ALEXIS Biochemicals: Hypothemycin

You are here: Product Lines > Signal Transduction > Kinases / Related Products > Tyrosine Kinases / Related Products > Tyrosine Kinase Inhibitors

ALX-350-007

Revised 07-Apr-08

Lavendustin A
SYNONYMS	5-Amino-[(N-2,5-dihydroxybenzyl)-N'-2-hydroxybenzyl]salicylic acid RG14355
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-350-007-M001		1 mg	75.00 USD
ALX-350-007-M005		5 mg	295.00 USD

Product Specification

FORMULA:	C₂₁H₁₉NO₆
MW:	381.4
CAS NUMBER:	125697-92-9
SOURCE/HOST:	Synthetic.
PURITY:	≥97% (TLC)
APPEARANCE:	Off-white to brown solid.
SOLUBILITY:	Soluble in DMSO, methanol or dilute aqueous base.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light and moisture. Hygroscopic.

Product Description

Cell permeable tyrosine kinase inhibitor with little effect on cAMP-dependent protein kinase (PKA) or protein kinase C (PKC). Inhibits autophosphorylation of EGFRs. Also inhibits NMDA-stimulated cGMP production.

Product Specific Literature References

Cellular oncogenes and retroviruses: J.M. Bishop; Annu. Rev. Biochem. 52, 301 (1983) Abstract
Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus: T. Onoda, et al.; J. Nat. Prod. 52, 1252 (1989) Abstract
Kinetic analysis of the inhibition of the epidermal growth factor receptor tyrosine kinase by Lavendustin-A and its analogue: C.-Y.J. Hsu, et al.; J. Biol. Chem. 266, 21105 (1991) Abstract
Long-term potentiation in the hippocampus is blocked by tyrosine kinase inhibitors: T.J. O'Dell, et al.; Nature 353, 558 (1991) Abstract
Blockade of nitric oxide synthesis by tyrosine kinase inhibitors in neurones: J. Rodriguez, et al.; Neuropharmacology 33, 1267 (1994) Abstract
Solid Phase Synthesis of Lavendustin A and Analogs: J. Green; J. Org. Chem. 60, 4287 (1995)
Suppression of VEGF-induced angiogenesis by the protein tyrosine kinase inhibitor, lavendustin A: D.E. Hu and T.-P.D. Fan; Br. J. Pharmacol. 114, 262 (1995) Abstract
Inhibition of atrial wall stretch-induced cardiac hormone secretion by lavendustin A, a potent tyrosine kinase inhibitor: P. Taskinen, et al.; Endocrinology 140, 4198 (1999) Abstract
Influence of the tyrosine kinase inhibitors STI571 (Glivec(R)), lavendustin A and genistein on human mast cell line (HMC-1(560)) activation: K. Lober, et al.; J. Cell Biochem. 103, 1076 (2007) Abstract

Related Products

ALX-350-091

Lavendustin A methyl ester

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • EGFR Kinase Inhibitors • Natural Products for Angiogenesis Research • Natural Products - Nitric Oxide Pathway Modulators

ALX-350-009

Revised 03-Apr-08

Daidzein
SYNONYMS	4',7-Dihydroxyisoflavone
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-350-009-M010		10 mg	20.00 USD
ALX-350-009-M025		25 mg	40.00 USD
ALX-350-009-M050		50 mg	60.00 USD

Product Specification

FORMULA:	C₁₅H₁₀O₄
MW:	254.2
CAS NUMBER:	486-66-8
MERCK INDEX:	14: 2801
RTECS:	DJ3100040
SOURCE/HOST:	Synthetic.
PURITY:	≥98%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO; slightly soluble in 100% ethanol; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	IRRITANT.

Product Description

Inactive analog of the tyrosine kinase inhibitor genistein (Prod. No. ALX-350-006). Shows anti-inflammatory effect.

Product Specific Literature References

Genistein, a specific inhibitor of tyrosine-specific protein kinases: T. Akiyama, et al.; J. Biol. Chem. 262, 5592 (1987) Abstract; Full Text
Role of tyrosine kinases in IgE-mediated signal transduction in human lung mast cells and basophils: S.E. Lavens, et al.; Am. J. Respir. Cell. Mol. Biol. 7, 637 (1992) Abstract
Tyrosine kinase inhibitors block calcium channel currents in vascular smooth muscle cells: S. Wijetunge, et al.; BBRC 189, 1620 (1992) Abstract
Genistein and daidzein, and their ß-glycoside conjugates: anti-tumor isoflavones in soybean foods from American and Asian diets: L. Coward, et al.; J. Agric. Food Chem. 41, 1961 (1993)
Stimulation of pS2 expression by diet-derived compounds: N. Sathyamoorthy, et al.; Cancer Res. 54, 957 (1994) Abstract
Daidzein inhibits insulin- or insulin-like growth factor-1-mediated signaling in cell cycle progression of Swiss 3T3 cells: K. Higashi and H. Ogawara; Biochim. Biophys. Acta 1221, 29 (1994) Abstract
Decreased circulating levels of tumor necrosis factor-alpha in postmenopausal women during consumption of soy-containing isoflavones: Y. Huang, et al.; J. Clin. Endocrinol. Metab. 90, 3956 (2005) Abstract
Gut bacterial metabolism of the soy isoflavone daidzein: exploring the relevance to human health: C. Atkinson, et al.; Exp. Biol. Med. (Maywood) 230, 155 (2005), Review Abstract
Clinical review: a critical evaluation of the role of soy protein and isoflavone supplementation in the control of plasma cholesterol concentrations: A. Dewell, et al.; J. Clin. Endocrinol. Metab. 91, 772 (2006), Review Abstract
Phytoestrogens and lipoproteins in women: C.N. Bairey Merz, et al.; J. Clin. Endocrinol. Metab. 91, 2209 (2006) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • Active Substances from Fruit and Vegetables • Natural Products - Anti-inflammatory Agents • Isoflavones

ALX-350-027

Revised 19-Aug-08

Calphostin C
SYNONYMS	UCN-1028C
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-350-027-C100		100 µg	85.00 USD
ALX-350-027-M001		1 mg	595.00 USD

Product Specification

FORMULA:	C₄₄H₃₈O₁₄
MW:	790.8
CAS NUMBER:	121263-19-2
SOURCE/HOST:	Isolated from Cladosporium cladosporioides MST-FP1798.
PURITY:	≥95% (HPLC)
APPEARANCE:	Dark red solid.
SOLUBILITY:	Soluble in 100% ethanol, methanol, DMSO or dimethyl formamide; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
USE/STABILITY:	Stock solutions are stable for 3 months when stored at -20°C.
HANDLING:	Protect from light.

Product Description

Potent and selective inhibitor of the protein kinase C (PKC) regulatory site of diacylglycerol and phorbol esters. At higher concentrations inhibits myosin light chain kinase, cAMP-dependent protein kinase, protein kinase G and pp60v-src protein tyrosine kinase. Induces apoptotic DNA fragmentation and cell death. Kills breast cancer cells. Has antiviral potential. Inhibits cardiac L-type Ca²⁺ channels.

Product Specific Literature References

Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C: E. Kobayashi, et al.; BBRC 159, 548 (1989) Abstract
Potent and specific inhibitors of protein kinase C of microbial origin: T. Tamaoki and H. Nakano; Biotechnology 8, 732 (1990) Abstract
Inhibition of protein kinase C by calphostin C is light-dependent: R.F. Bruns, et al.; BBRC 176, 288 (1991) Abstract
Irreversible oxidative inactivation of protein kinase C by photosensitive inhibitor calphostin C: R. Gopalakrishna, et al.; FEBS Lett. 314, 149 (1992) Abstract
Calphostin C, a specific protein kinase C inhibitor, activates human neutrophils: effect on phospholipase A2 and aggregation: S. Svetlov and S. Nigam; Biochim. Biophys. Acta 1177, 75 (1993) Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994) Abstract
Growth inhibition of herpes simplex virus-type 1 in calphostin C-treated astrocytes: C.G. Castagnino, et al.; Intervirology 38, 332 (1995) Abstract
Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels: H.C. Hartzell & A. Rinderknecht; Am. J. Physiol. 270, C1293 (1996) Abstract
Pharmacokinetic features and metabolism of calphostin C, a naturally occurring perylenequinone with antileukemic activity: C.L. Chen, et al.; Pharm. Res. 16, 1003 (1999) Abstract
Potent killing of paclitaxel- and doxorubicin-resistant breast cancer cells by calphostin C accompanied by cytoplasmic vacuolization: B. Guo, et al.; Breast Cancer Res. Treat. 82, 125 (2003) Abstract

Further Categories Containing This Product:

Myosin Light Chain Kinase Inhibitors • Tyrosine Kinase Inhibitors • PKA Inhibitors • PKC Inhibitors • PKG Inhibitors • Ca2+ Channels (L-type) • Natural Products - Antiviral / anti-HIV Agents • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents

ALX-350-029

Revised 07-Oct-08

Herbimycin A
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-029-C100		100 µg	110.00 USD
ALX-350-029-M001		1 mg	560.00 USD

Product Specification

FORMULA:	C₃₀H₄₂N₂O₉
MW:	574.7
CAS NUMBER:	70563-58-5
RTECS:	LX8930000
SOURCE/HOST:	Isolated from Streptomyces sp.
PURITY:	≥97%
APPEARANCE:	Yellow powder.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.

Product Description

Antibiotic. Cell permeable tyrosine kinase inhibitor. Inhibitor of HSP90, NF-κB activation and angiogenesis. Increases the sensitivity of certain cancer cells to chemotherapeutic agents. Blocks mitotic activity. Neurotoxic.

Product Specific Literature References

Herbimycin, a new antibiotic produced by a strain of Streptomyces: S. Omura, et al.; J. Antibiot. (Tokyo) 32, 255 (1979) Abstract
A new activity of herbimycin A: inhibition of angiogenesis: T. Yamashita, et al.; J. Antibiot. (Tokyo) 42, 1015 (1989) Abstract
Stimulation by Bt2cAMP of epidermal mucous metaplasia in retinol- pretreated chick embryonic cultured skin, and its inhibition by herbimycin A, an inhibitor for protein-tyrosine kinase: A. Obinata, et al.; Exp. Cell. Res. 193, 36 (1991) Abstract
IgE-induced tyrosine phosphorylation of phospholipase C-gamma 1 in rat basophilic leukemia cells: D.J. Park, et al.; J. Biol. Chem. 266, 24237 (1991) Abstract; Full Text
Bacterial lipopolysaccharide stimulates protein tyrosine phosphorylation in macrophages: S.L. Weinstein, et al.; PNAS 88, 4148 (1991) Abstract
Inhibition of interleukin 3 and granulocyte-macrophage colony- stimulating factor stimulated increase of active ras.GTP by herbimycin A, a specific inhibitor of tyrosine kinases: T. Satoh, et al.; J. Biol. Chem. 267, 2537 (1992) Abstract; Full Text
New insight into oncoprotein-targeted antitumor effect: herbimycin A as an antagonist of protein tyrosine kinase against Ph1-positive leukemia cells: M. Okabe and M. Uehara; Leuk. Lymphoma 12, 41 (1993) Abstract
Prevention of anti-CD3 monoclonal antibody-induced thymic apoptosis by protein tyrosine kinase inhibitors: K. Migita, et al.; J. Immunol. 153, 3457 (1994) Abstract
Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation: L. Whitesell, et al.; PNAS 91, 8324 (1994) Abstract; Full Text
Inhibition of PDGF-induced phospholipase D but not phospholipase C activation by herbimycin A: B.Y. Kim; BBRC 212, 1061 (1995) Abstract
Controlling the vasculature: angiogenesis, anti-angiogenesis and vascular targeting of gene therapy: T.-P.D. Fan, et al.; TIPS 16, 57 (1995), (Review) Abstract
Herbimycin A enhances apoptotic effect of chemotherapeutic drugs on K562 cells: H. Ren, et al.; Chin. Med. J. (Engl.) 111, 678 (1998) Abstract
Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs: M.V. Blagosklonny; Leukemia 16, 455 (2002) Abstract; Full Text
Geldanamycin and herbimycin A induce apoptotic killing of B chronic lymphocytic leukemia cells and augment the cells’ sensitivity to cytotoxic drugs: D.T. Jones, et al.; Blood 103, 1855 (2004) Abstract; Full Text
Herbimycin A abrogates nuclear factor-kappaB activation by interacting preferentially with the IkappaB kinase beta subunit: S. Ogino, et al.; Mol. Pharmacol. 65, 1344 (2004) Abstract; Full Text
Herbimycin A suppresses mitotic activity and egg production of female Schistosoma mansoni: J. Knobloch, et al.; Int. J. Parasitol. 36, 1261 (2006) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • Neurotoxins • Phospholipase D / Related Products • Antibiotics for Angiogenesis Research • HSP90 / HtpG / Related Products

ALX-350-037

Revised 04-Feb-05

Lavendustin B
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-350-037-M001		1 mg	80.00 USD

Product Specification

FORMULA:	C₂₁H₁₉NO₅
MW:	365.4
CAS NUMBER:	125697-91-8
SOURCE/HOST:	Synthetic.
PURITY:	≥98%
APPEARANCE:	Off-white solid.
SOLUBILITY:	Soluble in methanol, DMSO and dilute aqueous base.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Control for lavendustin A (Prod. No. ALX-350-007); 100-fold less potent than lavendustin A.

Product Specific Literature References

Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus: T. Onoda, et al.; J. Nat. Prod. 52, 1252 (1989) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors

ALX-350-057

Revised 20-Feb-08

Emodin
SYNONYMS	6-Methyl-1,3,8-trihydroxyanthraquinone
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-350-057-M025		25 mg	45.00 USD

Product Specification

FORMULA:	C₁₅H₁₀O₅
MW:	270.2
CAS NUMBER:	518-82-1
MERCK INDEX:	14: 3561
RTECS:	CB7920600
SOURCE/HOST:	Isolated from Frangula bark.
PURITY:	≥96% (HPLC)
APPEARANCE:	Orange to red solid.
SOLUBILITY:	Soluble in DMSO, 100% ethanol or 1N dilute aqueous ammonia; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	IRRITANT.

Product Description

Inhibitor of p56^lck tyrosine kinase. Has mutagenic and genotoxic effects, mainly in bacterial systems. Anticancer agent. Exhibits anti-proliferative effects in various cancer cell lines by efficient induction of apoptosis. Has inhibitory effects on angiogenic and metastasis regulatory processes. Anti-inflammatory compound. Suppresses NF-κB activation.

Product Specific Literature References

Emodin, a protein tyrosine kinase inhibitor from Polygonum cuspidatum: H. Jayasuriya, et al.; J. Nat. Prod. 55, 696 (1992) Abstract
Selective inhibition of the growth of ras-transformed human bronchial epithelial cells by emodin, a protein-tyrosine kinase inhibitor: T.C.K. Chan, et al.; BBRC 193, 1152 (1993) Abstract
Molecular mechanism of emodin action: transition from laxative ingredient to an antitumor agent: G. Srinivas, et al.; Med. Res. Rev. 27, 591 (2007), (Review) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • Other Toxins • Src Family Kinases / Related Products • Kinases in T Cell Signal Transduction / Related Products • Natural Products - Anti-inflammatory Agents • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • NF-kB Pathway Inhibitors • Natural Products - Antitumor Reagents

ALX-350-084

Revised 07-Apr-08

Lavendustin C methyl ester
SYNONYMS	Compound 5 methyl ester 5-Amino-N-(2,5-dihydroxybenzyl)methyl salicylate
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-350-084-M001		1 mg	50.00 USD
ALX-350-084-M005		5 mg	200.00 USD

Product Specification

FORMULA:	C₁₅H₁₅NO₅
MW:	289.3
SOURCE/HOST:	Synthetic.
PURITY:	≥97%
APPEARANCE:	Off-white solid.
SOLUBILITY:	Soluble in DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
HAZARD:	TOXIC.

Product Description

Inhibitor of EGFR tyrosine kinase with improved bioavailability over lavendustin C (Prod. No. ALX-270-066).

Product Specific Literature References

Synthesis and structure-activity studies of a series of [(hydroxybenzyl)amino]salicylates as inhibitors of EGF receptor- associated tyrosine kinase activity: H. Chen, et al.; J. Med. Chem. 36, 4094 (1993) Abstract
Structure-activity relationships in a series of 5-[(2,5- dihydroxybenzyl)amino]salicylate inhibitors of EGF-receptor-associated tyrosine kinase: importance of additional hydrophobic aromatic interactions: H. Chen, et al.; J. Med. Chem. 37, 845 (1994) Abstract

FORMULA:	C₂₂H₂₁NO₆
MW:	395.4
PURITY:	≥97%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.