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CAM Kinase Inhibitors
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ALX-270-017 Revised 27-Apr-06
H-89 . dihydrochloride
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SYNONYMS N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-270-017-M001   1 mg 22.00 USD Add To Cart
ALX-270-017-M005   5 mg 55.00 USD Add To Cart
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Product Specification
FORMULA: C20H20BrN3O2S . 2HCl
MW: 446.4 . 73.0
CAS NUMBER: 127243-85-0
PURITY: ≥97% (1H-NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or methanol; also soluble in ethanol: water (1:1).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for at least 3-4 weeks when stored at +4°C. We recommend using a fresh solution each day.

Product Description
Cell permeable potent and selective inhibitor of cAMP- and cGMP-dependent protein kinases (PKA and PKG) and protein kinase Cµ (PKCµ). In contrast, most other protein kinase C (PKC) isotypes are much more weakly inhibited. Also inhibits Ca2+/calmodulin-dependent protein kinase II, casein kinase I and myosin light chain kinase. Induces apoptosis.
Product Specific Literature References
Polyamines differentially inhibit cyclic AMP-dependent protein kinase- mediated phosphorylation in the brain of the tobacco hornworm, Manduca sexta: W.L. Combest, et al.; J. Neurochem. 51, 1581 (1988) Abstract
Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5- isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma: T. Chijiwa, et al.; J. Biol. Chem. 265, 5267 (1990) Abstract; Full Text
A selective inhibitor of cyclic AMP-dependent protein kinase, N-[2- bromocinnamyl(amino)ethyl]-5-isoquinolinesulfonamide (H-89), inhibits phosphatidylcholine biosynthesis in HeLa cells: C.C. Geilen; FEBS Lett. 309, 381 (1992) Abstract
Protein kinase A inhibitors enhance radiation-induced apoptosis: D. Findik, et al.; J. Cell. Biochem. 57, 12 (1995) Abstract
Characterization of activators and inhibitors of protein kinase C mu: F.-J. Johannes, et al.; Eur. J. Biochem. 227, 303 (1995) Abstract
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity: R.A. Engh, et al.; J. Biol. Chem. 271, 26157 (1996) Abstract; Full Text
Stimulation of the ERK pathway by GTP-loaded Rap1 requires the concomitant activation of Ras, protein kinase C, and protein kinase A in neuronal cells: T. Bouschet, et al.; J. Biol. Chem. 278, 4778 (2003) Abstract; Full Text
Further Categories Containing This Product:
CAM Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products • Casein Kinase Inhibitors
 
 
ALX-270-066 Revised 07-Apr-08
Lavendustin C
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SYNONYMS Compound 5
5-(N-2,5-Dihydroxybenzyl)aminosalicylic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-270-066-M001   1 mg 35.00 USD Add To Cart
Product Specification
FORMULA: C14H13NO5
MW: 275.3
SOURCE/HOST: Synthetic.
PURITY: ≥97%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Potent inhibitor of protein tyrosine kinases and Ca2+/calmodulin-dependent kinase II. Acts also as an inhibitor of EGFR tyrosine kinase and pp60c-src kinase.
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
Long-term potentiation in the hippocampus is blocked by tyrosine kinase inhibitors: T.J. O'Dell, et al.; Nature 353, 558 (1991) Abstract
Hypericin and pseudohypericin specifically inhibit protein kinase C: possible relation to their antiretroviral activity: I. Takahashi, et al.; BBRC 165, 1207 (1989) Abstract
Inhibition of crystal-induced neutrophil activation by a protein tyrosine kinase inhibitor: H.M. Burt, et al.; J. Leukoc. Biol. 55, 112 (1994) Abstract
Endotoxin increases intercellular resistance in microvascular endothelial cells by a tyrosine kinase pathway: D. Lidington, et al.; J. Cell Physiol. 185, 117 (2000) Abstract
Related Products
Further Categories Containing This Product:
CAM Kinase Inhibitors • Tyrosine Kinase Inhibitors • EGFR Kinase Inhibitors • Lipopolysaccharides [LPS] / Related Products
 
 
ALX-270-071 Revised 06-Aug-07
HA-1077 . dihydrochloride
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SYNONYMS Fasudil
1-(5-Isoquinolinesulfonyl)homopiperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
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ALX-270-071-M001   1 mg 21.00 USD Add To Cart
ALX-270-071-M005   5 mg 63.00 USD Add To Cart
Product Specification
FORMULA: C14H17N3O2S . 2HCl
MW: 291.4 . 73.0
CAS NUMBER: 103745-39-7
MERCK INDEX: 14: 3942
PURITY: ≥98%
APPEARANCE: Lyophilized.
SOLUBILITY: Soluble in water, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of myosin light chain kinase and Ca2+/calmodulin-dependent protein kinase II. Inhibits translocation of PKCβI, PKCβII and PKCζ.  Cell permeable Ca2+ antagonist with antivasospastic properties.
Product Specific Literature References
The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs: O. Shibuya, et al.; Acta Neurochir. 90, 53 (1988) Abstract
Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase: T. Asano, et al.; Br. J. Pharmacol. 98, 1091 (1989) Abstract
Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator: Y. Sasaki & Y. Sasaki; BBRC 171, 1182 (1990) Abstract
Effects of HA1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle: M. Seto, et al.; Eur. J. Pharmacol. 195, 267 (1991) Abstract
A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture: M. Shirotani, et al.; J. Pharmacol. Exp. Ther. 259, 738 (1991) Abstract
Effects of isoquinoline derivatives, HA1077 and H-7, on cytosolic Ca2+ level and contraction in vascular smooth muscle: S. Takizawa, et al.; Eur. J. Pharmacol. 250, 431 (1993) Abstract
Rho kinase inhibitor HA-1077 prevents Rho-mediated myosin phosphatase inhibition in smooth muscle cells: H. Nagumo, et al.; Am. J. Physiol. Cell. Physiol. 278, C57 (2000) Abstract
Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCbetaI, PKCbetaII and PKCzeta in human neutrophils: X. Siomboing, et al.; Mediators Inflamm. 10, 315 (2001) Abstract
Effects of HA-1077 and Y-27632, Two Rho-Kinase Inhibitors, in the Human Umbilical Artery: M. Ark, et al.; Cell Biochem. Biophys. 41, 331 (2004) Abstract
Further Categories Containing This Product:
CAM Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors
 
 
ALX-270-477 Revised 19-Aug-08
STO-609
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SYNONYMS 7-Oxo-7H-benzimidazo[2,1-a]benz[de]isoquinoline-3-carboxylic acid acetic acid
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY CAM Kinase Inhibitors
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ALX-270-477-M001   1 mg 45.00 USD Add To Cart
Product Specification
FORMULA: C19H10N2O3 · CH3COOH
MW: 314.3 . 60.1
CAS NUMBER: 52029-86-4
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow to orange solid.
SOLUBILITY: Soluble in DMSO (10mg/ml; warm) or 100mM sodium hydroxide (20mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING: Protect from light. Hygroscopic.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Cell permeable, highly selective, potent and ATP-competitive inhibitor of CaM-KK (Ca2+/calmodulin-dependent protein kinase kinase) (IC50=120ng/ml and 40ng/ml for CaM-KKα and CaM-KKβ isoforms, respectively). Inhibits autophosphorylation through binding to the catalytic domain of CaM-KK.
Product Specific Literature References
STO-609, a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase: H. Tokumitsu, et al.; J. Biol. Chem. 277, 15813 (2002) Abstract; Full Text
A single amino acid difference between alpha and beta Ca2+/calmodulin-dependent protein kinase kinase dictates sensitivity to the specific inhibitor, STO-609: H. Tokumitsu, et al.; J. Biol. Chem. 278, 10908 (2003) Abstract; Full Text
Calmodulin-dependent kinase kinase/calmodulin kinase I activity gates extracellular-regulated kinase-dependent long-term potentiation: J.M. Schmitt, et al.; J. Neurosci. 25, 1281 (2005) Abstract; Full Text
The Ca2+/calmodulin-dependent protein kinase kinases are AMP-activated protein kinase kinases: R.L. Hurley, et al.; J. Biol. Chem 280, 29060 (2005) Abstract; Full Text
AMP-activated protein kinase mediates VEGF-stimulated endothelial NO production: J.A. Reihill, et al.; BBRC 354, 1084 (2007) Abstract; Full Text
Ca2+/calmodulin-dependent protein kinase kinase-alpha regulates skeletal muscle glucose uptake independent of AMP-activated protein kinase and Akt activation: C.A. Witczak, et al.; Diabetes 56, 1403 (2007) Abstract
Phosphatidylinositol ether lipid analogues induce AMP-activated protein kinase-dependent death in LKB1-mutant non small cell lung cancer cells: R.M. Memmott, et al.; Cancer Res. 68, 580 (2008) Abstract
Small molecule antagonizes autoinhibition and activates AMP-activated protein kinase in cells: T. Pang, et al.; J. Biol. Chem. 283, 16051 (2008) Abstract; Full Text
 
 
ALX-350-075 Revised 08-Apr-08
Rottlerin
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SYNONYMS Mallotoxin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-075-M010   10 mg 40.00 USD Add To Cart
ALX-350-075-M025   25 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C30H28O8
MW: 516.6
CAS NUMBER: 82-08-6
MERCK INDEX: 14: 8272
RTECS: AM6913800
SOURCE/HOST: Isolated from Mallotus philippinensis.
PURITY: ≥98% (HPLC)
APPEARANCE: Orange to brown solid.
SOLUBILITY: Soluble in DMSO, chloroform or 100% ethanol. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Mitochondrial uncoupler that depolarizes the mitochondrial membrane potential, reduces cellular ATP levels, activates 5‘-AMP-activated protein kinase (AMPK) and affects mitochondrial production of reactive oxygen species (ROS). Potent activator of multiple Ca2+-sensitive K+ channels. Blocks several kinases and non-kinase proteins in vitro. Has been widely-used as a selective inhibitor of protein kinase Cδ (PKCδ). However, recent studies indicate that rottlerin has no direct effect on PKCδ and that it should not be used to determine the involvement of PKCδ in biological processes.
Product Specific Literature References
The mouse ear edema: a quantitatively evaluable assay for tumor promoting compounds and for inhibitors of tumor promotion: M. Gschwendt, et al.; Cancer Lett. 25, 177 (1984) Abstract
Rottlerin, a novel protein kinase inhibitor: M. Gschwendt, et al.; BBRC 199, 93 (1994) Abstract
Elongation factor-2 kinase: effective inhibition by the novel protein kinase inhibitor rottlerin and relative insensitivity towards staurosporine: M. Gschwendt, et al.; FEBS Lett. 338, 85 (1994) Abstract
Rottlerin: an inappropriate and ineffective inhibitor of PKCdelta: S.P. Soltoff; TIPS 28, 453 (2007) Abstract
Further Categories Containing This Product:
PKA Inhibitors • CAM Kinase Inhibitors • Casein Kinase Inhibitors • PKC Inhibitors
 
 
ALX-380-027 Revised 09-May-08
K-252a
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-027-C100   100 µg 98.00 USD Add To Cart
ALX-380-027-C500   500 µg 290.00 USD Add To Cart
ALX-380-027-M001   1 mg 395.00 USD Add To Cart
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
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-029-C100   100 µg 98.00 USD Add To Cart
ALX-380-029-C500   500 µg 295.00 USD Add To Cart
ALX-380-029-M001   1 mg 420.00 USD Add To Cart
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-380-284 Revised 08-Apr-08
Cyclosporin D
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SYNONYMS Val2-cyclosporin
7-L-Valine-cyclosporin A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Immunomodulators
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ALX-380-284-M001   1 mg 80.00 USD Add To Cart
ALX-380-284-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C63H113N11O12
MW: 1216.6
CAS NUMBER: 63775-96-2
MERCK INDEX: 14: 2752
SOURCE/HOST: Isolated from Fusarium solani.
PURITY: ≥95% (HPLC)
APPEARANCE: Colorless to off-white crystalline solid.
SOLUBILITY: Soluble in 100% ethanol, acetone or ethyl acetate; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE TERATOGENIC. TOXIC. MAY BE CARCINOGENIC.

Product Description
Weak immunosuppressor. Potent inhibitor of tumor promoting phorbol ester TPA/PMA (Prod. No. ALX-445-004) in vivo. Potent inhibitor of Ca2+/calmodulin dependent EF-2 phosphorylation in vitro.
Product Specific Literature References
The weak immunosuppressant cyclosporine D as well as the immunologically inactive cyclosporine H are potent inhibitors in vivo of phorbol ester TPA-induced biological effects in mouse skin and of Ca2+/calmodulin dependent EF-2 phosphorylation in vitro: M. Gschwendt, et al.; BBRC 150, 545 (1988) Abstract
Further Categories Containing This Product:
MPTP [Mitochondrial Transition Pore] / Related Products • CAM Kinase Inhibitors
 
 
ALX-380-286 Revised 08-Apr-08
Cyclosporin H
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SYNONYMS Csh-cyclosporin
5-(N-Methyl-D-valine)-cyclosporin A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - I