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MAP Kinase Pathways
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ALX-270-263 Revised 03-Apr-08
(-)-Epigallocatechin gallate
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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
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-263-M010   10 mg 20.00 USD Add To Cart
ALX-270-263-M050   50 mg 60.00 USD Add To Cart
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
 
 
ALX-270-339 Revised 04-Mar-05
SP600125
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SYNONYMS Anthra(1,9-cd)pyrazol-6(2H)-one
1,9-Pyrazoloanthrone
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY JNK [SAPK1] / Related Products
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ALX-270-339-M005   5 mg 52.00 USD Add To Cart
ALX-270-339-M025   25 mg 190.00 USD Add To Cart
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Product Specification
FORMULA: C14H8N2O
MW: 220.2
CAS NUMBER: 129-56-6
RTECS: CB4585000
PURITY: ≥98%
APPEARANCE: Yellow to brown solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Protect from light.

Product Description
Potent, cell permeable, selective, and reversible inhibitor of c-Jun N-terminal kinase (JNK) (IC50=40nM for JNK-1 and JNK-2 and 90nM for JNK-3). The inhibition is competitive with respect to ATP. Exhibits over 300-fold greater selectivity for JNK as compared to ERK1 and p38. Inhibits the phosphorylation of c-Jun and blocks the expression of IL-2, IFN-γ, TNF-α, and COX-2. Blocks IL-1-induced accumulation of phospho-Jun and induction of c-Jun transcription.
Product Specific Literature References
SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase: B.L. Bennett, et al.; PNAS 98, 13681 (2001) Abstract; Full Text
Role of JNK in hypertonic activation of Cl(-)-dependent Na(+)/H(+) exchange in Xenopus oocytes: G.G. Goss, et al.; Am. J. Physiol. Cell. Physiol. 281, C1978 (2001) Abstract
c-Jun N-terminal kinase is required for metalloproteinase expression and joint destruction in inflammatory arthritis: Z. Han, et al.; J. Clin. Invest. 108, 73 (2001) Abstract; Full Text
TAK1/JNK and p38 have opposite effects on rat hepatic stellate cells: B. Schnabl, et al.; Hepatology 34, 953 (2001) Abstract
An inhibitor of c-jun aminoterminal kinase (SP600125) represses c-Jun activation, DNA-binding and PMA-inducible 92-kDa type IV collagenase expression: M. Shin, et al.; Biochim. Biophys. Acta 1589, 311 (2002) 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
 
 
ALX-270-385 Revised 17-Jul-07
Aloisine A
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SYNONYMS RP107
7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-385-M001   1 mg 30.00 USD Add To Cart
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
 
 
ALX-270-443 Revised 05-May-08
AS601245
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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
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-443-M001   1 mg 50.00 USD Add To Cart
ALX-270-443-M005   5 mg 150.00 USD Add To Cart
ALX-270-443-M025   25 mg 520.00 USD Add To Cart
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
 
 
ALX-270-489 Revised 28-Jul-08 New product
N-(4-Amino-5-cyano-6-ethoxypyridin-2-yl)-2-(2,5-dimethoxyphenyl)acetamide
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY JNK [SAPK1] / Related Products
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ALX-270-489-M005   5 mg 210.00 USD Add To Cart
Product Specification
FORMULA: C18H20N4O4
MW: 356.4
CAS NUMBER: 894804-07-0
PURITY: ≥95% (HPLC)
APPEARANCE: Brown solid.
SOLUBILITY: 10mg/ml soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light. After reconstitution, prepare aliquots and store at -20°C. Packaged under inert gas.

Product Description
Pyridinylamide compound. Cell permeable, ATP-competitive, reversible inhibitor of JNK1 (Ki=2nM), JNK2 (Ki=4nM) and JNK3 (Ki=52nM). Inhibits c-Jun phosphorylation (EC50=920nM) in HepG2 cells. Blocks growth of PTEN null mouse embryonic fibroblasts.
Product Specific Literature References
Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity: B.G. Szczepankiewicz, et al.; J. Med. Chem. 49, 3563 (2006) Abstract
Identification of the JNK signaling pathway as a functional target of the tumor suppressor PTEN: I. Vivanco, et al.; Cancer Cell 11, 555 (2007) Abstract
 
 
ALX-270-490 Revised 22-Jul-08 New product
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)-1-naphthylamide
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY JNK [SAPK1] / Related Products
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ALX-270-490-M005   5 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C20H16N2OS . H2O
MW: 332.4 . 18.0
CAS NUMBER: 312917-14-9
PURITY: ≥95% (HPLC)
APPEARANCE: Tan solid.
SOLUBILITY: 10mg/ml soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Protect from light. Packaged under inert gas.
HAZARD: IRRITANT.

Product Description
Thienylnaphthamide compound. Potent inhibitor of JNK2 (pIC50=6.5) and JNK3 (pIC50=6.7) targeting the ATP-binding site. Has no activity against JNK1.
Product Specific Literature References
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3: R.M. Angell, et al.; Bioorg. Med. Chem. Lett. 17, 1296 (2007) Abstract
 
 
ALX-380-051 Revised 20-Jun-08
Anisomycin
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SYNONYMS 2-(p-Methoxybenzyl)-3,4-pyrrolidinediol-3-acetate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Other Signal Transduction Pathway Modulators
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-051-M010   10 mg 35.00 USD Add To Cart
ALX-380-051-M050   50 mg 140.00 USD Add To Cart
ALX-380-051-M100   100 mg 250.00 USD Add To Cart
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
 
 
ALX-380-267 Revised 11-Feb-08
LL-Z1640-2
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Protein Kinase Inhibitors
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ALX-380-267-M001   1 mg 50.00 USD Add To Cart
ALX-380-267-M005   5 mg 200.00 USD Add To Cart
Product Specification
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 or ethil acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of the JNK/p38 pathways. Inhibits anisomycin-induced but not TNF-induced JNK/p38 activation. Potent protein kinase inhibitor.
Product Specific Literature References
A radicicol-related macrocyclic nonaketide compound, antibiotic LL-Z1640-2, inhibits the JNK/p38 pathways in signal-specific manner: K. Takehana, et al.; BBRC 257, 19 (1999) Abstract
Inhibition of HgCl2-induced mitogen-activated protein kinase activation by LL-Z1640-2 in CCRF-CEM cells: M. Matsuoka, et al.; Eur. J. Pharmacol. 409, 155 (2000) Abstract
Cadmium induces phosphorylation of p53 at serine 15 in MCF-7 cells: M. Matsuoka & H. Igisu; BBRC 282, 1120 (2001) Abstract
Effects of pentachlorophenol and tetrachlorohydroquinone on mitogen-activated protein kinase pathways in Jurkat T cells: B. Wispriyono, et al.; Environ. Health Perspect. 110, 139 (2002) Abstract; Full Text
Pharmacological inhibitors of MAPK pathways: J.M. English & M.H. Cobb; TIPS 23, 40 (2002), (Review) Abstract
Suppression of cadmium-induced JNK/p38 activation and HSP70 family gene expression by LL-Z1640-2 in NIH3T3 cells: N. Sugisawa, et al.; Toxicol. Appl. Pharmacol. 196, 206 (2004) Abstract
JNK (c-Jun NH2 terminal kinase) and p38 during ischemia reperfusion injury in the small intestine: T. Murayama, et al.; Transplantation 81, 1325 (2006) Abstract
Involvement of the extracellular signal-regulated protein kinase pathway in phosphorylation of p53 protein and exerting cytotoxicity in human neuroblastoma cells (SH-SY5Y) exposed to acrylamide: T. Okuno, et al.; Arch. Toxicol. 80, 146 (2006) Abstract
Protein kinases as small molecule inhibitor targets in inflammation: M. Gaestel, et al.; Curr. Med. Chem. 14, 2214 (2007), (Rev