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ALX-270-104

Revised 21-Mar-07

NPC-15437 . dihydrochloride
SYNONYMS	(S)-2,6-diamino-N-{[1'-(1''-oxotridecyl)-2'-piperidinyl]methyl}hexanamide . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-104-M001		1 mg	90.00 USD
ALX-270-104-M005		5 mg	350.00 USD

Product Specification

FORMULA:	C₂₅H₅₀N₄O₂ . 2 HCl
MW:	438.7 . 73.0
CAS NUMBER:	136449-85-9; 141774-20-1
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in water, DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Hygroscopic.

Product Description

Selective inhibitor of protein kinase C (PKC).

Product Specific Literature References

NPC 15437 interacts with the C1 domain of protein kinase C. An analysis using mutant PKC constructs: J.P. Sullivan, et al.; FEBS Lett. 285, 120 (1991) Abstract
2,6-Diamino-N-([1-oxotridecyl)-2-piperidinyl]methyl)hexanamide (NPC 15437): a selective inhibitor of protein kinase C: J.P. Sullivan, et al.; Agents Actions 34, 142 (1991) Abstract
2,6-Diamino-N-([1-(1-oxotridecyl)-2-piperidinyl] methyl)hexanamide (NPC 15437): a novel inhibitor of protein kinase C interacting at the regulatory domain: J.P. Sullivan, et al.; Mol. Pharmacol. 41, 38 (1992) Abstract

ALX-300-006

Revised 03-Jul-06

1-O-Octadecyl-2-O-methyl-rac-glycero-3-phosphocholine
SYNONYMS	rac-ET-18-OCH₃ Edelfosine
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Phospholipids / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-300-006-M050		50 mg	45.00 USD
ALX-300-006-M250		250 mg	180.00 USD

Product Specification

FORMULA:	C₂₇H₅₈NO₆P
MW:	523.7
CAS NUMBER:	70641-51-9
RTECS:	YK0718000
PURITY:	≥99%
APPEARANCE:	White to off-white amorphous solid.
SOLUBILITY:	Soluble in chloroform (50mg/ml), 100% ethanol (5mg/ml) or water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Hygroscopic.
HAZARD:	MAY BE MUTAGENIC. HARMFUL.

Product Description

Produces strong antitumor and antimetastatic activities. Inhibits phosphatidylinositol specific phospholipase C and protein kinase C (PKC). Induces apoptosis.

Product Specific Literature References

Antiinvasive effect of racemic 1-O-octadecyl-2-O-methylglycero-3- phosphocholine on MO4 mouse fibrosarcoma cells in vitro: G.A. Storme, et al.; Cancer Res. 45, 351 (1985) Abstract
Cytotoxic ether phospholipids. Different affinities to lysophosphocholine acyltransferases in sensitive and resistant cells: D.B.J. Herrmann & H.A. Neumann; J. Biol. Chem. 261, 7742 (1986) Abstract; Full Text
Inhibition of Na,K-ATPase and sodium pump by anticancer ether lipids and protein kinase C inhibitors ET-18-OCH3 and BM 41.440: K. Oishi, et al.; BBRC 157, 1000 (1988) Abstract
Solubilization of the NADPH-oxidase from bone marrow derived macrophages by dialkylphospholipid and purification by HPLC-anion exchange chromatography: J. Storch & E. Ferber; Biol. Chem. Hoppe-Seyler 369, 403 (1988) Abstract
Molecular dynamics of antitumor ether-linked phospholipids in model membranes: a spin-label study: C.-S. Lai, et al.; BBRC 160, 1189 (1989) Abstract
The ether lipid 1-octadecyl-2-methyl-rac-glycero-3-phosphocholine induces expression of fos and jun proto-oncogenes and activates AP-1 transcription factor in human leukaemic cells: F. Mollinedo, et al.; Biochem. J. 302, 325 (1994) Abstract
Ether lipids enhance the cytotoxic effect of teniposide and paclitaxel in liposomes against leukaemic cells in culture: B.B. Lundberg; Anticancer Drug Des. 12, 503 (1997) Abstract
Selective induction of apoptosis in cancer cells by the ether lipid ET- 18-OCH3 (Edelfosine): molecular structure requirements, cellular uptake, and protection by Bcl-2 and Bcl-X(L): F. Mollinedo, et al.; Cancer Res. 57, 1320 (1997) Abstract
The inhibition of cell signaling pathways by antitumor ether lipids: G. Arthur & R. Bittman; Biochim. Biophys. Acta. 1390, 85 (1998) Abstract
Cytotoxic etherphospholipid analogues: D. Berkovic; Gen Pharmacol. 31, 511 (1998) Abstract
Involvement of c-Jun NH2-terminal kinase activation and c-Jun in the induction of apoptosis by the ether phospholipid 1-O-octadecyl-2-O- methyl-rac-glycero-3-phosphocholine: C. Gajate, et al.; Mol. Pharmacol. 53, 602 (1998) Abstract
The anticancer drug edelfosine is a potent inhibitor of neovascularization in vivo: W.R. Vogler, et al.; Cancer Invest. 16, 549 (1998) Abstract
Liposomal ET-18-OCH(3) induces cytochrome c-mediated apoptosis independently of CD95 (APO-1/Fas) signaling: O. Cuvillier, et al.; Blood 94, 3583 (1999) Abstract
Induction of apoptosis in human mitogen-activated peripheral blood T- lymphocytes by the ether phospholipid ET-18-OCH3: involvement of the Fas receptor/ligand system: C. Cabaner, et al.; Br. J. Pharmacol. 127, 813 (1999) Abstract
Alkyl-lysophospholipids activate the SAPK/JNK pathway and enhance radiation-induced apoptosis: G.A. Ruiter, et al.; Cancer Res. 59, 2457 (1999) Abstract
Intracellular triggering of Fas, independently of FasL, as a new mechanism of antitumor ether lipid-induced apoptosis: C. Gajate, et al.; Int. J. Cancer 85, 674 (2000) Abstract
Involvement of mitochondria and caspase-3 in ET-18-OCH(3)-induced apoptosis of human leukemic cells: C. Gajate, et al.; Int. J. Cancer 86, 208 (2000) Abstract

Further Categories Containing This Product:

Phospholipase C / Related Products • PKC Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Apoptosis Inducers)

ALX-300-004

Revised 13-Mar-08

1-O-Octadecyl-2-O-methyl-sn-glycero-3-phosphocholine
SYNONYMS	2-O-Methyl-PAF-C-18 sn-ET-18-OCH₃ Edelfosine
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Phospholipids / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-300-004-M050		50 mg	40.00 USD
ALX-300-004-M250		250 mg	160.00 USD
ALX-300-004-G001		1 g	480.00 USD

Product Specification

FORMULA:	C₂₇H₅₈NO₆P
MW:	523.7
CAS NUMBER:	77286-66-9
PURITY:	≥98%
APPEARANCE:	White amorphous powder.
SOLUBILITY:	Soluble in 100% ethanol, DMSO or dimethyl formamide.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Hygroscopic.

Product Description

Produces strong antitumor and antimetastatic activities. Inhibits phosphatidylinositol specific phospholipase C and protein kinase C from various leukemic cells. Antineoplastic activity.

Product Specific Literature References

Selective destruction of human leukemic cells by alkyl- lysophospholipids: R. Andreesen, et al.; Cancer Res. 38, 3894 (1978) Abstract
Disturbance of phospholipid metabolism during the selective destruction of tumor cells induced by alkyl-lysophospholipids: M. Modolell, et al.; Cancer Res. 39, 4681 (1979) Abstract
Phospholipid-sensitive Ca2+-dependent protein phosphorylation system in various types of leukemic cells from human patients and in human leukemic cell lines HL60 and K562, and its inhibition by alkyl- lysophospholipid: D.M. Helfman, et al.; Cancer Res. 43, 2955 (1983) Abstract
Purging leukemic cells from simulated human remission marrow with alkyl- lysophospholipid: S. Okamoto, et al.; Blood 69, 1381 (1987) Abstract
HL-60 cells become resistant towards antitumor ether-linked phospholipids following differentiation into a granulocytic form: D.S. Vallari, et al.; BBRC 156, 1 (1988) Abstract
The ether lipid 1-octadecyl-2-methyl-rac-glycero-3-phosphocholine induces expression of fos and jun proto-oncogenes and activates AP-1 transcription factor in human leukaemic cells: F. Mollinedo, et al.; Biochem. J. 302, 325 (1994) Abstract
Ether lipids enhance the cytotoxic effect of teniposide and paclitaxel in liposomes against leukaemic cells in culture: B.B. Lundberg; Anticancer Drug Des. 12, 503 (1997) Abstract
Selective induction of apoptosis in cancer cells by the ether lipid ET- 18-OCH3 (Edelfosine): molecular structure requirements, cellular uptake, and protection by Bcl-2 and Bcl-X(L): F. Mollinedo, et al.; Cancer Res. 57, 1320 (1997) Abstract
The inhibition of cell signaling pathways by antitumor ether lipids: G. Arthur & R. Bittman; Biochim. Biophys. Acta. 1390, 85 (1998) Abstract
Cytotoxic etherphospholipid analogues: D. Berkovic; Gen Pharmacol. 31, 511 (1998) Abstract
Involvement of c-Jun NH2-terminal kinase activation and c-Jun in the induction of apoptosis by the ether phospholipid 1-O-octadecyl-2-O- methyl-rac-glycero-3-phosphocholine: C. Gajate, et al.; Mol. Pharmacol. 53, 602 (1998) Abstract
The anticancer drug edelfosine is a potent inhibitor of neovascularization in vivo: W.R. Vogler, et al.; Cancer Invest. 16, 549 (1998) Abstract
Liposomal ET-18-OCH(3) induces cytochrome c-mediated apoptosis independently of CD95 (APO-1/Fas) signaling: O. Cuvillier, et al.; Blood 94, 3583 (1999) Abstract
Alkyl-lysophospholipids activate the SAPK/JNK pathway and enhance radiation-induced apoptosis: G.A. Ruiter, et al.; Cancer Res. 59, 2457 (1999) Abstract
Induction of apoptosis in human mitogen-activated peripheral blood T- lymphocytes by the ether phospholipid ET-18-OCH3: involvement of the Fas receptor/ligand system: C. Cabaner, et al.; Br. J. Pharmacol. 127, 813 (1999) Abstract
Intracellular triggering of Fas, independently of FasL, as a new mechanism of antitumor ether lipid-induced apoptosis: C. Gajate, et al.; Int. J. Cancer 85, 674 (2000) Abstract
Involvement of mitochondria and caspase-3 in ET-18-OCH(3)-induced apoptosis of human leukemic cells: C. Gajate, et al.; Int. J. Cancer 86, 208 (2000) Abstract

Further Categories Containing This Product:

Phospholipase C / Related Products • PKC Inhibitors • Antitumor Agents (Enzyme Inhibitors)

ALX-380-210

Revised 08-Apr-08

7-Oxostaurosporine
SYNONYMS	Antibiotic BMY 41950 Antibiotic RK 1409 LCM76-L
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-210-M001		1 mg	330.00 USD

Product Specification

FORMULA:	C₂₈H₂₄N₄O₄
MW:	480.5
CAS NUMBER:	141196-69-2
SOURCE/HOST:	Isolated from Streptomyces sp. MST-AS5345.
PURITY:	≥98% (HPLC)
APPEARANCE:	Yellow solid.
SOLUBILITY:	Soluble in DMSO, dimethyl formamide, methanol or 100% ethanol; slightly soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Antibiotic. Potent inhibitor of protein kinase C (PKC). Inhibits the cell cycle at the G2 stage.

Product Specific Literature References

A new inhibitor of protein kinase C, RK-1409 (7-oxostaurosporine). I. Taxonomy and biological activity: H. Osada, et al.; J. Antibiot. 45, 189 (1992) Abstract
A new inhibitor of protein kinase C, RK-1409 (7-oxostaurosporine). II. Fermentation, isolation, physico-chemical properties and structure: H. Koshino, et al.; J. Antibiot. 45, 195 (1992) Abstract

Further Categories Containing This Product:

PKC Inhibitors • Cell Cycle Blockers & Inhibitors / Related Products • Staurosporine / Related Products • Antibiotics for Cell Cycle Research • Alkaloids

ALX-270-113

Revised 08-Apr-08

Phloretin
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-270-113-M100		100 mg	37.00 USD

Product Specification

FORMULA:	C₁₅H₁₄O₅
MW:	274.3
CAS NUMBER:	60-82-2
MERCK INDEX:	14: 7326
PURITY:	≥98%
APPEARANCE:	Off-white to beige solid.
SOLUBILITY:	Soluble in acetone, DMSO, 100% ethanol or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Flavonoid. Protein kinase C (PKC) inhibitor. PGF_2a receptor antagonist. In astrocytes, these receptors are linked to phospholipase C, thus affecting phosphoinositide hydrolysis and intracellular Ca²⁺ levels. Inhibits myo-inositol uptake and 5’-iodothyronine deiodinase. Prevents TNF-α stimulated upregulation of VCAM-1, ICAM-1 and E-selectin. Enhances adiponectin expression.

Product Specific Literature References

Effects on water diffusion of inhibitors affecting various transport processes in human red blood cells: G. Benga, et al.; Eur. J. Cell Biol. 59, 219 (1992) Abstract
Phloretin as an antagonist of prostaglandin F2 alpha receptor in cultured rat astrocytes: J. Kitanaka, et al.; J. Neurochem. 60, 704 (1993) Abstract
Characterization of the inhibition by stilbene disulphonates and phloretin of lactate and pyruvate transport into rat and guinea-pig cardiac myocytes suggests the presence of two kinetically distinct carriers in heart cells: X. Wang, et al.; Biochem. J. 290, 249 (1993) Abstract
The effect of glucose and galactose toxicity on myo-inositol transport and metabolism in human skin fibroblasts in culture: G.T. Berry, et al.; Pediat. Res. 35, 141 (1994) Abstract
Activating effect of the flavonoid phloretin on Ca(2+)-activated K+ channels in myelinated nerve fibers of Xenopus laevis: D.S. Koh, et al.; Neurosci. Lett. 165, 167 (1994) Abstract
Thyroid hormones in tissues from fetal and adult rats: G. Morreale de Escobar; Endocrinology 134, 2410 (1994) Abstract
Gonadotropin-releasing hormone induced Ca2+ influx in nonsecreting pituitary adenoma cells: role of voltage-dependent Ca2+ channels and protein kinase C: N. Prevarskaya, et al.; Mol. Cell. Neurosci. 5, 699 (1994) Abstract
The flavonoid phloretin suppresses stimulated expression of endothelial adhesion molecules and reduces activation of human platelets: V. Stangl, et al.; J. Nutr. 135, 172 (2005) Abstract
Phloretin enhances adipocyte differentiation and adiponectin expression in 3T3-L1 cells: M. Hassan, et al.; BBRC 361, 208 (2007) Abstract

Further Categories Containing This Product:

Adiponectin [ACRP30] / Related Products • Adhesion Molecules & Receptors Other Products • PKC Inhibitors • Active Substances from Fruit and Vegetables

ALX-380-281

Revised 20-Jun-08

PKC412
SYNONYMS	4’-N-Benzoyl-staurosporine Midostaurin CGP 41251
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-380-281-M001		1 mg	60.00 USD
ALX-380-281-M005		5 mg	240.00 USD

Product Specification

FORMULA:	C₃₅H₃₀N₄O₄
MW:	570.6
CAS NUMBER:	120685-11-2
MERCK INDEX:	14: 6185
SOURCE/HOST:	Semisynthetic product prepared from staurosporine (a fermentation product of Streptomyces staurosporeus) (Prod. No. ALX-380-014).
PURITY:	≥96% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in DMSO (10mg/ml), MDC (10mg/ml) or methanol (5mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Inhibitor of a variety of serine/threonine and tyrosine kinases, like protein kinase C (PKC), cyclic AMP-dependent protein kinase (PKA), S6 kinase, Akt (protein kinase B; PKB) and epidermal growth factor receptor (EGFR) tyrosine kinase activity. Potently inhibits FLT-3 kinase in vitro and in vivo. Apoptosis inducer. Showed broad antiproliferative activity against various tumor cell lines. Selectively inhibits T lymphocyte production of TNF-α. Upregulates endothelial nitric oxide synthase (eNOS; NOS III).

Product Specific Literature References

Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251: E. Andrejauskas-Buchdunger & U. Regenass; Cancer Res. 52, 5353 (1992) Abstract; Full Text
Analogs of staurosporine: potential anticancer drugs?: A. Gescher; Gen. Pharmacol. 31, 721 (1998), (Review) Abstract
Differential effects of UCN-01, staurosporine and CGP 41 251 on cell cycle progression and CDC2/cyclin B1 regulation in A431 cells synchronized at M phase by nocodazole: T. Akiyama, et al.; Anticancer Drugs 10, 67 (1999) Abstract
Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent: D. Fabbro, et al.; Pharmacol. Ther. 82, 293 (1999) Abstract
The phosphatidylinositide 3’-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C: A. Tenzer, et al.; Cancer Res. 61, 8203 (2001) Abstract; Full Text
Phase I and pharmacokinetic study of PKC412, an inhibitor of protein kinase C: D.J. Propper, et al.; J. Clin. Oncol. 19, 1485 (2001) Abstract; Full Text
A protein kinase C inhibitor induces phenotypic reversion of ras-transformed pancreatic cancer cells and cooperatively blocks tumor cell proliferation with an anti- ras peptide.: D. Way, et al.; Cancer Chemother. Pharmacol. 49, 429 (2002) Abstract
Protein kinase C inhibitors: H.C. Swannie & S.B. Kaye; Curr. Oncol. Rep. 4, 37 (2002), (Review) Abstract
PKC412 inhibits the zinc finger 198-fibroblast growth factor receptor 1 fusion tyrosine kinase and is active in treatment of stem cell myeloproliferative disorder: J. Chen, et al.; PNAS 101, 14479 (2004) Abstract; Full Text
Cotreatment with 17-allylamino-demethoxygeldanamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3: P. George, et al.; Cancer Res. 64, 3645 (2004) Abstract; Full Text
Effects of the kinase inhibitor CGP41251 (PKC 412) on lymphocyte activation and TNF-alpha production: M.S. Si, et al.; Int. Immunopharmacol. 5, 1141 (2005) Abstract
N-Benzoylstaurosporine (PKC412) inhibits Akt kinase inducing apoptosis in multiple myeloma cells.: N.J. Bahlis, et al.; Leuk. Lymphoma 46, 899 (2005) Abstract
Midostaurin upregulates eNOS gene expression and preserves eNOS function in the microcirculation of the mouse: H. Li, et al.; Nitric Oxide 12, 231 (2005) Abstract
Inhibitors of the PI3-kinase/Akt pathway induce mitotic catastrophe in non-small cell lung cancer cells: T.H. Hemström, et al.; Int. J. Cancer 119, 1028 (2006) Abstract
Antitumor and normal cell protective effect of PKC412 in the athymic mouse model of ovarian cancer: M. Kim, et al.; Ann. Clin. Lab. Sci. 36, 455 (2006) Abstract
PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects.: K.V. Gleixner, et al.; Blood 107, 752 (2006) Abstract; Full Text
Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT: K.V. Gleixner, et al.; Haematologica 92, 1451 (2007) Abstract; Full Text
PKC 412 small-molecule tyrosine kinase inhibitor: single-compound therapy for pancreatic cancer: J. El Fitori, et al.; Cancer 110, 1457 (2007) Abstract
PKC412 (CGP41251) modulates the proliferation and lipopolysaccharide-induced inflammatory responses of RAW 264.7 macrophages: K. Miyatake, et al.; BBRC 360, 115 (2007) Abstract
Divergent cytotoxic effects of PKC412 in combination with conventional antileukemic agents in FLT3 mutation-positive versus -negative leukemia cell lines.: Y. Furukawa, et al.; Leukemia 21, 1005 (2007) Abstract
PKC412 demonstrates JNK-dependent activity against human multiple myeloma cells: J. Sharkey, et al.; Blood 109, 1712 (2007) Abstract
The FLT3 inhibitor PKC412 exerts differential cell cycle effects on leukemic cells depending on the presence of FLT3 mutations: T. Odgerel, et al.; Oncogene 27, 3102 (2008) Abstract
The FLT3 inhibitor PKC412 in combination with cytostatic drugs in vitro in acute myeloid leukemia: L. Möllgard, et al.; Cancer Chemother. Pharmacol. 62, 439 (2008) Abstract

SEQUENCE:	Myr-Ser-Ile-Tyr-Arg-Arg-Gly-Ala-Arg-Arg-Trp-Arg-Lys-Leu-OH
FORMULA:	C₉₀H₁₅₄N₃₀O₁₇
MW:	1928.4
PEPTIDE CONTENT:	≥60%
PURITY:	≥95% (HPLC)
APPEARANCE:	White to off-white powder.
FORMULATION:	Counter Ion: TFA
SOLUBILITY:	Soluble in water or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

CAS NUMBER:	1405-20-5
MERCK INDEX:	14: 7573
RTECS:	TR1150000
SOURCE/HOST:	Isolated from Bacillus polymyxa.
APPEARANCE:	White to off-white powder.
PURITY DETAIL:	Mixture of Polymyxin B1, B2, B3 and B1-I.
SOLUBILITY:	Soluble in water.
ACTIVITY:	≥6000U/mg.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	HARMFUL.
Polymyxin B₁