ALEXIS Biochemicals: Rocaglamide

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ALX-350-333

Revised 05-Apr-08

Harpagoside
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Anti-inflammatory Agents

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-333-M005		5 mg	90.00 USD
ALX-350-333-M025		25 mg	360.00 USD

Product Specification

FORMULA:	C₂₄H₃₀O₁₁
MW:	494.5
CAS NUMBER:	19210-12-9
SOURCE/HOST:	Isolated from Scrophularia ningpoensis Hemsl (Figwort).
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Anti-inflammatory and anti-diabetic compound. Suppresses LPS-induced inducible nitric oxide synthase (iNOS; NOS II) and cyclooxygenase-2 (COX-2) expression through inhibition of NF-κB activation.

Product Specific Literature References

Antiinflammatory effects of different extracts and harpagoside isolated from Scrophularia frutescens: L. D. Garcia, et al.; Farmaco. 51, 443 (1996) Abstract
Physicochemical properties of harpagoside and its in vitro release from Harpagophytum procumbens extract tablets: S. Chrubasik, et al.; Phytomedicine 6, 469 (2000) Abstract
Scropolioside-D2 and harpagoside-B: two new iridoid glycosides from Scrophularia deserti and their antidiabetic and antiinflammatory activity: B. Ahmed, et al.; Biol. Pharm. Bull. 26, 462 (2003) Abstract; Full Text
Downregulation of iNOS expression in rat mesangial cells by special extracts of Harpagophytum procumbens derives from harpagoside-dependent and independent effects: M. Kaszkin, et al.; Phytomedicine 11, 585 (2004) Abstract
High anti-inflammatory activity of harpagoside-enriched extracts obtained from solvent-modified super- and subcritical carbon dioxide extractions of the roots of Harpagophytum procumbens: M. Gunther, et al.; Phytochem. Anal. 17, 1 (2006) Abstract
Harpagoside suppresses lipopolysaccharide-induced iNOS and COX-2 expression through inhibition of NF-kappa B activation: T.H. Huang, et al.; J. Ethnopharmacol. 104, 149 (2006) Abstract
Simultaneous determination of harpagoside and cinnamic acid in rat plasma by high-performance liquid chromatography: application to a pharmacokinetic study: P. Li, et al.; Anal. Bioanal. Chem. 389, 2259 (2007) Abstract

Further Categories Containing This Product:

NOS Inhibitors (NOS Induction & Enzyme Activity) • NF-kB Pathway Inhibitors • Natural Products - Nitric Oxide Pathway Modulators • COX Other Products • Natural Products - NF-kB Pathway Inhibitors

ALX-350-120

Revised 01-Apr-08

Helenalin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Anti-inflammatory Agents

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-120-MC05		0.5 mg	240.00 USD

Product Specification

FORMULA:	C₁₅H₁₈O₄
MW:	262.3
CAS NUMBER:	6754-13-8
SOURCE/HOST:	Isolated from Arnica chamissonis.
PURITY:	≥97% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO (10mg/ml) or 100% ethanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	TOXIC.
IDENTITY:	Identity determined by ¹H-NMR.

Product Description

Potent anti-inflammatory and antineoplastic agent. Induces a CD95 death receptor-independent apoptosis even when the mitochondria protecting proteins Bcl-X_Lor Bcl-2 are overexpressed. Also an inhibitor of NF-κB.

Product Specific Literature References

Helenalin, an anti-inflammatory sesquiterpene lactone from Arnica, selectively inhibits transcription factor NF-kappaB: G. Lyss, et al.; J. Biol. Chem. 378, 951 (1997) Abstract
The anti-inflammatory sesquiterpene lactone helenalin inhibits the transcription factor NF-kappaB by directly targeting p65: G. Lyss, et al; J. Biol. Chem. 273, 33508 (1998) Abstract
Constituents of Helenium species.XIII. The structure of Helenalin and Mexicanin A: W. Herz, et al.; JACS 85, 19 (1963)

Further Categories Containing This Product:

Bcl-2 Family Modulators • NF-kB Pathway Inhibitors • Natural Products - NF-kB Pathway Inhibitors • Antitumor Agents (Apoptosis Inducers) • Natural Products - Apoptosis Inducers & Inhibitors

ALX-385-011

Revised 05-Apr-08

(±)-Hesperetin
SYNONYMS	(±)-3',5,7-Trihydroxy-4'-methoxyflavanone
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Flavanones

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-385-011-G001		1 g	21.00 USD

Product Specification

FORMULA:	C₁₆H₁₄O₆
MW:	302.3
CAS NUMBER:	520-33-2
MERCK INDEX:	14: 4670
PURITY:	≥95% (HPLC)
APPEARANCE:	Off-white to yellow powder.
SOLUBILITY:	Soluble in 100% ethanol; slightly soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C

Product Description

Antioxidant flavonoid. Induces G1-phase cell cycle arrest. Anti-inflammatory. Suppresses NF-κB activation. Reduces cholesterol biosynthesis. Inhibits lipid peroxidation. Neuroprotective against neuronal oxidative damage.

Product Specific Literature References

Structure-antioxidant activity relationships of flavonoids and phenolic acids: C.A. Rice-Evans, et al.; Free Radical Biol. & Med. 20, 933 (1996), (Review) Abstract
Lipid-lowering efficacy of hesperetin metabolites in high-cholesterol fed rats: H. K. Kim, et al.; Clin. Chim. Acta 327, 129 (2003) Abstract
Antioxidant and neuroprotective effects of hesperidin and its aglycone hesperetin: J. Cho; Arch. Pharm. Res. 29, 699 (2006) Abstract
Modulation of the age-related nuclear factor-kappaB (NF-kappaB) pathway by hesperetin: J. Y. Kim, et al.; Aging Cell 5, 401 (2006) Abstract
Hesperetin Induced G1-Phase Cell Cycle Arrest in Human Breast Cancer MCF-7 Cells: Involvement of CDK4 and p21: E.J. Choi; Nutr. Cancer 59, 115 (2007) Abstract

Further Categories Containing This Product:

Cell Cycle Blockers & Inhibitors / Related Products • Active Substances from Fruit and Vegetables • NF-kB Pathway Inhibitors • Natural Products - Antioxidants • Natural Products - Anti-inflammatory Agents • Natural Products - NF-kB Pathway 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-350-245

Revised 07-Apr-08

Lactacystin (native)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Proteasome / Ubiquitin Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-245-MC01		0.1 mg	60.00 USD
ALX-350-245-MC05		0.5 mg	250.00 USD
ALX-350-245-M001		1 mg	445.00 USD

Product Specification

FORMULA:	C₁₅H₂₄N₂O₇S
MW:	376.4
CAS NUMBER:	133343-34-7
SOURCE/HOST:	Isolated from Streptomyces sp.
PURITY:	≥97% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in acetonitrile (20mg/ml), 100% ethanol (1mg/ml), methanol, DMSO (20mg/ml), dimethyl formamide (20mg/ml) or water (5mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Organic stock solutions are stable for 3 months when stored at -20°C. Subject to hydrolysis in aqueous buffers. We do not recommend storing the aqueous solutions for more than one day.
HANDLING:	Protect from light.

Product Description

Cell permeable and irreversible proteasome inhibitor. Specifically inhibits 26S proteasome (MCP; multicatalytic proteinase complex). Blocks proteasome activity by targeting the catalytic β-subunit. Has no effect on serine or cysteine proteases. Induces apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation by inhibiting IκB degradation. Inhibits the ubiquitin proteasome pathway in cell culture (IC₅₀=10µM). Inhibits cathepsin A. Upregulates HSP70 and HSP22, suggesting an initial neuroprotective pathway.

Product Specific Literature References

Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells: S. Omura, et al.; J. Antibiot. 44, 116 (1991) Abstract
A beta-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line: G. Fenteany, et al.; PNAS 91, 3358 (1994) Abstract
Lactacystin, a specific inhibitor of the proteasome, induces apoptosis in human monoblast U937 cells: S. Imajo-Ohmi, et al.; BBRC 217, 1070 (1995) Abstract
The neuritogenesis inducer lactacystin arrests cell cycle at both G0/G1 and G2 phases in neuro 2a cells: M. Katagiri, et al.; J. Antibiotics (Tokyo) 48, 344 (1995) Abstract
Degradation process of ligand-stimulated platelet-derived growth factor beta-receptor involves ubiquitin-proteasome proteolytic pathway: S. Mori, et al.; J. Biol. Chem. 270, 29447 (1995) Abstract; Full Text
Structure-activity relationships of lactacystin, the first non-protein neurotrophic factor: T. Nagamitsu, et al.; J. Antibiotics (Tokyo) 48, 747 (1995) Abstract
Neuronal differentiation of Neuro 2a cells by lactacystin and its partial inhibition by the protein phosphatase inhibitors calyculin A and okadaic acid: H. Tanaka, et al.; BBRC 216, 291 (1995) Abstract
Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin: G. Fenteany, et al.; Science 268, 726 (1995) Abstract
Proteasome-dependent regulation of p21WAF1/CIP1 expression: M.V. Blagosklonny, et al.; BBRC 227, 564 (1996) Abstract
Enhancement of CPP32-like activity in the TNF-treated U937 cells by the proteasome inhibitors: E. Fujita, et al.; BBRC 224, 74 (1996) Abstract
Degradation of 3-hydroxy-3-methylglutaryl-CoA reductase in endoplasmic reticulum membranes is accelerated as a result of increased susceptibility to proteolysis: T.P. McGee, et al.; J.Biol. Chem. 271, 25630 (1996) Abstract; Full Text
Lactacystin increases LDL receptor level on HepG2 cells: H. Miura, et al.; BBRC 227, 684 (1996) Abstract
Proteasome pathway operates for the degradation of ornithine decarboxylase in intact cells: Y. Murakami, et al.; Biochem. J. 317, 77 (1996) Abstract; Full Text
Lactacystin, an inhibitor of the proteasome, blocks the degradation of a mutant precursor of glycosylphosphatidylinositol-linked protein in a pre-Golgi compartment: K. Oda, et al.; BBRC 219, 800 (1996) Abstract
Degradation of a mutant secretory protein, alpha1-antitrypsin Z, in the endoplasmic reticulum requires proteasome activity: D. Qu, et al.; J. Biol. Chem. 271, 22791 (1996) Abstract; Full Text
Accelerated degradation of PML-retinoic acid receptor alpha (PML-RARA) oncoprotein by all-trans-retinoic acid in acute promyelocytic leukemia: possible role of the proteasome pathway: H. Yoshida, et al.; Cancer Res. 56, 2945 (1996) Abstract
The proteasome inhibitor lactacystin induces apoptosis and sensitizes chemo- and radioresistant human chronic lymphocytic leukaemia lymphocytes to TNF-alpha-initiated apoptosis: J. Delic, et al.; Br. J. Cancer 77, 1103 (1998) Abstract
Lactacystin, proteasome function, and cell fate: G. Fenteany & S.L. Schreiber; J. Biol. Chem. 273, 8545 (1998), (Review) Abstract; Full Text
Proteasome inhibitors prevent the degradation of familial Alzheimer's disease-linked presenilin 1 and potentiate A beta 42 recovery from human cells: P. Marambaud, et al.; Mol. Med. 4, 147 (1998) Abstract
The role of proteolysis during differentiation of Trypanosoma brucei from the bloodstream to the procyclic form: M.C. Mutomba & C.C. Wang; Mol. Biochem. Parasitol. 93, 11 (1998) Abstract
Lactacystin, a proteasome inhibitor: discovery and its application in cell biology: H. Tomoda & S. Omura; Yakugaku Zasshi 120, 935 (2000), Review Abstract
Lactacystin inhibits cathepsin A activity in melanoma cell lines: L. Kozlowski, et al.; Tumour Biol. 22, 211 (2001) Abstract
Proteasome inhibition by lactacystin in primary neuronal cells induces both potentially neuroprotective and pro-apoptotic transcriptional responses: a microarray analysis: E.H. Yew, et al.; J. Neurochem. 94, 943 (2005) Abstract

Further Categories Containing This Product:

Heat Shock Proteins Other Products • Proteasome / Related Products • NF-kB Pathway Inhibitors • Antibiotics for Angiogenesis Research • Antibiotics - NF-kB Inhibitors • Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Antibiotics

ALX-350-260

Revised 11-Aug-08

Lactacystin (synthetic)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Proteasome / Ubiquitin Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-260-MC01		0.1 mg	95.00 USD
ALX-350-260-M001		1 mg	730.00 USD

Product Specification

FORMULA:	C₁₅H₂₄N₂O₇S
MW:	376.4
CAS NUMBER:	133343-34-7
SOURCE/HOST:	Synthetic.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in acetonitrile (20mg/ml), 100% ethanol (1mg/ml), methanol, DMSO (20mg/ml), dimethyl formamide (20mg/ml) or water (5mg/ml).
ACTIVITY:	k_obs/[I]=4’000M^-1sec^-1 versus 20S:PA28 complex.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Organic stock solutions are stable for 3 months when stored at -20°C. Subject to hydrolysis in aqueous buffers. We do not recommend storing aqueous solutions for more than one day.
HANDLING:	Protect from light. Avoid freeze/thaw cycles.
IDENTITY:	Identity determined by ¹H-NMR.

Product Description

Cell permeable and irreversible proteasome inhibitor. Specifically inhibits 26S proteasome (MCP; multicatalytic proteinase complex). Blocks proteasome activity by targeting the catalytic β-subunit. Has no effect on serine or cysteine proteases. Induces apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation by inhibiting IκB degradation. Inhibits the ubiquitin proteasome pathway in cell culture (IC₅₀=10µM). Inhibits cathepsin A . Upregulates HSP70 and HSP22, suggesting an initial neuroprotective pathway.

Product Specific Literature References

Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells: S. Omura, et al.; J. Antibiot. 44, 113 (1991) Abstract
A beta-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line: G. Fenteany, et al.; PNAS 91, 3358 (1994) Abstract
Lactacystin, a specific inhibitor of the proteasome, induces apoptosis in human monoblast U937 cells: S. Imajo-Ohmi, et al.; BBRC 217, 1070 (1995) Abstract
The neuritogenesis inducer lactacystin arrests cell cycle at both G0/G1 and G2 phases in neuro 2a cells: M. Katagiri, et al.; J. Antibiot. (Tokyo) 48, 344 (1995) Abstract
Degradation process of ligand-stimulated platelet-derived growth factor beta-receptor involves ubiquitin-proteasome proteolytic pathway: S. Mori, et al.; J. Biol. Chem. 270, 29447 (1995) Abstract; Full Text
Structure-activity relationships of lactacystin, the first non-protein neurotrophic factor: T. Nagamitsu, et al.; J. Antibiotics 48, 747 (1995) Abstract
Neuronal differentiation of Neuro 2a cells by lactacystin and its partial inhibition by the protein phosphatase inhibitors calyculin A and okadaic acid: H. Tanaka, et al.; BBRC 216, 291 (1995) Abstract
Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin: G. Fenteany, et al.; Science 268, 726 (1995) Abstract
Proteasome-dependent regulation of p21WAF1/CIP1 expression: M.V. Blagosklonny, et al.; BBRC 227, 564 (1996) Abstract
Enhancement of CPP32-like activity in the TNF-treated U937 cells by the proteasome inhibitors: E. Fujita, et al.; BBRC 224, 74 (1996) Abstract
Degradation of 3-hydroxy-3-methylglutaryl-CoA reductase in endoplasmic reticulum membranes is accelerated as a result of increased susceptibility to proteolysis: T.P. McGee, et al.; J.Biol. Chem. 271, 25630 (1996) Abstract; Full Text
Lactacystin increases LDL receptor level on HepG2 cells: H. Miura, et al.; BBRC 227, 684 (1996) Abstract
Proteasome pathway operates for the degradation of ornithine decarboxylase in intact cells: Y. Murakami, et al.; Biochem. J. 317, 77 (1996) Abstract
Lactacystin, an inhibitor of the proteasome, blocks the degradation of a mutant precursor of glycosylphosphatidylinositol-linked protein in a pre-Golgi compartment: K. Oda, et al.; BBRC 219, 800 (1996) Abstract
Degradation of a mutant secretory protein, alpha1-antitrypsin Z, in the endoplasmic reticulum requires proteasome activity: D. Qu, et al.; J. Biol. Chem. 271, 22791 (1996) Abstract; Full Text
Accelerated degradation of PML-retinoic acid receptor alpha (PML-RARA) oncoprotein by all-trans-retinoic acid in acute promyelocytic leukemia: possible role of the proteasome pathway: H. Yoshida, et al.; Cancer Res. 56, 2945 (1996) Abstract
Lactacystin and clasto-lactacystin beta-lactone modify multiple proteasome beta-subunits and inhibit intracellular protein degradation and major histocompatibility complex class I antigen presentation: A. Craiu, et al.; J. Biol. Chem. 272, 13437 (1997) Abstract; Full Text
The proteasome inhibitor lactacystin induces apoptosis and sensitizes chemo- and radioresistant human chronic lymphocytic leukaemia lymphocytes to TNF-alpha-initiated apoptosis: J. Delic, et al.; Br. J. Cancer 77, 1103 (1998) Abstract
Lactacystin, proteasome function, and cell fate: G. Fenteany & S.L. Schreiber; J. Biol. Chem. 273, 8545 (1998), (Review) Abstract; Full Text
The role of proteolysis during differentiation of Trypanosoma brucei from the bloodstream to the procyclic form: M.C. Mutomba, et al.; Mol. Biochem. Parasitol. 93, 11 (1998) Abstract
Proteasome inhibitors prevent the degradation of familial Alzheimer's disease-linked presenilin 1 and potentiate A beta 42 recovery from human cells: P. Marambaud, et al.; Mol. Med. 4, 147 (1998) Abstract
Proteasome inhibitors MG132 and lactacystin hyperphosphorylate HSF1 and induce hsp70 and hsp27 expression: D. Kim, et al.; BBRC 254, 264 (1999) Abstract
Proteasome inhibitors induce mitochondria-independent apoptosis in human glioma cells: H. Kitagawa, et al.; FEBS Lett. 443, 181 (1999) Abstract
Lactacystin, a specific inhibitor of the proteasome, induces apoptosis and activates caspase-3 in cultured cerebellar granule cells: L.A. Pasquini, et al.; J. Neurosci. Res. 59, 601 (2000) Abstract
Proteasome inhibitors induce cytochrome c-caspase-3-like protease- mediated apoptosis in cultured cortical neurons: J.H. Qiu, et al.; J. Neurosci. 20, 259 (2000) Abstract
Lactacystin activates FLICE (caspase 8) protease and induces apoptosis in Fas-resistant adult T-cell leukemia cell lines: Y. Yamada, et al.; Eur. J. Haematol. 64, 315 (2000) Abstract
Lactacystin, a proteasome inhibitor: discovery and its application in cell biology: H. Tomoda & S. Omura; Yakugaku Zasshi 120, 935 (2000), Review Abstract
Lactacystin inhibits cathepsin A activity in melanoma cell lines: L. Kozlowski, et al.; Tumour Biol. 22, 211 (2001) Abstract
Proteasome inhibition by lactacystin in primary neuronal cells induces both potentially neuroprotective and pro-apoptotic transcriptional responses: a microarray analysis: E.H. Yew, et al.; J. Neurochem. 94, 943 (2005) Abstract

Further Categories Containing This Product:

ALX-430-095

Revised 23-Jan-08

Leflunomide
SYNONYMS	HWA486 5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide) N-(4-Trifluoromethylphenyl)-5-methylisoxazol-4-carboxamide
PRODUCT LINE	Immunology
PRODUCT CATEGORY	Immunomodulators Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-430-095-M010		10 mg	15.00 USD
ALX-430-095-M050		50 mg	40.00 USD
ALX-430-095-G001		1 g	380.00 USD

Product Specification

FORMULA:	C₁₂H₉F₃N₂O₂
MW:	270.2
CAS NUMBER:	75706-12-6
MERCK INDEX:	14: 5432
RTECS:	NY2354200
PURITY:	≥99% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Keep under inert gas. Protect from light.
HAZARD:	HARMFUL.

Product Description

Immunosuppressive drug that inhibits T and B cell responses in vivo. Inhibitor of tyrosine phosphorylation (tyrosine kinase inhibitor), of dihydroorotate dehydrogenase, an enzyme for de novo pyrimidine synthesis, of TNF-dependent NF-κB activation, and of COX-2. The physiological activity of leflunomide is attributed mainly to its metabolite A77 1726 (Prod. No. ALX-430-096).

Product Specific Literature References

Immunopharmacological profile of a novel isoxazol derivative, HWA 486, with potential antirheumatic activity-I. Disease modifying action on adjuvant arthritis of the rat: R.R. Bartlett & R. Schleyerbach; Int. J. Immunopharmacol. 7, 7 (1985) Abstract
Leflunomide (HWA 486), a novel immunomodulating compound for the treatment of autoimmune disorders and reactions leading to transplantation rejection: R.R. Bartlett, et al.; Agents Actions 32, 10 (1991) Abstract
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993) Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995) Abstract; Full Text
Molecular mechanisms of action of new xenobiotic immunosuppressive drugs: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide: T.R. Brazelton & R.E. Morris; Curr. Opin. Immunol. 8, 710 (1996) Abstract
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract
Regulation of B cell function by the immunosuppressive agent leflunomide: K.F. Siemasko, et al.; Transplantation 61, 635 (1996) Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996) Abstract
Potencies of leflunomide and HR325 as inhibitors of prostaglandin endoperoxide H synthase-1 and -2: comparison with nonsteroidal anti- inflammatory drugs: A.P. Curnock, et al.; J. Pharmacol. Exp. Ther. 282, 339 (1997) Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997) Abstract
Leflunomide, a novel immunomodulating agent, prevents the development of allergic sensitization in an animal model of allergic asthma: E. Eber, et al.; Clin. Exp. Allergy 28, 376 (1998)