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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.

Product Description

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).

Product Specific Literature References

K-252b, c and d, potent inhibitors of protein kinase C from microbial origin: S. Nakanishi, et al.; J. Antibiot. (Tokyo) 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. Rüegg & G.M. Burgess; TIPS 10, 218 (1989), (Review) 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
K-252b selectively potentiates cellular actions and trk tyrosine phosphorylation mediated by neurotrophin-3: B. Knusel, et al.; J. Neurochem. 59, 715 (1992) Abstract
K-252 compounds: modulators of neurotrophin signal transduction: B. Knusel & F. Hefti; J. Neurochem. 59, 1987 (1992) 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

Further Categories Containing This Product:

PKA Inhibitors • CAM Kinase Inhibitors • PKG Inhibitors • Myosin Light Chain Kinase Inhibitors • Staurosporine / Related Products • Alkaloids

ALX-270-075

Revised 08-Oct-08

KT5720
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKA Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-075-C100		100 µg	110.00 USD
ALX-270-075-C500		500 µg	330.00 USD
ALX-270-075-M001		1 mg	590.00 USD

Product Specification

FORMULA:	C₃₂H₃₁N₃O₅
MW:	537.6
CAS NUMBER:	108068-98-0
SOURCE/HOST:	Semisynthetic.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in methanol (5mg/ml) or DMSO (1mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.

Product Description

Potent, reversible, cell permeable and selective inhibitor of cAMP-dependent protein kinase (PKA).

Product Specific Literature References

K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases: H. Kase, et al.; BBRC 142, 436 (1987) Abstract
Multiple kinase arrest points in the G1 phase of nontransformed mammalian cells are absent in transformed cells: D.M. Gadbois, et al.; PNAS 89, 8626 (1992) Abstract
Effects of selective inhibition of protein kinase C, cyclic AMP- dependent protein kinase, and Ca(2+)-calmodulin-dependent protein kinase on neurite development in cultured rat hippocampal neurons: L. Cabell and G. Audesirk; Int. J. Dev. Neurosci. 11, 357 (1993), (Review) Abstract

Further Categories Containing This Product:

Staurosporine / Related Products • Alkaloids

ALX-270-087

Revised 12-Mar-08

KT5823
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKG Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-087-C100		100 µg	110.00 USD
ALX-270-087-C500		500 µg	330.00 USD
ALX-270-087-M001		1 mg	590.00 USD

Product Specification

FORMULA:	C₂₉H₂₅N₃O₅
MW:	495.5
CAS NUMBER:	126643-37-6
SOURCE/HOST:	Semisynthetic.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO, dimethyl formamide or ethyl acetate.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.

Product Description

Potent and selective inhibitor of cGMP-dependent protein kinase (PKG).

Product Specific Literature References

K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases: H. Kase, et al.; BBRC 142, 436 (1987) Abstract

Further Categories Containing This Product:

Staurosporine / Related Products • Alkaloids

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-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