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ALX-270-448

Revised 24-Jul-06

ALK5 Inhibitor I
SYNONYMS	TGF-β RI Kinase Inhibitor I 3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole
PRODUCT LINE	Chemokines & Cytokines
PRODUCT CATEGORY	Transforming Growth Factor beta [TGFbeta] & Receptors / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-448-M001		1 mg	30.00 USD
ALX-270-448-M005		5 mg	90.00 USD

Product Specification

FORMULA:	C₁₇H₁₂N₄
MW:	272.3
PURITY:	≥97% (¹H-NMR)
APPEARANCE:	Yellow to brown solid.
SOLUBILITY:	Soluble in DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stable for 2 years after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:	Protect from light.
HAZARD:	MAY BE CARCINOGENIC. HARMFUL.

Product Description

Cell permeable, potent, selective and ATP-competitive inhibitor of TGF-β RI kinase (IC₅₀=51nM). Displays ~15-fold greater selectivity over p38α MAPK (IC₅₀=740nM). Inhibits TGF-β-dependent cellular growth (IC₅₀=89nM in NIH 3T3 mouse fibroblasts) and transcription activation (IC₅₀=47nM in mink lung cells).

Product Specific Literature References

Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain: J.S. Sawyer, et al.; J. Med. Chem. 46, 3953 (2003) Abstract
Successful shape-based virtual screening: the discovery of a potent inhibitor of the type I TGFbeta receptor kinase (TbetaRI): J. Singh, et al.; Bioorg. Med. Chem. Lett. 13, 4355 (2003) Abstract

Further Categories Containing This Product:

MAPK Pathway Inhibitors

ALX-270-445

Revised 20-Jul-06

ALK5 Inhibitor II
SYNONYMS	TGF-β RI Kinase Inhibitor II 2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine
PRODUCT LINE	Chemokines & Cytokines
PRODUCT CATEGORY	Transforming Growth Factor beta [TGFbeta] & Receptors / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-445-M001		1 mg	60.00 USD
ALX-270-445-M005		5 mg	240.00 USD

Product Specification

FORMULA:	C₁₇H₁₃N₅
MW:	287.3
PURITY:	≥97% (¹H-NMR)
APPEARANCE:	Yellow solid.
SOLUBILITY:	5mg/ml soluble in DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stable for 2 years after receipt when stored at -20°C. Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING:	Protect from light.

Product Description

Cell permeable, potent, selective and ATP-competitive inhibitor of TGF-β RI kinase (IC₅₀=23nM, 4nM and 18nM for binding, auto-phosphorylation and cellular assay in HepG2 cells of TGF-β RI kinase, respectively). Minimally affects a panel of 9 closely related kinases including p38 MAPK (IC₅₀>16µM).

Product Specific Literature References

Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors: F. Gellibert, et al.; J. Med. Chem. 47, 4494 (2004) Abstract

Further Categories Containing This Product:

MAPK Pathway Inhibitors

ALX-385-008

Revised 13-Mar-08

Apigenin
SYNONYMS	4',5,7-Trihydroxyflavone
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Flavones

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-385-008-M010		10 mg	35.00 USD
ALX-385-008-M050		50 mg	105.00 USD

Product Specification

FORMULA:	C₁₅H₁₀O₅
MW:	270.2
CAS NUMBER:	520-36-5
MERCK INDEX:	14: 730
SOURCE/HOST:	Synthetic.
PURITY:	≥90% (HPLC)
APPEARANCE:	Light yellow to slightly brown powder.
SOLUBILITY:	Soluble in diluted potassium hydroxide or DMSO; slightly soluble in 100% ethanol (hot). Insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	IRRITANT.

Product Description

Antioxidant flavonoid. Has chemopreventive and antitumor properties. Induces apoptosis. Inhibits the proliferation of malignant tumor cells by G2/M arrest. MAP kinase (MAPK/ERK) inhibitor. Inhibits hypoxia-inducible factor-1 (HIF-1) and vascular endothelial growth factor (VEGF) expression.

Product Specific Literature References

Apigenin and tangeretin enhance gap junctional intercellular communication in rat liver epithelial cells: C. Chaumontet, et al.; Carcinogenesis 15, 2325 (1994) Abstract
Apigenin induces morphological differentiation and G2-M arrest in rat neuronal cells: F. Sato, et al.; BBRC 204, 578 (1994) Abstract
Reversion of v-H-ras-transformed NIH 3T3 cells by apigenin through inhibiting mitogen activated protein kinase and its downstream oncogenes: M.L. Kuo and N.C. Yang; BBRC 212, 767 (1995) Abstract
Structure-antioxidant activity relationships of flavonoids and phenolic acids: C.A. Rice-Evans, et al.; Free Radical Biol. & Med. 20, 933 (1996), (Review) Abstract
Apigenin inhibits endothelial-cell proliferation in G(2)/M phase whereas it stimulates smooth-muscle cells by inhibiting P21 and P27 expression: V. Trochon, et al.; Int. J. Cancer 85, 691 (2000) Abstract
Induction of caspase-dependent, p53-mediated apoptosis by apigenin in human neuroblastoma: R. Torkin, et al.; Mol. Cancer Ther. 4, 1 (2005) Abstract
Apigenin and cancer chemoprevention: progress, potential and promise: D. Patel, et al.; Int. J. Oncol. 30, 233 (2007), (Review) Abstract
Apigenin inhibits tumor angiogenesis through decreasing HIF-1alpha and VEGF expression: J. Fang, et al.; Carcinogenesis 28, 858 (2007) Abstract
Apigenin-induced cell cycle arrest is mediated by modulation of MAPK, PI3K-Akt, and loss of cyclin D1 associated retinoblastoma dephosphorylation in human prostate cancer cells: S. Shukla & S. Gupta; Cell Cycle 6, 1102 (2007) Abstract
Apigenin blocks lipopolysaccharide-induced lethality in vivo and proinflammatory cytokines expression by inactivating NF-kappaB through the suppression of p65 phosphorylation: C. Nicholas, et al.; J. Immunol. 179, 7121 (2007) Abstract

Further Categories Containing This Product:

MAPK Pathway Inhibitors • Antitumor Agents (Anti-proliferative) • Antitumor Agents (Enzyme Inhibitors) • Natural Products - Protein Kinase Inhibitors • Hypoxia-inducible Factor [HIF] / Related Products • VEGFs & VEGF-Rs Other Products • Natural Products for Angiogenesis Research • Natural Products - Chemopreventive Agents • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents • Natural Products - Antioxidants

ALX-270-328

Revised 04-Mar-05

2-(4-Chlorophenyl)-4-(fluorophenyl)-5-pyridin-4-yl-1,2-dihydropyrazol-3-one
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	MAPK Pathway Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-328-C500		500 µg	135.00 USD

Product Specification

FORMULA:	C₂₀H₁₃ClFN₃O
MW:	365.8
PURITY:	≥98%
APPEARANCE:	Off-white to orange brown powder.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light. Keep under inert gas.

Product Description

Potent p38 (SAPK2a) inhibitor (IC₅₀=35nM).

Product Specific Literature References

Pyrroles and other heterocycles as inhibitors of p38 kinase: S.E. de Laszlo, et al.; Bioorg. Med. Chem. Lett. 8, 2689 (1998) Abstract

ALX-350-290

Revised 19-Oct-07

Debromohymenialdisine
SYNONYMS	DBH 4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-290-C100		100 µg	90.00 USD

Product Specification

FORMULA:	C₁₁H₁₁N₅O₂
MW:	245.2
CAS NUMBER:	125118-55-0
SOURCE/HOST:	Isolated from sponge Stylotella aurantium.
PURITY:	≥95%
APPEARANCE:	Yellow solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light. Keep under inert gas.

Product Description

Inhibitor of G2 DNA damage checkpoint (IC₅₀=8µM) and check point kinases 1 (Chk1) (IC₅₀=3µM) and 2 (Chk2) (IC₅₀=3.5µM) [1,3]. Unlike other checkpoint inhibitors DBH does not inhibit ataxia-telangiectasia mutated (ATM) or ATM-Rad3-related protein. Also inhibits MAP kinase kinase 1 (MEK-1) (IC₅₀=881nM) but is not as potent as 10Z-hymenialdisine (Prod. No. ALX-350-289) (IC₅₀=6nM) [2].

Product Specific Literature References

[1] Inhibition of the G2 DNA damage checkpoint and of protein kinases Chk1 and Chk2 by the marine sponge alkaloid debromohymenialdisine: D. Curman, et al.; J. Biol. Chem. 276, 17914 (2001) Abstract; Full Text
[2] Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1): D. Tasdemir, et al.; J. Med. Chem. 45, 529 (2002) Abstract
[3] G2 checkpoint abrogators as anticancer drugs: T. Kawabe; Mol. Cancer Ther. 3, 513 (2004) Abstract

Further Categories Containing This Product:

MAPK Pathway Inhibitors • Chk1 & Chk2 / Related Products • Natural Products for Cell Cycle Research • Alkaloids

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 • Antitumor Agents (Enzyme 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 • Natural Products - Protein Kinase Inhibitors • Active Substances from Fruit and Vegetables • Antitumor Agents (DNA Interaction & Gene Regulation) • Antitumor Agents (Apoptosis Inducers) • Natural Products - Anti-inflammatory Agents • Natural Products - Antitumor Reagents • Natural Products - Nitric Oxide Pathway Modulators • Natural Products for Angiogenesis Research • Natural Products - Apoptosis Inducers & Inhibitors

ALX-350-289

Revised 05-Apr-08

10Z-Hymenialdisine
SYNONYMS	4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-289-C500		500 µg	190.00 USD

Product Specification

FORMULA:	C₁₁H₁₀BrN₅O₂
MW:	324.1
CAS NUMBER:	82005-12-7
SOURCE/HOST:	Isolated from sponge Axinella damicornis (Stylissa damicornis).
PURITY:	≥97%
APPEARANCE:	Yellow needles.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
HAZARD:	TOXIC.

Product Description

Originally isolated from the sponges Axinella verrucosa and Acantella aurantiaca. Potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC₅₀=6nM). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-β (GSK-3β) and CDK5/p35 in Alzheimer’s disease. Inhibitor of DNA damage checkpoint at G2 phase (IC₅₀=6µM), cyclin-dependent kinases CDK1/cyclin B (IC₅₀=22nM), CDK2/cyclin A (IC₅₀=70nM), CDK2/cyclin E (IC₅₀=40nM), CDK4/cyclin D1 (IC₅₀=600nM), CDK5/p25 (IC₅₀=28nM), GSK-3β (IC₅₀=10nM), and casein kinase 1 (CK1) (IC₅₀=35nM). Inhibitor of NF-κB activation and of various pro-inflammatory cytokines such as IL-1, IL-2 (IC₅₀=2.4µM), IL-6, IL-8, TNF-α (IC₅₀=1.4µM) and nitric oxide (NO) (IC₅₀=0.8µM) in a variety of cell lines.

Product Specific Literature References

Isolation and x-ray crystal structure of a novel bromo-compound from two marine sponges: G. Cimino, et al.; Tetrahedron Lett. 23, 767 (1982)
Bioactive alkaloids from the tropical marine sponge Axinella carteri: A. Supriyono, et al.; Z. Naturforsch. [C] 50, 669 (1995) Abstract
The natural product hymenialdisine inhibits interleukin-8 production in U937 cells by inhibition of nuclear factor-kappaB: J.J. Breton & M.C. Chabot-Fletcher; J. Pharmacol. Exp. Ther. 282, 459 (1997) Abstract; Full Text
Inhibition of NFkappaB-mediated interleukin-1beta-stimulated prostaglandin E2 formation by the marine natural product hymenialdisine: A. Roshak, et al.; J. Pharmacol. Exp. Ther. 283, 955 (1997) Abstract; Full Text
Inhibition of interleukin-1-induced proteoglycan degradation and nitric oxide production in bovine articular cartilage/chondrocyte cultures by the natural product, hymenialdisine: A.M. Badger, et al.; J. Pharmacol. Exp. Ther. 290, 587 (1999) Abstract; Full Text
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent: L. Meijer, et al.; Chem. Biol. 7, 51 (2000) Abstract
Inhibition of the G2 DNA damage checkpoint and of protein kinases Chk1 and Chk2 by the marine sponge alkaloid debromohymenialdisine: D. Curman, et al.; J. Biol. Chem. 276, 17914 (2001) Abstract; Full Text
An investigation of cell proliferation and soluble mediators induced by interleukin 1beta in human synovial fibroblasts: comparative response in osteoarthritis and rheumatoid arthritis: H. Inoue, et al.; Inflamm. Res. 50, 65 (2001) Abstract
Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1): D. Tasdemir, et al.; J. Med. Chem. 45, 529 (2002) Abstract
Inhibition of cytokine production by hymenialdisine derivatives: V. Sharma, et al.; J. Med. Chem. 47, 3700 (2004) Abstract

Further Categories Containing This Product:

CDK & Cyclin Inhibitors • MAPK Pathway Inhibitors • Natural Products - NF-kB Pathway Inhibitors • Natural Products for Cell Cycle Research • Natural Products - Nitric Oxide Pathway Modulators • NF-kB Pathway Inhibitors • DNA Damage Checkpoint Other Products • Alkaloids • GSK-3 Inhibitors

ALX-350-030

Revised 07-Apr-08

Hypericin (native)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-030-M001		1 mg	50.00 USD
ALX-350-030-M005		5 mg	200.00 USD
ALX-350-030-M010		10 mg	370.00 USD

Product Specification

FORMULA:	C₃₀H₁₆O₈
MW:	504.4
CAS NUMBER:	548-04-9
MERCK INDEX:	14: 4863
SOURCE/HOST:	Isolated from Hypericum perforatum.
PURITY:	≥98%
APPEARANCE:	Black to black-red powder.
SOLUBILITY:	Soluble in DMSO, 100% ethanol, methanol, acetone, ethylmethylketone, pyridine or other organic solvents and bases.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.
HAZARD:	MAY BE TERATOGENIC. HARMFUL. MAY BE MUTAGENIC.

Product Description

Inhibitor of protein kinase C (PKC). Shows anti-viral and anti-retroviral activity. Displays antineoplastic and antitumor activities. Inhibits casein kinase II (CKII) and MAP kinase. Bright red fluorescence emission and photostability. Antidepressant.

Product Specific Literature References

Therapeutic agents with dramatic antiretroviral activity and little toxicity at effective doses: aromatic polycyclic diones hypericin and pseudohypericin: D. Meruelo, et al.; PNAS 85, 5230 (1988) Abstract
Hypericin and pseudohypericin specifically inhibit protein kinase C: possible relation to their antiretroviral activity: I. Takahashi, et al.; BBRC 165, 1207 (1989) Abstract
Evaluation of the antiviral activity of anthraquinones, anthrones and anthraquinone derivatives against human cytomegalovirus: D.L. Barnard, et al.; Antiviral Res. 17, 63 (1992) Abstract
Photosensitized inhibition of growth factor-regulated protein kinases by hypericin: P. Agostinis, et al.; Biochem. Pharmacol. 49, 1615 (1995) Abstract
Growth inhibition and apoptosis in human neuroblastoma SK-N-SH cells induced by hypericin, a potent inhibitor of protein kinase C: W. Zhang, et al.; Cancer Lett. 96, 31 (1995)