ALEXIS Biochemicals: Oligomycin C

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Antibiotics - ATPase Inhibitors

Antibiotics - NF-kB Inhibitors

Antibiotics - Protein Kinase Inhibitors

Staurosporine / Related Products

Antibiotics - Other Signal Transduction Pathway Modulators

ALX-380-054

Revised 18-Jun-08

Geldanamycin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-054-C100		100 µg	28.00 USD
ALX-380-054-C500		500 µg	50.00 USD
ALX-380-054-M001		1 mg	75.00 USD
ALX-380-054-M005		5 mg	300.00 USD

Product Specification

FORMULA:	C₂₉H₄₀N₂O₉
MW:	560.6
CAS NUMBER:	30562-34-6
RTECS:	LX8920000
SOURCE/HOST:	Isolated from Streptomyces hygroscopicus.
PURITY:	≥96%
APPEARANCE:	Yellow solid.
SOLUBILITY:	Slightly soluble in methanol, chloroform or DMSO; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Potent antitumor antibiotic. Inhibitor of pp60^src tyrosine kinase and of c-myc gene expression in murine lymphoblastoma cells. Inhibits the transforming activity of abl, erbB, fps, src, and yes. Binds specifically to heat shock protein 90 (HSP90) and to its endoplasmic reticulum homolog GP96 (GRP94). Capable of destabilizing several oncogene and proto-oncogene products. Potent inhibitor of the nuclear hormone receptor family. Protects against α-synuclein toxicity to dopaminergic neurons in Drosophila. Destabilizes mutant p53 protein from a number of breast, leukemic, and prostate cell lines. Inhibits basal and hypoxia-induced expression of c-Jun (IC₅₀=75nM) and abolishes hypoxia-induced increase in c-Jun N-terminal kinase (JNK) activity. Inhibits telomerase activity through inhibition of HSP90, a chaperone required for the assembly and activation of telomerase in human cells. ~10-fold more potent than herbimycin A (Prod. No. ALX-350-029)

Product Specific Literature References

Geldanamycin, a new antibiotic: C. DeBoer, et al.; J. Antibiot. 23, 442 (1970) Abstract
Phenotypic change from transformed to normal induced by benzoquinonoid ansamycins accompanies inactivation of p60src in rat kidney cells infected with Rous sarcoma virus: Y. Uehara, et al.; Mol. Cell. Biol. 6, 2198 (1986) Abstract
Inhibition of c-myc gene expression in murine lymphoblastoma cells by geldanamycin and herbimycin, antibiotics of benzoquinoid ansamycin group: H. Yamaki, et al.; J.Antibiot. 42, 604 (1989) 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
Geldanamycin selectively destabilizes and conformationally alters mutated p53: M.V. Blagosklonny, et al.; Oncogene 11, 933 (1995) Abstract
Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives: R.C. Schnur, et al.; J. Med. Chem. 38, 3806 (1995) Abstract
p185erbB2 binds to GRP94 in vivo. Dissociation of the p185erbB2/GRP94 heterocomplex by benzoquinone ansamycins precedes depletion of p185erbB2: C. Chavany, et al.; J. Biol. Chem. 271, 4974 (1996) Abstract; Full Text
Stable and specific binding of heat shock protein 90 by geldanamycin disrupts glucocorticoid receptor function in intact cells: L. Whitesell & P. Cook; Mol. Endocrinol. 10, 705 (1996) Abstract
Geldanamycin as a potential anti-cancer agent: its molecular target and biochemical activity: L. Neckers, et al.; Invest. New Drugs 17, 361 (1999), (Review) Abstract
Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs: M.V. Blagosklonny; Leukemia 16, 455 (2002), (Review) Abstract
Pharmacological prevention of Parkinson disease in Drosophila: P.K. Auluck & N.M. Bonini; Nat. Med. 8, 1185 (2002) Abstract
Effects of geldanamycin on signaling through activator-protein 1 in hypoxic HT29 human colon adenocarcinoma cells: I.A. Vasilevskaya and P.J. O'Dwyer; Cancer Res. 59, 3935 (1999) Abstract
Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells: R. Villa, et al.; Carcinogenesis 24, 851 (2003) Abstract
Chaperoning oncogenes: HSP90 as a target of geldanamycin: L. Neckers; Handb. Exp. Pharmacol. 259 (2006), (Review) Abstract
Geldanamycin interferes with the 90-kDa heat shock protein, affecting lipopolysaccharide-mediated interleukin-1 expression and apoptosis within macrophages: H.Y. Hsu, et al.; Mol. Pharmacol. 71, 344 (2007) Abstract; Full Text
Relationship among ligand conformations in solution, in the solid state, and at the Hsp90 binding site: geldanamycin and radicicol: P. Thepchatri, et al.; JACS 129, 3127 (2007) Abstract
Inhibition of heat shock protein 90 impairs epidermal growth factor-mediated signaling in gastric cancer cells and reduces tumor growth and vascularization in vivo: S.A. Lang, et al.; Mol. Cancer Ther. 6, 1123 (2007) Abstract; Full Text
Geldanamycin, a heat-shock protein 90-binding agent, induces thymocyte apoptosis through destabilization of Lck in presence of 12-O-tetradecanoylphorbol 13-acetate: K. Ohta, et al.; Biomed. Res. 28, 33 (2007) Abstract; Full Text
Low dose geldanamycin inhibits hepatocyte growth factor and hypoxia-stimulated invasion of cancer cells: F. Koga, et al.; Cell Cycle 6, 1393 (2007) Abstract
The heat-shock protein 90 inhibitor, geldanamycin, induces apoptotic cell death in Epstein-Barr virus-positive NK/T-cell lymphoma by Akt down-regulation: Y.K. Jeon, et al.; J. Pathol. 213, 170 (2007) Abstract
Geldanamycin, a HSP90 inhibitor, attenuates the hypoxia-induced vascular endothelial growth factor expression in retinal pigment epithelium cells in vitro: W.C. Wu, et al.; Exp. Eye Res. 85, 721 (2007) Abstract
HSP90 antagonist, geldanamycin, inhibits proliferation, induces apoptosis and blocks migration of rhabdomyosarcoma cells in vitro and seeding into bone marrow in vivo: E. Lesko, et al.; Anticancer Drugs 18, 1173 (2007) Abstract
Geldanamycin enhances hepatocyte growth factor stimulation of eNOS phosphorylation in endothelial cells: K. Makondo, et al.; Eur. J. Pharmacol. 582, 110 (2007) Abstract
Hsp90-inhibitor geldanamycin abrogates G(2) arrest in p53-negative leukemia cell lines through the depletion of Chk1: K. Sugimoto, et al.; Oncogene 27, 3091 (2008) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • Chaperone-mediated Autophagy [CMA] • Antitumor Antibiotics • HSP90 / HtpG / Related Products • Antitumor Agents (DNA Interaction & Gene Regulation)

ALX-350-233

Revised 30-Oct-07

Gramicidin A (high purity)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Other Signal Transduction Pathway Modulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-233-M001		1 mg	25.00 USD
ALX-350-233-M005		5 mg	70.00 USD

Product Specification

SEQUENCE:	HCO-Val-Gly-Ala-D-Leu-Ala-D-Val-Val-D-Val-Trp-D-Leu-Trp-D-Leu-Trp-D-Leu-Trp-NHCH₂CH₂OH
FORMULA:	C₉₉H₁₄₀N₂₀O₁₇
MW:	1882.3
CAS NUMBER:	11029-61-01
MERCK INDEX:	14: 4532
SOURCE/HOST:	Isolated from Bacillus brevis.
PURITY:	≥95%
APPEARANCE:	Off-white solid.
PURITY DETAIL:	Contaminants: gB and gC isomers: <1% (HPLC).
SOLUBILITY:	Soluble in DMSO, in the lower alcohols or in acetic acid.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Naturally occurring ion channel forming pentadecapeptide. Causes K⁺/H⁺-exchange in mitochondria in a non-voltage dependent manner.

Product Specific Literature References

Purification of gramicidin A: C.J. Stankovic, et al.; Anal. Biochem. 184, 100 (1990) Abstract
The permeation properties of small organic cations in gramicidin A channels: S.A. Seoh & D. Busath; Biophys. J. 64, 1017 (1993) Abstract
Palmitoylation-induced conformational changes of specific side chains in the gramicidin transmembrane channel: R.E. Koeppe, 2nd, et al.; Biochemistry 34, 9299 (1995) Abstract
Two mechanisms of H+/OH- transport across phospholipid vesicular membrane facilitated by gramicidin A: B.S. Prabhananda & M.H. Kombrabail; Biophys. J. 71, 3091 (1996) Abstract
Effects of gramicidin-A on the adsorption of phospholipids to the air-water interface: S.C. Biswas, et al.; Biochim. Biophys. Acta 1717, 41 (2005) Abstract

Further Categories Containing This Product:

Peptides • K+ Channels Other Products

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-380-116

Revised 07-Apr-08

Hypothemycin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Antifungal

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-116-C250		250 µg	140.00 USD
ALX-380-116-M001		1 mg	420.00 USD

Product Specification

FORMULA:	C₁₉H₂₂O₈
MW:	378.4
CAS NUMBER:	76958-67-3
SOURCE/HOST:	Isolated from Phoma sp.
PURITY:	≥98% (HPLC)
APPEARANCE:	Off-white solid.
SOLUBILITY:	Soluble in DMSO or acetone; insoluble in methanol or water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Exhibits antifungal and cytotoxic activity against some tumor cell lines partly attributed to inhibition of Ras-inducible genes. Inhibits proliferation of mouse and human T cells and modulates production of cytokines during T cell activation. Facilitates the ubiquitinylation process of cyclin D1. Has been identified as a potent and selective inhibitor of threonine/tyrosine-specific kinase, MEK, and other protein kinases that contain a conserved cysteine residue in the ATP-binding site in both in vitro and in vivo studies.

Product Specific Literature References

Metabolites of pyrenomycetes XIII: Structure of (+) hypothemycin, an antibiotic macrolide from hypomyces trichothecoides: M.S.R. Nair & S.T. Carey; Tetrahedron Lett. 21, 2011 (1980)
Metabolites of pyrenomycetes. XIV: Structure and partial stereochemistry of the antibiotic macrolides hypothemycin and dihydrohypothemycin: M.S.R. Nair, et al.; Tetrahedron 37, 2445 (1981)
Revised structure and stereochemistry of hypothemycin: T. Agatsuma et al.; Chem. Pharm. Bull. 41, 373 (1993)
Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor: H. Tanaka, et al.; Jpn. J. Cancer Res. 90, 1139 (1999) Abstract
Hypothemycin inhibits the proliferative response and modulates the production of cytokines during T cell activation: R. Camacho, et al.; Immunopharmacology 44, 255 (1999) Abstract
Suppression of oncogenic transformation by hypothemycin associated with accelerated cyclin D1 degradation through ubiquitin-proteasome pathway: H. Sonoda, et al.; Life Sci. 65, 381 (1999) Abstract
Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK: A. Zhao, et al.; J. Antibiot. 52, 1086 (1999) Abstract
Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides: A. Schirmer, et al.; PNAS 103, 4234 (2006) Abstract; Full Text
Chemistry and biology of resorcylic acid lactones: N. Winssinger, et al.; Chem. Commun. (Camb). 1, 22 (2007), (Review) Abstract

Further Categories Containing This Product:

MAPK Pathway Inhibitors • Antitumor Antibiotics • Antibiotics - Protein Kinase Inhibitors • Tyrosine Kinase Inhibitors • Antitumor Agents (DNA Interaction & Gene Regulation) • Antibiotics - Proteasome / Ubiquitin Modulators • Ubiquitination Other Products • CDKs & Cyclins Other Products • Ras Signalling Pathway Other Products

ALX-380-103

Revised 17-Jun-08

K-252c
SYNONYMS	Staurosporinone Staurosporine Aglycone
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-103-M001		1 mg	80.00 USD
ALX-380-103-M005		5 mg	320.00 USD
ALX-380-103-M100		100 mg
ALX-380-103-M500		500 mg
ALX-380-103-G001		1 g

Product Specification

FORMULA:	C₂₀H₁₃N₃O
MW:	311.4
CAS NUMBER:	85753-43-1
PURITY:	≥95%
APPEARANCE:	Yellow crystalline solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Inhibitor of protein kinase C (PKC). Aglycone of staurosporine.

Product Specific Literature References

K-252b, c and d, potent inhibitors of protein kinase C from microbial origin: S. Nakanishi, et al.; J. Antibiot. 39, 1066 (1986) Abstract
The structures of the novel protein kinase C inhibitors K-252a, b, c and d: T. Yasuzawa, et al.; J. Antibiot. 39, 1072 (1986) Abstract
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989) Abstract
Synthesis of the Staurosporine aglycon: C.J. Moody & K.F. Rahimtoola; J. Org. Chem. 57, 2105 (1992)
Non-glycosidic/non-aminoalkyl-substituted indolocarbazoles as inhibitors of protein kinase C: J. Kleinschroth, et al.; Bioorg. Med. Chem. Lett. 3, 1959 (1993)
Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds: S. Fabre, et al.; Bioorg. Med. Chem. 1, 193 (1993) Abstract
Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976: G. Martiny-Baron, et al.; J. Biol. Chem. 268, 9194 (1993) Abstract
Oxidative cyclisations with palladium acetate. A short synthesis of staurosporine aglycone: W. Harris, et al.; Tetrahedron Lett. 34, 8361 (1993)
Staurosporine aglycone (K252-c) and arcyriaflavin A from the marine ascidian, Eudistoma sp: P.A. Horton, et al.; Experientia 50, 843 (1994) Abstract
A facile synthesis of staurosporine aglycone: G. Xie& J.W. Lown; Tetrahedron Lett. 35, 5555 (1994)
Staurosporine, a potentially important gift from a microorganism: S. Omura, et al.; J. Antibiot. 48, 535 (1995) Abstract
A General Approach to the Synthesis of Bisindolylmaleimides: Synthesis of Staurosporine Aglycone: M.M. Faul et al.; Synthesis 1511 (1995)
Design and implementation of an efficient synthesis approach to furanosylated indolocarbazoles: total synthesis of (+)- and (-)-K252a: J.L. Wood, et al.; J. Am. Chem. Soc. 119, 9641 (1997)
Advances in indolo[2,3-a]carbazole chemistry: design and synthesis of protein kinase C and topoisomerase I inhibitors: U. Pindur, et al.; Curr. Med. Chem. 6, 29 (1999) Abstract
Synthesis of pyrrolidin-2-ones and of Staurosporine aglycon (K-252c) by intermolecular Michael reaction: S. Mahboobi, et al.; J. Org. Chem. 64, 4697 (1999)
Kinase inhibitors: not just for kinases anymore: S.L. McGovern & B.K. Shoichet; J. Med. Chem. 46, 1478 (2003) Abstract
A short synthesis of staurosporinone (K-252c): S.P. Gaudencio; Tetrahedron Lett. 44, 2577 (2003)
Biological targets of antitumor indolocarbazoles bearing a sugar moiety: M. Prudhomme; Curr. Med. Chem. Anticancer Agents 4, 509 (2004) Abstract
Staurosporine and rebeccamycin aglycones are assembled by the oxidative action of StaP, StaC, and RebC on chromopyrrolic acid: A.R. Howard-Jones & C.T. Walsh; J. Am. Chem. Soc. 128, 12289 (2006) Abstract
Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a: R.L. Hudkins, et al.; J. Med. Chem. 50, 433 (2007) Abstract

General Information

BACKGROUND/TECHNICAL INFORMATION

Please also see our Product Flyer "K-252c - A Key Aglycone for Medicinal Chemistry".

Further Categories Containing This Product:

Staurosporine / Related Products • Alkaloids

ALX-380-027

Revised 09-May-08

K-252a
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-027-C100		100 µg	98.00 USD
ALX-380-027-C500		500 µg	290.00 USD
ALX-380-027-M001		1 mg	395.00 USD

Product Specification

FORMULA:	C₂₇H₂₁N₃O₅
MW:	467.5
CAS NUMBER:	97161-97-2
SOURCE/HOST:	Isolated from Nocardiopsis sp.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in DMSO, methanol or methylene chloride (5mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Alkaloid isolated from soil fungi. General, cell permeable protein kinase inhibitor. Potent inhibitor of Ca²⁺/calmodulin kinase II. Inhibits myosin light chain kinase, cAMP-dependent protein kinase (PKA), protein kinase C (PKC), and cGMP-dependent protein kinase (PKG). Induces apoptosis.

Product Specific Literature References

K-252a, a potent inhibitor of protein kinase C from microbial origin: H. Kase, et al.; J. Antibiot. (Tokyo) 39, 1059 (1986) Abstract
The structures of the novel protein kinase C inhibitors K-252a, b, c and d: T. Yasuzawa, et al.; J. Antibiot. (Tokyo) 39, 1072 (1986) Abstract
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989), (Review) Abstract
K252a is a potent and selective inhibitor of phosphorylase kinase: L.H. Elliott, et al.; BBRC 171, 148 (1990) Abstract
Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926: Y. Hashimoto, et al.; BBRC 181, 423 (1991) Abstract
Differentiation of PC12 cells with K-ras: comparison with nerve growth factor: D.L. Simpson, et al.; J. Neurosci. Res. 28, 486 (1991) Abstract
K-252a inhibits nerve growth factor-induced trk proto-oncogene tyrosine phosphorylation and kinase activity: M.M. Berg, et al.; J. Biol. Chem. 267, 13 (1992) Abstract; Full Text
K-252 compounds: modulators of neurotrophin signal transduction: B. Knusel & F. Hefti; J. Neurochem. 59, 1987 (1992) Abstract
pp42/44MAP kinase is a component of the neurogenic pathway utilized by nerve growth factor in PC12 cells: E.D. Lloyd & M.W. Wooten; J. Neurochem. 59, 1099 (1992) Abstract
K-252a and staurosporine selectively block autophosphorylation of neurotrophin receptors and neurotrophin-mediated responses: S.H. Nye, et al.; Mol. Biol. Cell 3, 677 (1992) Abstract
K-252a and staurosporine promote choline acetyltransferase activity in rat spinal cord cultures: M.C. Glicksman, et al.; J. Neurochem. 61, 210 (1993) Abstract
Staurosporine-related compounds, K252a and UCN-01, inhibit both cPKC and nPKC: K. Mizuno, et al.; FEBS Lett. 330, 114 (1993) Abstract
Ecto-protein kinase and surface protein phosphorylation in PC12 cells: interactions with nerve growth factor: Z. Pawlowska, et al.; J. Neurochem. 60, 678 (1993) Abstract
Staurosporine, K-252a, and K-252b stabilize calcium homeostasis and promote survival of CNS neurons in the absence of glucose: B. Cheng, et al.; J. Neurochem. 62, 1319 (1994) Abstract
K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996), Review Abstract

Further Categories Containing This Product:

CDK & Cyclin Inhibitors • PKA Inhibitors • CAM Kinase Inhibitors • PKG Inhibitors • Myosin Light Chain Kinase Inhibitors • Apoptosis Inducers & Inhibitors Other Products • Staurosporine / Related Products • Alkaloids

ALX-380-029

Revised 20-Feb-08

K-252b
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-029-C100		100 µg	98.00 USD
ALX-380-029-C500		500 µg	295.00 USD
ALX-380-029-M001		1 mg	420.00 USD

Product Specification

FORMULA:	C₂₆H₁₉N₃O₅
MW:	453.5
CAS NUMBER:	99570-78-2
SOURCE/HOST:	Isolated from Nocardiopsis sp.
PURITY:	≥98% (HPLC)
APPEARANCE:	Off-white to brown powder.
SOLUBILITY:	Soluble in DMSO, dimethyl formamide or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.