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ALX-270-385

Revised 17-Jul-07

Aloisine A
SYNONYMS	RP107 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	CDK & Cyclin Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-385-M001		1 mg	30.00 USD

Product Specification

FORMULA:	C₁₆H₁₇N₃O
MW:	267.3
PURITY:	≥95%
APPEARANCE:	Yellow solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light. Packaged under inert gas.

Product Description

Cell permeable, potent, selective, reversible and ATP-competitive inhibitor of CDK1/cyclin B (IC₅₀=150nM), CDK2/cyclin A (IC₅₀=120nM), CDK2/cyclin E (IC₅₀=400nM), CDK5/p25
(IC₅₀=200nM), CDK5/p35 (IC₅₀=160nM) and GSK-3α (IC₅₀=500nM). Also inhibits GSK-3β (IC₅₀=650nM) and c-Jun N-terminal kinase (JNK) (IC₅₀~3-10µM). Poor inhibitor of CK1, CK2, CDK4/cyclin D1, MAPKK, PKA, PKG, PKCs and c-raf (IC₅₀≥100µM). Blocks cell cycle in both G1 and G2 phase.

Product Specific Literature References

Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects: Y. Mettey, et al.; J. Med. Chem. 46, 222 (2003) Abstract

Further Categories Containing This Product:

GSK-3 Inhibitors • JNK [SAPK1] / Related Products • Cell Cycle Blockers & Inhibitors / Related Products

ALX-380-051

Revised 20-Jun-08

Anisomycin
SYNONYMS	2-(p-Methoxybenzyl)-3,4-pyrrolidinediol-3-acetate
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Other Signal Transduction Pathway Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-051-M010		10 mg	35.00 USD
ALX-380-051-M050		50 mg	140.00 USD
ALX-380-051-M100		100 mg	250.00 USD

Product Specification

FORMULA:	C₁₄H₁₉NO₄
MW:	265.3
CAS NUMBER:	22862-76-6
MERCK INDEX:	14: 670
RTECS:	BZ9800000
SOURCE/HOST:	Isolated from Streptomyces griseolus.
PURITY:	≥98% (HPLC)
APPEARANCE:	White crystalline solid.
SOLUBILITY:	Soluble in DMSO (25mg/ml), 100% ethanol, methanol or ethyl acetate (10mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	TOXIC.

Product Description

Antibiotic. Activator of p38 and MAP kinases. Synergistic with growth factors and phorbol esters to superinduce cFos and cJun, by acting as a potent signalling agonist. Induces apoptosis in the human monoblastoid cell line. Used in the eradication of bean mildew. Inhibits other pathogenic fungi in plants.

Product Specific Literature References

Anisomycin, a new anti-protozoan antibiotic: B. A. Sobin & F. W. Tanner; J. Am. Chem. Soc. 76, 4053 (1954)
DNA fragmentation and cytolysis in U937 cells treated with diphtheria toxin or other inhibitors of protein synthesis: S.K. Kochi & R.J. Collier; Exp. Cell. Res. 208, 296 (1993) Abstract
The stress-activated protein kinase subfamily of c-Jun kinases: J.M. Kyriakis, et al.; Nature 369, 156 (1994) Abstract
Role of SAPK/ERK kinase-1 in the stress-activated pathway regulating transcription factor c-Jun: I. Sanchez, et al.; Nature 372, 794 (1994) Abstract
Anisomycin and rapamycin define an area upstream of p70/85S6k containing a bifurcation to histone H3-HMG-like protein phosphorylation and c-fos-c-jun induction: E. Kardalinou, et al.; Mol. Cell. Biol. 14, 1066 (1994) Abstract
Protein synthesis inhibitor phase shifts vasopressin rhythms in long- term suprachiasmatic cultures: K. Shinohara & T. Oka; NeuroReport 5, 2201 (1994) Abstract
Anisomycin selectively desensitizes signalling components involved in stress kinase activation and fos and jun induction: C.A. Hazzalin, et al.; Mol Cell Biol 18, 1844 (1998) Abstract
Anisomycin treatment paradigm affects duration of long-term potentiation in slices of the amygdala: P. Okulski, et al.; Neuroscience 114, 1 (2002) Abstract
Downregulation of Ski and SnoN co-repressors by anisomycin: A. Vazquez-Macias, et al.; FEBS Lett. 579, 3701 (2005) Abstract
Anisomycin and the reconsolidation hypothesis: J.W. Rudy, et al.; Learn. Mem. 13, 1 (2006), Review Abstract
A chemical screen identifies anisomycin as an anoikis sensitizer that functions by decreasing FLIP protein synthesis: I.A. Mawji, et al.; Cancer Res. 67, 8307 (2007) Abstract
Anisomycin abrogates repression of protooncogene c-fos transcription in E1A + cHa-ras-transformed cells through activation of MEK/ERK kinase cascade: A. N. Kukushkin, et al.; J. Cell. Biochem. 103, 1005 (2008) Abstract

Further Categories Containing This Product:

MAPK Pathway Activators • Antibiotics - Apoptosis Inducers & Inhibitors • JNK [SAPK1] / Related Products

ALX-270-443

Revised 05-May-08

AS601245
SYNONYMS	1,3-Benzothiazol-2-yl-(2-{[2-(3-pyridinyl)ethyl]amino}-4-pyrimidinyl) acetonitrile JNK Inhibitor V
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	JNK [SAPK1] / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-443-M001		1 mg	50.00 USD
ALX-270-443-M005		5 mg	150.00 USD
ALX-270-443-M025		25 mg	520.00 USD

Product Specification

FORMULA:	C₂₀H₁₆N₆S
MW:	372.5
CAS NUMBER:	345987-15-7
PURITY:	≥95% (HPLC)
APPEARANCE:	White to yellow solid.
PURITY DETAIL:	Sum of two isomers.
SOLUBILITY:	Soluble in DMSO (10mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:	Hygroscopic. Packaged under inert gas. Protect from light.
HAZARD:	HARMFUL.
IDENTITY:	Identity determined by ¹H-NMR.

Product Description

Potent and cell permeable ATP competitive JNK inhibitor (hJNK1: IC₅₀=150nM, hJNK2: IC₅₀=220nM and hJNK3: IC₅₀=70 nM). Displays anti-inflammatory properties and has been shown to reduce TNF-α plasma levels induced by LPS in mice.

Product Specific Literature References

AS601245 (1,3-benzothiazol-2-yl (2-[[2-(3-pyridinyl) ethyl] amino]-4 pyrimidinyl) acetonitrile): a c-Jun NH2-terminal protein kinase inhibitor with neuroprotective properties: S. Carboni, et al.; J. Pharmacol. Exp. Ther. 310, 25 (2004) Abstract; Full Text
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase: P. Gaillard, et al.; J. Med. Chem. 48, 4596 (2005) Abstract

Further Categories Containing This Product:

TNF-alpha & TNF Receptors Other Products • Anti-inflammatory Agents Other Products

ALX-270-263

Revised 03-Apr-08

(-)-Epigallocatechin gallate
SYNONYMS	EGCG (2R,3R)-2-(3,4,5-Trihydroxyphenyl)-3,4-dihydro-1[2H]-benzopyran-3,5,7-triol 3-(3,4,5-trihydroxybenzoate)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Antioxidants

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-263-M010		10 mg	20.00 USD
ALX-270-263-M050		50 mg	60.00 USD

Product Specification

FORMULA:	C₂₂H₁₈O₁₁
MW:	458.4
CAS NUMBER:	989-51-5
MERCK INDEX:	14: 3526
SOURCE/HOST:	Isolated from green tea.
PURITY:	≥98% (HPLC)
APPEARANCE:	Off-white to yellow powder.
SOLUBILITY:	Soluble in 100% ethanol, dimethyl formamide or DMSO; slightly soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
USE/STABILITY:	Stock solutions in DMSO are stable for up to 3 months when stored at -20°C.
HANDLING:	After reconstitution, prepare aliquots and store at -20°C. Keep under inert gas. Protect from light.

Product Description

Antitumor reagent. Antioxidant. Protects cells from lipid peroxidation and DNA damage induced by reactive free radicals. Inhibits inducible nitric oxide synthase (iNOS; NOS II). Chemopreventive anticancer agent. Induces apoptosis in human cancer cell lines. Inhibits MAP kinase mediated signalling pathways. Inhibits angiogenesis. Inhibits telomerase and DNA methyltransferase. Anti-inflammatory agent.

Product Specific Literature References

Inhibitory effect of topical application of a green tea polyphenol fraction on tumor initiation and promotion in mouse skin: M.T. Huang, et al.; Carcinogenesis 13, 947 (1992) Abstract
Inhibition of 12-O-tetradecanoylphorbol-13-acetate and other skin tumor-promoter-caused induction of epidermal interleukin-1 alpha mRNA and protein expression in SENCAR mice by green tea polyphenols: S.K. Katiyar, et al.; J. Invest. Dermatol. 105, 394 (1995) Abstract
Growth inhibition and regression of human prostate and breast tumors in athymic mice by tea epigallocatechin gallate: S. Liao, et al.; Cancer Lett. 96, 239 (1995) Abstract
Inhibition of N-methyl-N'-nitro-N-nitrosoguanidine-induced carcinogenesis by (-)-epigallocatechin gallate in the rat glandular stomach: T. Yamane, et al.; Cancer Res. 55, 2081 (1995) Abstract
(-)-Epigallocatechin gallate, a polyphenolic tea antioxidant, inhibits peroxynitrite-mediated formation of 8-oxodeoxyguanosine and 3-nitrotyrosine: E.S. Fiala, et al.; Experientia 52, 922 (1996) Abstract
Green tea constituent epigallocatechin-3-gallate and induction of apoptosis and cell cycle arrest in human carcinoma cells: N. Ahmad, et al.; J. Natl. Cancer Inst. 89, 1881 (1997) Abstract
Inhibition of inducible nitric oxide synthase gene expression and enzyme activity by epigallocatechin gallate, a natural product from green tea: M.M. Chan, et al.; Biochem. Pharmacol. 54, 1281 (1997) Abstract
(-)-Epigallocatechin-3-gallate blocks the induction of nitric oxide synthase by down-regulating lipopolysaccharide-induced activity of transcription factor nuclear factor-kappaB: Y.L. Lin & J.K. Lin; Mol. Pharmacol. 52, 465 (1997) Abstract
Telomerase inhibition, telomere shortening, and senescence of cancer cells by tea catechins: I. Naasani, et al.; BBRC 249, 391 (1998) Abstract
Epigallocatechin suppression of proliferation of vascular smooth muscle cells: correlation with c-jun and JNK: L.H. Lu, et al.; Br. J. Pharmacol. 124, 1227 (1998) Abstract
ESR study on the structure-antioxidant activity relationship of tea catechins and their epimers: Q. Guo, et al.; Biochim. Biophys. Acta 1427, 13 (1999) Abstract
Pharmacokinetics of the green tea derivative, EGCG, by the topical route of administration in mouse and human skin: K. Dvorakova, et al.; Cancer Chemother. Pharmacol. 43, 331 (1999) Abstract
Polyphenolic antioxidant (-)-epigallocatechin-3-gallate from green tea reduces UVB-induced inflammatory responses and infiltration of leukocytes in human skin: S.K. Katiyar, et al.; Photochem. Photobiol. 69, 148 (1999) Abstract
Antioxidant chemistry of green tea catechins. Identification of products of the reaction of (-)-epigallocatechin gallate with peroxyl radicals: S. Valcic, et al.; Chem. Res. Toxicol. 12, 382 (1999) Abstract
Antimutagenic and anticarcinogenic activity of tea polyphenols: Y. Kuroda & Y. Hara; Mutat. Res. 436, 69 (1999) Abstract
Inhibitory effect of green and black tea on tumor growth: A.H. Conney, et al.; Proc. Soc. Exp. Biol. Med. 220, 229 (1999) Abstract
Green tea epigallocatechin gallate: a natural inhibitor of fatty-acid synthase: X. Wang & W. Tian; BBRC 288, 1200 (2001) Abstract
Epigallocatechin gallate, a constituent of green tea, represses hepatic glucose production: M.E. Waltner-Law, et al.; J. Biol. Chem. 277, 34933 (2002) Abstract; Full Text
The specificities of protein kinase inhibitors: an update:: J. Bain, et al.; Biochem. J. 371, 199 (2003) Abstract; Full Text
Selective inhibition of ADAMTS-1, -4 and -5 by catechin gallate esters: M.N. Vankemmelbeke, et al.; Eur. J. Biochem. 270, 2394 (2003) Abstract
Epigallocatechin-3-gallate, constituent of green tea, suppresses the LPS-induced phenotypic and functional maturation of murine dendritic cells through inhibition of mitogen-activated protein kinases and NF-kappaB: S.C. Ahn, et al.; BBRC 313, 148 (2004) Abstract
Epigallocatechin-3-gallate inhibits epidermal growth factor receptor signaling pathway. Evidence for direct inhibition of ERK1/2 and AKT kinases: J.F. Sah, et al.; J. Biol. Chem. 279, 12755 (2004) Abstract
Inhibition of c-Jun NH2-terminal kinase activity improves ischemia/reperfusion injury in rat lungs: M. Ishii, et al.; J. Immunol. 172, 2569 (2004) Abstract
A constituent of green tea, epigallocatechin-3-gallate, activates endothelial nitric oxide synthase by a phosphatidylinositol-3-OH-kinase-, cAMP-dependent protein kinase-, and Akt-dependent pathway and leads to endothelial-dependent vasorelaxation: M. Lorenz, et al.; J. Biol. Chem. 279, 6190 (2004) Abstract; Full Text
Green tea polyphenols prevent toxin-induced hepatotoxicity in mice by down-regulating inducible nitric oxide-derived prooxidants: J.H. Chen, et al.; Am. J. Clin. Nutr. 80, 742 (2004) Abstract; Full Text
Neuroprotective effects of (-)-epigallocatechin gallate following hypoxia-ischemia-induced brain damage: novel mechanisms of action: B.A. Sutherland, et al.; FASEB J. 19, 258 (2005) Abstract; Full Text
Tea flavanols inhibit angiotensin-converting enzyme activity and increase nitric oxide production in human endothelial cells: I.A. Persson, et al.; J. Pharm. Pharmacol. 58, 1139 (2006) Abstract

General Literature References

Anticarcinogenic effects of (-)-epigallocatechin gallate: H. Fujiki, et al.; Prev. Med. 21, 503 (1992), (Review) Abstract
Absorption, metabolism and antioxidative effects of tea catechin in humans: T. Miyazawa; Biofactors 13, 55 (2000), (Review) Abstract
Inhibition of tumour invasion and angiogenesis by epigallocatechin gallate (EGCG), a major component of green tea: Y.D. Jung and L.M. Ellis; Int. J. Exp. Pathol. 82, 309 (2001), (Review) Abstract
Anti-invasive effects of green tea polyphenol epigallocatechin-3-gallate (EGCG), a natural inhibitor of metallo and serine proteases: R. Benelli, et al.; Biol. Chem. 383, 101 (2002), (Review) Abstract

Further Categories Containing This Product:

Flavanols • NOS Inhibitors (NOS Induction & Enzyme Activity) • MAPK Pathway Inhibitors • Akt [PKB] / Related Products • EGFR Kinase Inhibitors • PKC Inhibitors • Telomerase / Related Products • Natural Products - Chemopreventive Agents • Fatty Acid Synthase [FAS] / Related Products • JNK [SAPK1] / Related Products • Active Substances from Fruit and Vegetables • Antitumor Agents (DNA Interaction & Gene Regulation) • Natural Products - Anti-inflammatory Agents • Natural Products for Angiogenesis Research • Natural Products - Nitric Oxide Pathway Modulators • Natural Products - Protein Kinase Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents • Antitumor Agents (Apoptosis Inducers) • Antitumor Agents (Enzyme Inhibitors)

ALX-159-600

Revised 14-Jul-08

JNK Inhibitor 1 (L-stereoisomer)
SYNONYMS	L-JNKI1 c-Jun N-terminal Kinase Peptide Inhibitor 1, L-stereoisomer
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	JNK [SAPK1] / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-159-600-R100		100 µl	125.00 USD
ALX-159-600-R200		200 µl	225.00 USD

Product Specification

SEQUENCE:	GRKKRRQRRR-PP-RPKRPTTLNLFPQVPRSQD-amide
FORMULA:	C₁₆₄H₂₈₆N₆₆O₄₀
MW:	3822.5
CONCENTRATION:	1mM
PURITY:	≥97% (HPLC)
FORMULATION:	Liquid. Sterile, ready-to-use solution in PBS.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
HANDLING:	After opening, prepare aliquots and store at -20°C. Avoid freeze/thaw cycles. Keep on ice at all times.
POSITIVE CONTROL:	Prod. No. ALX-168-009/1

Product Images

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Product Description

Cell permeable JNK (c-Jun N-terminal kinase) inhibitor. For increased cell permeability the peptide was covalently linked to the 10 aa recognized by the TAT transporter. Neuroprotective agent for stroke.

Product Specific Literature References

[1] Cell-permeable peptide inhibitors of JNK: novel blockers of beta-cell death: C. Bonny, et al.; Diabetes 50, 77 (2001) Abstract; Full Text
Hyperosmolarity and CD95L trigger CD95/EGF receptor association and tyrosine phosphorylation of CD95 as prerequisites for CD95 membrane trafficking and DISC formation: R. Reinehr, et al.; FASEB J. 17, 731 (2003) Abstract
Translation inhibitors sensitize prostate cancer cells to TRAIL-induced apoptosis by activating c-Jun N-terminal kinase: N.K. Sah, et al.; J. Biol. Chem. 278, 20593 (2003) Abstract; Full Text
A peptide inhibitor of c-Jun N-terminal kinase protects against excitotoxicity and cerebral ischemia: T. Borsello, et al.; Nat. Med. 9, 1180 (2003) Abstract
Activation of JNK in sensory neurons protects against sensory neuron cell death in diabetes and on exposure to glucose/oxidative stress in vitro: S.A. Price, et al.; Ann. NY Acad. Sci. 1010, 95 (2003)
Insulin-secreting beta-cell dysfunction induced by human lipoproteins: M.E. Roehrich, et al.; J. Biol. Chem. 278, 18368 (2003) Abstract; Full Text
Inhibition of c-Jun NH2-terminal kinase activity improves ischemia/reperfusion injury in rat lungs: M. Ishii, et al.; J. Immunol. 172, 2569 (2004) Abstract

General Information

BACKGROUND/TECHNICAL INFORMATION

A protein inhibitor named IB1 has been described that competitively blocks the interaction between JNK and c-Jun, thereby inhibiting the signalling events downstream of JNK [2,3] like c-Jun, ATF2 and ELK1 phosphorylation. To convert IB1 into cell-permeable inhibitors of JNK (JNKI peptides) the minimal 20 aa inhibitory sequence of IB1 was covalently linked to the 10 amino acids recognized by TAT transporter [4].
The L-JNKI1 and the protease resistant D-JNKI1 peptides represent the only potent inhibitors that are specific for JNK (JNK1, JNK2 and JNK3). Different from chemical inhibitors that directly affect kinase activity e.g. by competing with the ATP-binding site of the protein kinase, JNKI1 rather inhibits the interaction between JNK and its substrate, resulting in a JNK K.O. phenotype. In contrast to pure diffusion the TAT-peptides are actively transported into cells, where they remain until their proteolytic degradation. They can be used for in vitro as well as for in vivo applications (IC50~1µM).
D-JNKI1 is the only form found to be active on neuronal cells, probably due to a high level of proteolytic degradation of the L-stereoisomer (T. Borsello and C. Bonny; unpublished data). As these peptides tend to be toxic in neurons above concentrations of 5µM, it is recommended to use concentrations of ~1µM or less. When interpreting results of c-Jun inhibition, one should also note that a number of other c-Jun kinases are thought to contribute to c-Jun phosphorylation (C. Bonny, personal communication).

*For in vivo applications in mice it is suggested to start with 30-50µl of a 1mM stock solution administered intraperitoneally. Cellular uptake of L-JNKI1 peptides can now be confirmed using the FITC-conjugated L-TAT control peptide (Prod. No. ALX-168-009F).
Note: L-TAT control peptides should only be used with L-JNKI1.

General Literature References

[2] IB1, a JIP-1-related nuclear protein present in insulin-secreting cells: C. Bonny, et al.; J. Biol. Chem. 273, 1843 (1998) Abstract; Full Text
[3] A cytoplasmic inhibitor of the JNK signal transduction pathway: M. Dickens, et al.; Science 277, 693 (1997) Abstract
[4] In vivo protein transduction: delivery of a biologically active protein into the mouse: S.R. Schwarze, et al.; Science 285, 1569 (1999) Abstract

ALX-159-600	JNK Inhibitor 1 (L-stereoisomer)
ALX-152-028	Bax (58-75) (human) (cell permeable)
ALX-163-011	NBD Peptide / NF-κB Blocker (cell permeable)
ALX-152-027	Bim_L (147-164) (human) (cell permeable)
ALX-152-029	Bok (66-83) (human) (cell permeable)

FORMULA:	C₁₉H₂₂O₇
MW:	362.4
CAS NUMBER:	66018-38-0
SOURCE/HOST:	Isolated from Deuteromycetes sp.
PURITY:	≥95% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in methanol, chloroform, acetone, DMSO or ethil acetate; insoluble in ethanol and n-hexane.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

SEQUENCE:	FITC-β-A-RKKRRQRRRA-amide
FORMULA:	C₈₀H₁₂₈N₃₄O₁₇S
MW:	1870.2
CONCENTRATION:	1mM
PURITY:	≥90% (HPLC)
FORMULATION:	Liquid. In sterile PBS.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
HANDLING:	Avoid freeze/thaw cycles. After opening, prepare aliquots and store at -20°C. Keep on ice at all times.