
Discovery of an allosteric site in the caspases: J.A. Hardy, et al.; PNAS 101, 12461 (2004) Abstract; Full Text
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-260-094 Revised 09-May-06
D2R (high purity)
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SYNONYMS (L-Asp)2 rhodamine 110 (high purity) . TFA salt
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Caspase Substrates
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ALX-260-094-M001   1 mg 120.00 USD Add To Cart
ALX-260-094-5001   5x1 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C28H24N4O9 . CF3COOH
MW: 560.5 . 114.0
PURITY: ≥98%
APPEARANCE: Off-white to orange powder.
SOLUBILITY: Soluble in DMSO.
RECONSTITUTION: Reconstitute in DMSO followed by the addition of ethanol at a ratio 1:1.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Aliquots in DMSO:ethanol (1:1) are stable for at least 1 month when stored at -20°C and stable for at least 6 months when stored at -80°C. Use high purity reagents only as the dye is instable in water. Discard surplus aqueous solutions.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Protect from light.

Product Description
Substrate for detection of intracellular caspase activation by flow cytometry and fluorescence microscopy after apoptosis induction in intact hematopoietic cell lines. For detailed application protocols see [2].
Product Specific Literature References
[1] Rhodamine 110-linked amino acids and peptides as substrates to measure caspase activity upon apoptosis induction in intact cells: H. Hug, et al.; Biochemistry 38, 13906 (1999) Abstract
[2] Fluorogenic substrates as detectors of caspase activity during natural killer cell-induced apoptosis: M. Los, et al.; Methods Mol. Biol. 121, 155 (2000) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION D2R can be used to detect caspase activity (predominantly caspase-3) in intact cells by flow cytometry [1], fluorescence microscopy as well as in cell extracts followed by analysis with a fluorometer (λex: 488nm/λem 550nm). Free (cleaved) Rhodamine 110 emits light both in the FL1 and FL2 channel. Dual staining is possible by employing the FL3 channel for flow cytometry. At least 160 assays can be performed (100µl sample volume (e.g. whole blood sample) and 100µM D2R) [2]. Optimal substrate concentrations for other applications range from 25-50µM D2R and have to be determined empirically for the particular cell system.
 
 
ALX-350-366 Revised 03-Apr-08
Azaspiracid-1
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SYNONYMS AZA-1
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Toxins
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ALX-350-366-C001   1 µg 180.00 USD Add To Cart
Product Specification
FORMULA: C47H71NO12
MW: 842.1
CAS NUMBER: 214899-21-5
SOURCE/HOST: Islolated from marine mussel.
CONCENTRATION:

2μg/ml

PURITY: ≥95%
FORMULATION: Liquid. In methanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HAZARD: VERY TOXIC. MAY BE TERATOGENIC.

Product Description
Activator of JNK (c-Jun-N-terminal kinase). Cellular growth inhibitor and inducer of cytoskeletal alterations. Activator of caspases. Modulator of intracellular cAMP (cyclic adenosine monophosphate) and calcium levels. Inhibitor of cholesterol biosynthesis in human T lymphocyte cells. Potent teratogen to finfish. Cytotoxic to mammalian cells.
Product Specific Literature References
Multiple organ damage caused by a new toxin azaspiracid, isolated from mussels produced in Ireland: E. Ito, et al.; Toxicon 38, 917 (2000) Abstract
Azaspiracid-1, a potent, nonapoptotic new phycotoxin with several cell targets: Y. Roman, et al.; Cell. Signal. 14, 703 (2002) Abstract
Teratogenic effects of azaspiracid-1 identified by microinjection of Japanese medaka (Oryzias latipes) embryos: J.R. Coleman, et al.; Toxicon 45, 881 (2005) Abstract
Cytotoxic and cytoskeletal effects of azaspiracid-1 on mammalian cell lines: M.J. Twiner, et al.; Toxicon 45, 891 (2005) Abstract
Azaspiracids modulate intracellular pH levels in human lymphocytes: A. Alfonso, et al.; BBRC 346, 1091 (2006) Abstract
Cell growth inhibition and actin cytoskeleton disorganization induced by azaspiracid-1 structure-activity studies: N. Vilarino, et al.; Chem. Res. Toxicol. 19, 1459 (2006) Abstract
The c-Jun-N-terminal kinase is involved in the neurotoxic effect of azaspiracid-1: C. Vale, et al.; Cell Physiol. Biochem. 20, 957 (2007) Abstract
Effects of azaspiracid-1, a potent cytotoxic agent, on primary neuronal cultures. A structure-activity relationship study: C. Vale, et al.; J. Med. Chem. 50, 356 (2007) Abstract
Irreversible cytoskeletal disarrangement is independent of caspase activation during in vitro azaspiracid toxicity in human neuroblastoma cells: N. Vilarino, et al.; Biochem. Pharmacol. 74, 327 (2007) Abstract
Transcriptional profiling and inhibition of cholesterol biosynthesis in human T lymphocyte cells by the marine toxin azaspiracid: M.J. Twiner, et al.; Genomics 91, 289 (2008) Abstract
 
 
ALX-420-031 Revised 11-Jun-04
PETCM
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SYNONYMS α-(Trichloromethyl)-4-pyridineethanol
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Prothymosin alpha
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ALX-420-031-M010   10 mg 30.00 USD Add To Cart
ALX-420-031-M050   50 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C8H8Cl3NO
MW: 240.5
CAS NUMBER: 10129-56-3
PURITY: ≥95%
APPEARANCE: White to brownish powder.
SOLUBILITY: Soluble in dimethyl formamide, DMSO or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: HARMFUL. IRRITANT.
MELTINGPOINT: 164°C

Product Description
Activator of caspase-3 in cell extracts. Relieves prothymosin α inhibition and promotes apoptosome formation at a physiological concentration of deoxyadenosine triphosphate.
Product Specific Literature References
Distinctive roles of PHAP proteins and prothymosin-alpha in a death regulatory pathway: X. Jiang, et al.; Science 299, 223 (2003) Abstract
Further Categories Containing This Product:
Caspases Other Products
 
 
ALX-420-035 Revised 03-May-05
Apoptosis Activator 2
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SYNONYMS 1-[(3,4-Dichlorophenyl)methyl]-1H-indole-2,3-dione
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Apoptosis Inducers & Inhibitors Other Products
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ALX-420-035-M005   5 mg 45.00 USD Add To Cart
ALX-420-035-M025   25 mg 180.00 USD Add To Cart
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Product Specification
FORMULA: C15H9NO2Cl2
MW: 306.1
CAS NUMBER: 79183-19-0
PURITY: ≥98% (NMR)
APPEARANCE: Orange to red solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Induces apoptosis by promoting the oligomerization of Apaf-1 into the mature, functional apoptosome, triggering caspase-9 activation resulting in activated caspase-3. Shows strong selectivity for cancer cells against normal cell lines. Acts in a similar way like apoptosis inducer PETCM (Prod. No. ALX-420-031).
Product Specific Literature References
Direct activation of the apoptosis machinery as a mechanism to target cancer cells: J.T. Nguyen and J.A. Wells; PNAS 100, 7533 (2003) Abstract; Full Text
Further Categories Containing This Product:
Caspases Other Products
 
 
ALX-430-146 Revised 30-Nov-06
PAC-1
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SYNONYMS 4-(Phenylmethyl)[[2-hydroxy-3-(2-propenyl)phenyl]methylene]hydrazide-1-piperazine acetic acid
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Apoptosis Inducers)
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ALX-430-146-M010   10 mg 45.00 USD Add To Cart
ALX-430-146-M050   50 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C23H28N4O2
MW: 392.5
CAS NUMBER: 315183-21-2
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in acetonitrile, DMSO, dioxane or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
First molecule to directly activate procaspase-3 to caspase-3 in vitro. Has been shown to induce apoptosis in cancer cells.
Product Specific Literature References
Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy: K.S. Putt, et al.; Nat. Chem. Biol. 2, 543 (2006) Abstract
Further Categories Containing This Product:
Caspases Other Products
 
 
ALX-260-005 Revised 03-Mar-05
Chymostatin
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SYNONYMS (S)-1-Carboxy-2-phenylethyl)-carbamoyl-α-[2-iminohexahydro-4(S)-pyrimidyl]-(S)-glycyl-X-phenylalaninal
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-260-005-M001   1 mg 22.00 USD Add To Cart
ALX-260-005-M005   5 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C21H38N4O8
MW: 605.0 (average)
CAS NUMBER: 9076-44-2
SOURCE/HOST: Microbial.
SOLUBILITY: Soluble in DMSO (20 mg/ml) or glacial acetic acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of serine proteinases having a chymotrypsin-like specificity like α-, β-, δ- and γ-chymotrypsin, chymases, cathepsin G, and most cysteine proteinases including papain and cathepsin A, B, H, and L. Mixture of type A (R=L-Leu), type B (R=L-Val), type C (R=L-Ile).
Product Specific Literature References
Chymostatin, a new chymotrypsin inhibitor produced by actinomycetes: H. Umezawa, et al.; J. Antibiot. 23, 425 (1970) Abstract
Further Categories Containing This Product:
Proteases Other Products
 
 
ALX-260-007 Revised 16-Feb-05
E-64
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SYNONYMS N-[N-(L-3-trans-Carboxyoxirane-2-carbonyl]-L-leucyl)-agmatine
L-trans-Epoxysuccinyl-leucylamide-(4-guanido)-butane
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-260-007-M005   5 mg 55.00 USD Add To Cart
ALX-260-007-M025   25 mg 195.00 USD Add To Cart
Product Specification
FORMULA: C15H27N5O5
MW: 357.4
CAS NUMBER: 66701-25-5
SOURCE/HOST: Synthetic.
PURITY: ≥99%
SOLUBILITY: Soluble in DMSO or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Irreversible inhibitor of cysteine proteinases like papain, cathepsin B and L. Acts by forming a thioether bond with the thiol of the active cysteine. Does not inhibit serine proteinases.
Product Specific Literature References
K. Hanada, et al.; Agric. Biol. Chem. 42, 529 (1978)
K. Hanada, et al.; Agric. Biol. Chem. 42, 523 (1978)
Further Categories Containing This Product:
Proteases Other Products
 
 
ALX-260-014 Revised 19-Aug-08
Calpeptin
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SYNONYMS Z-Leu-norleucinal
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calpains / Related Products
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ALX-260-014-M005   5 mg 85.00 USD Add To Cart
ALX-260-014-M010   10 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C20H30N2O4
MW: 362.5
CAS NUMBER: 117591-20-5
PURITY: ≥94% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: 5mg/ml soluble in DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 2 months when stored at -20°C.
HANDLING: Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C. Protect from light and moisture.

Product Description
Membrane permeable inhibitor of calpain I and II and cathepsin L. Promotes neurite elongation in differentiating PC12 cells. Prevents Ca2+-ionophore induced degradation of actin binding protein and P235 in platelets. Inhibits myosin light chain phosphorylation in platelets stimulated by collagen, ionomycin (Prod. No. ALX-450-006) or thrombin.
Product Specific Literature References
Inhibitory effect of di- and tripeptidyl aldehydes on calpains and cathepsins: T. Sasaki, et al.; J. Enz. Inhib. 3, 195 (1990) Abstract
Cell-penetrating inhibitors of calpain: S. Mehdi; TIBS 16, 150 (1991) Abstract
Specificity of calcium-activated neutral pr