ALEXIS Biochemicals: ERT Protein Kinase Substrate Amide

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ALX-270-364

Revised 03-Mar-05

3-(3,5-Di-tert-butyl-4-hydroxybenzylidenyl)indolin-2-one
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Tyrosine Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-364-M001		1 mg	50.00 USD
ALX-270-364-M005		5 mg	200.00 USD

Product Specification

FORMULA:	C₂₃H₂₇NO₂
MW:	349.5
CAS NUMBER:	40526-64-5
SOURCE/HOST:	Synthetic.
PURITY:	≥97% (¹H-NMR, HPLC)
APPEARANCE:	Yellow crystals.
SOLUBILITY:	Soluble in DMSO (35mg/ml) or methanol (2.5mg/ml). Sparingly soluble in aqueous buffers (25µg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
USE/STABILITY:	Stable as a powder for at least 2 years when stored at +4°C in the dark. Stock solutions made in DMSO should be stored in the dark and used within one month.
HANDLING:	Protect from light. Keep cool and dry.
IDENTITY:	Identity determined by ¹H-NMR, ¹³C-NMR, IR, ESI-MS and UV.

Product Description

Receptor tyrosine kinase (RTK) inhibitor. Inhibits FLK-1 RTK (IC₅₀~8µM) and EGF RTK. Consists of the E- and Z-isomers [1].

Product Specific Literature References

[1] Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases: L. Sun, et al.; J. Med. Chem. 41, 2588 (1998) Abstract

ALX-480-045

Revised 23-Jan-08

N6,O2’-Dibutyryladenosine 3’,5’-cyclic Monophosphate . sodium salt
SYNONYMS	Dibutyryl-cAMP . Na cAMP, DB-, . Na Bucladesine . Na
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	cAMP Derivatives

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-480-045-M005		5 mg	25.00 USD
ALX-480-045-M025		25 mg	75.00 USD

Product Specification

FORMULA:	C₁₈H₂₃N₅O₈P . Na
MW:	468.4 . 23.0
CAS NUMBER:	16980-89-5
PURITY:	≥97%
APPEARANCE:	White lyophilized solid.
SOLUBILITY:	Soluble in water (200mM), DMSO (200mM) or 96% ethanol (25mM).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Solutions must be stored in the refrigerator and should be lyophilized and frozen for longer storage periods.

Product Description

Membrane permeable activator of cAMP-dependent protein kinase (cAMP agonist). The product releases butyrate due to intracellular and extracellular esterase action. Butyrate was shown to have distinct biological effects.

Product Specific Literature References

Analogs of cyclic AMP and cyclic GMP: general methods of synthesis and the relationship of structure to enzymic activity: R.B. Meyer & J.P. Miller; Life Sci. 14, 1019 (1974) Abstract
The preparation of acylated derivatives of cyclic nucleotides: T. Posternak & G. Weimann; Meth. Enzymol. 38, 399 (1974) Abstract
Lack of correlation between activation of cyclic AMP-dependent protein kinase and inhibition of contraction of rat vas deferens by cyclic AMP analogs: Y.-J. Hei, et al.; Mol. Pharmacol. 39, 233 (1991) Abstract
Up-regulation of oxytocin receptors in rabbit amnion by adenosine 3',5'- monophosphate: A. Hinko and M.S. Soloff; Endocrinology 132, 126 (1993) Abstract
Transcription of the gene for parathyroid hormone-related peptide from the human is activated through a cAMP-dependent pathway by prostaglandin E1 in HTLV-I-infected T cells: K. Ikeda, et al.; J. Biol. Chem. 268, 1174 (1993) Abstract; Full Text
Apoptosis of vascular smooth muscle cells. Protein kinase C and oncoprotein Bcl-2 are involved in regulation of apoptosis in non- transformed rat vascular smooth muscle cells: D. Leszczynski, et al.; Am. J. Pathol. 145, 1265 (1994) Abstract

Further Categories Containing This Product:

PKA Activators

ALX-480-046

Revised 17-Sep-08

N2,2'-O-Dibutyrylguanosine 3',5'-cyclic Monophosphate . sodium salt
SYNONYMS	Dibutyryl-cGMP . Na DBcGMP . Na
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	cGMP Derivatives

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-480-046-M005		5 mg	40.00 USD
ALX-480-046-M025		25 mg	160.00 USD

Product Specification

FORMULA:	C₁₈H₂₃N₅O₉P . Na
MW:	484.4 . 23.0
CAS NUMBER:	51116-00-8
PURITY:	≥97% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in water, 100% ethanol, DMSO, dimethyl formamide or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
IDENTITY:	Identity determined by ¹H-NMR, MS and UV.

Product Description

Activates cGMP-dependent protein kinase (PKG). Cell permeable. For a better and more selective agonist, use 8-pCPT-cGMP (Prod. No. ALX-480-031 or Prod. No. ALX-480-088).

Product Specific Literature References

Analogs of cyclic AMP and cyclic GMP: general methods of synthesis and the relationship of structure to enzymic activity: R.B. Meyer & J.P. Miller; Life Sci. 14, 1019 (1974) Abstract
Relaxation of hormonally stimulated smooth muscular tissues by the 8- bromo derivative of cyclic GMP: K.D. Schultz, et al.; Naunyn-Schmiedeberg's Arch. Pharmacol. 306, 1 (1979) Abstract
Relaxation of vascular and tracheal smooth muscle by cyclic nucleotide analogs that preferentially activate purified cGMP-dependent protein kinase: S.G. Francis, et al.; Mol. Pharmacol. 34, 506 (1988) Abstract
Cyclic GMP analogs inhibit gamma thrombin-induced arachidonic acid release in human platelets: D.C. Sane, et al.; BBRC 165, 708 (1989) Abstract
Analysis of the functional role of cGMP-dependent protein kinase in intact human platelets using a specific activator 8-para-chlorophenylthio-cGMP: E. Butt, et al.; Biochem. Pharmacol. 43, 2591 (1992) Abstract

Further Categories Containing This Product:

PKG Activators

ALX-270-095

Revised 07-May-08

5,6-Dichloro-1-β-D-ribofuranosyl benzimidazole
SYNONYMS	DRB 5,6-Dichlorobenzimidazole riboside
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Adenosine Derivatives Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-095-M005		5 mg	20.00 USD
ALX-270-095-M025		25 mg	70.00 USD

Product Specification

FORMULA:	C₁₂H₁₂Cl₂N₂O₄
MW:	319.1
CAS NUMBER:	53-85-0
RTECS:	DD7310000
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white crystalline solid.
SOLUBILITY:	Soluble in 100% ethanol, DMSO (100mM) or dimethyl formamide (100mM).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+20°C
USE/STABILITY:	Solutions should be stored in the refrigerator and should be lyophilized and frozen for longer storage periods.
IDENTITY:	Identity determined by ¹H-NMR, MS and UV.

Product Description

Selective casein kinase II inhibitor. Inhibitor of RNA synthesis in eukaryotic cells.

Product Specific Literature References

Halobenzimidazole ribosides and RNA synthesis of cells and viruses: I. Tamm & P. Sehgal; Adv. Virus Res. 22, 187 (1978) Abstract
Mechanism of action of 5,6-dichloro-1-beta-D- ribofuranosylbenzimidazole. II. A resistant human cell mutant with an altered transcriptional machinery: B. Mittleman, et al.; J. Mol. Biol. 165, 461 (1983) Abstract
Mechanism of action of DRB. III. Effect on specific in vitro initiation of transcription: R. Zandomeni, et al.; J. Mol. Biol. 167, 561 (1983) Abstract
Casein kinase type II is involved in the inhibition by 5,6-dichloro-1- beta-D-ribofuranosylbenzimidazole of specific RNA polymerase II transcription: R. Zandomeni, et al.; J. Biol. Chem. 261, 3414 (1986) Abstract; Full Text
Inhibition of germinal vesicle breakdown in bovine oocytes by 5,6- dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB): C.E. Farin & L. Yang; Mol. Reprod. Dev. 37, 284 (1994) Abstract

Further Categories Containing This Product:

Casein Kinase Inhibitors

ALX-480-047

Revised 23-Jul-08

5,6-Dichloro-1-β-D-ribofuranosyl benzimidazole 3',5'-cyclic Monophosphothioate, Sp-Isomer . sodium salt
SYNONYMS	Sp-5,6-DCl-cBIMPS . Na 5,6-DCI-cBIMPS . Na, Sp-Isomer
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Other Cyclic Nucleotides

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-480-047-C100		100 µg	30.00 USD
ALX-480-047-M001		1 mg	190.00 USD

Product Specification

FORMULA:	C₁₂H₁₀Cl₂N₂O₅PS . Na
MW:	396.2 . 23.0
CAS NUMBER:	120912-54-1
PURITY:	≥99%
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in DMSO (167 mM), dimethyl formamide (167 mM), 96 % ethanol (167 mM), methanol (25 mM), water (25 mM) and aqueous buffers such as PBS (pH 7.4; 1.4 mM), 25 mM TRIS (pH 7.4-; 25 mM), 25 mM HEPES (pH 7.2; 35.7 mM) and Na₂HPO₄ (pH 7.0; 2.8 mM).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Potent, specific and site selective activator of cAMP-dependent protein kinases especially suitable for intact cells showing preference for site B of type II isozyme. Completely stable against mammalian phosphodiesterases type I and III and only extremely slowly hydrolyzed by type II. Surpasses the widely used but problematic dibutyryl-cAMP (Prod. No. ALX-480-045) or 8-CPT-cAMP (Prod. No. ALX-480-030) in terms of metabolic stability, membrane permeability and potency.

Product Specific Literature References

Characterization of Sp-5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole- 3',5'-monophosphorothioate (Sp-5,6-DCl-cBiMPS) as a potent and specific activator of cyclic-AMP-dependent protein kinase in cell extracts and intact cells: M. Sandberg, et al.; Biochem J. 279, 521 (1991) Abstract

Further Categories Containing This Product:

PKA Activators

ALX-480-050

Revised 17-Jul-07

6-Dimethylaminopurine
SYNONYMS	N⁶,N⁶-Dimethyladenine 6-DMAP
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	CDK & Cyclin Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-480-050-M100		100 mg	15.00 USD

Product Specification

FORMULA:	C₇H₉N₅
MW:	163.2
CAS NUMBER:	938-55-6
PURITY:	≥97%
APPEARANCE:	Crystalline.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C

Product Description

Non-selective inhibitor of cdc2 and other kinases.

Product Specific Literature References

Inhibition of cyclin-dependent kinases by purine analogues: J. Vesley, et al.; Eur. J. Biochem. 224, 771 (1994)

ALX-300-052

Revised 16-Apr-05

1,2-Dioctanoyl-sn-glycerol
SYNONYMS	DOG
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Mono- & Diacylglycerols

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-300-052-M010		10 mg	30.00 USD
ALX-300-052-M050		50 mg	90.00 USD
ALX-300-052-M100		100 mg	150.00 USD

Product Specification

FORMULA:	C₁₉H₃₆O₅
MW:	344.5
CAS NUMBER:	60514-48-9
PURITY:	≥98%
APPEARANCE:	Clear colorless liquid.
SOLUBILITY:	Soluble in DMSO or chloroform.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	At room temperature DOG is an oil. Due to its instability, keep it cool and dry.

Product Description

Potent activator of protein kinase C (PKC).

Product Specific Literature References

Diacylglycerols release LH: structure-activity relations reveal a role for protein kinase C: P.M. Conn, et al.; BBRC 126, 532 (1985) Abstract
sn-1,2-Dioctanoylglycerol. A cell-permeable diacylglycerol that mimics phorbol diester action on the epidermal growth factor receptor and mitogenesis: R.J. Davis, et al.; J. Biol. Chem. 260, 1562 (1985) Abstract; Full Text
Diacylglycerols mimic phorbol diester induction of leukemic cell differentiation: J.G. Ebeling, et al.; PNAS 82, 815 (1985) Abstract
Activation of protein kinase C by Triton X-100 mixed micelles containing diacylglycerol and phosphatidylserine: Y.A. Hannun, et al.; J. Biol. Chem. 260, 10039 (1985) Abstract; Full Text
Exogenous sn-1,2-diacylglycerols containing saturated fatty acids function as bioregulators of protein kinase C in human platelets: E.G. Lapetina, et al.; J. Biol. Chem. 260, 1358 (1985) Abstract; Full Text

Further Categories Containing This Product:

PKC Activators

ALX-380-110

Revised 03-Apr-08

17-DMAG
SYNONYMS	17-[2-(Dimethylamino)ethyl]amino-17-desmethoxygeldanamycin NSC 707545
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics for Angiogenesis Research

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-110-C100		100 µg	50.00 USD
ALX-380-110-M001		1 mg	150.00 USD

Product Specification

FORMULA:	C₃₂H₄₈N₄O₈
MW:	616.8
CAS NUMBER:	150270-08-9
SOURCE/HOST:	Semisynthetic from geldanamycin (Prod. No. ALX-380-054).
PURITY:	≥99%
APPEARANCE:	Purple to black powder.
SOLUBILITY:	Soluble in water, 100% ethanol (10mg/ml) or DMSO (>25mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Less toxic, more potent synthetic derivative of geldanamycin. Inhibitor of angiogenesis. Inhibitor of heat shock protein 90 (HSP90). Inducer of apoptosis with higher antitumor activity than 17-AAG (Prod. No. ALX-380-091).

Product Specific Literature References

Pharmacokinetics, tissue distribution, and metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (NSC 707545) in CD2F1 mice and Fischer 344 rats: M.J. Egorin, et al.; Cancer Chemother. Pharmacol. 49, 7 (2002) Abstract
Biliary excretion of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) and metabolites by Fischer 344 rats: S.M. Musser, et al.; Cancer Chemother. Pharmacol. 52, 139 (2003) Abstract
Crystal structure and molecular modeling of 17-DMAG in complex with human Hsp90: J.M. Jez, et al.; Chem. Biol. 10, 361 (2003) Abstract
Synthesis and biological activities of novel 17-aminogeldanamycin derivatives: Z.Q. Tian, et al.; Bioorg. Med. Chem. 12, 5317 (2004) Abstract
Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator: G. Kaur, et al.; Clin. Cancer Res. 10, 4813 (2004) Abstract
Enhanced tumor cell radiosensitivity and abrogation of G2 and S phase arrest by the Hsp90 inhibitor 17-(Dimethylaminoethylamino)-17-demethoxygeldanamycin: E.E. Bull, et al.; Clin. Cancer Res. 10, 8077 (2004) Abstract
ErbB3 expression predicts tumor cell radiosensitization induced by Hsp90 inhibition: H. Dote, et al.; Cancer Res. 65, 6967 (2005) Abstract
In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative: M. Hollingshead, et al.; Cancer Chemother. Pharmacol. 56, 115 (2005) Abstract
Comparison of 17-dimethylaminoethylamino-17-demethoxy-geldanamycin (17DMAG) and 17-allylamino-17-demethoxygeldanamycin (17AAG) in vitro: effects on Hsp90 and client proteins in melanoma models: V. Smith, et al.; Cancer Chemother. Pharmacol. 56, 126 (2005) Abstract
Preclinical toxicity of a geldanamycin analog, 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG), in rats and dogs: potential clinical relevance: E.R. Glaze, et al.; Cancer Chemother. Pharmacol. 56, 637 (2005) Abstract
17-Allyamino-17-demethoxygeldanamycin and 17-NN-dimethyl ethylene diamine-geldanamycin have cytotoxic activity against multiple gynecologic cancer cell types: D.R. Gossett, et al.; Gynecol. Oncol. 96, 381 (2005) Abstract
Structure-based design of 7-carbamate analogs of geldanamycin: G. Rastelli, et al.; Biooorg. Med. Chem. Lett. 15, 5016 (2005) Abstract
Generation of a novel anti-geldanamycin antibody: E. Barzilay, et al.; BBRC 330, 561 (2005) Abstract
Determination of the heat shock protein 90 inhibitor 17-dimethylaminoethylamino-17-demethoxygeldanamycin in plasma by liquid chromatography-electrospray mass spectrometry: K. Hwang, et al.; J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. 830, 35 (2006) Abstract

FORMULA:	C₁₃H₉NOSe
MW:	274.2
CAS NUMBER:	60940-34-3
PURITY:	≥98% (NMR)
APPEARANCE:	White to off-white crystalline solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.