ALEXIS Biochemicals: K-252b

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ALX-270-016

Revised 05-May-08

H-7 . dihydrochloride
SYNONYMS	(±)-1-(5-Isoquinolinesulfonyl)-2-methylpiperazine . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-016-M010		10 mg	60.00 USD
ALX-270-016-M025		25 mg	120.00 USD

Product Specification

FORMULA:	C₁₄H₁₇N₃O₂S . 2 HCl
MW:	291.4 . 73.0
CAS NUMBER:	108930-17-2
PURITY:	≥98%
APPEARANCE:	White to light yellow solid.
SOLUBILITY:	Soluble in water, 100% ethanol or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Inhibitor of protein kinase C (PKC), cAMP- and cGMP-dependent protein kinase (PKA and PKG). Also inhibits myosin light chain kinase. Induces apoptotic DNA fragmentation and cell death. Inhibits telomerase activity in treated NPC-076 cells.

Product Specific Literature References

1-(5-Isoquinolinesulfonyl)-2-methylpiperazine (H-7) is a selective inhibitor of protein kinase C in rabbit platelets: S. Kawamoto & H. Hidaka; BBRC 125, 258 (1984) Abstract
Stimulus-dependent inhibition of platelet aggregation by the protein kinase C inhibitors polymyxin B, H-7 and staurosporine: C. Schächtele, et al.; BBRC 151, 542 (1988) Abstract
Blockade of the spinal excitatory effect of cAMP on the startle reflex by intrathecal administration of the isoquinoline sulfonamide H-8: comparison to the protein kinase C inhibitor H-7: N.M. Boulis & M. Davis; Brain Res. 525, 198 (1990) Abstract
Potent selective inhibition of 7-O-methyl UCN-01 against protein kinase C: I. Takahashi, et al.; J. Pharmacol. Exp. Ther. 255, 1218 (1990) Abstract
The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source: J. Quick, et al.; BBRC 187, 657 (1992) Abstract
Modulation of neutrophil superoxide generation by inhibitors of protein kinase C, calmodulin, diacylglycerol and myosin light chain kinases, and peptidyl prolyl cis-trans isomerase: H. Bergstrand, et al.; J. Pharmacol. Exp. Ther. 263, 1334 (1992) Abstract
C. Gimond and M. Aumailley; Exp. Cell Res. 203, 365 (1992) 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
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
Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture: W.C. Ku, et al.; Biochem. Biophys. Res. Commun. 241, 730 (1997) Abstract

Further Categories Containing This Product:

Myosin Light Chain Kinase Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products • PKA Inhibitors

ALX-270-017

Revised 27-Apr-06

H-89 . dihydrochloride
SYNONYMS	N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKA Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-017-M001		1 mg	22.00 USD
ALX-270-017-M005		5 mg	55.00 USD

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 • Casein Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products

ALX-270-039

Revised 15-Nov-06

A-3 . hydrochloride
SYNONYMS	N-(2-Aminoethyl)-5-chloronaphthalene-1-sulfonamide . HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKA Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-039-M010		10 mg	65.00 USD
ALX-270-039-M050		50 mg	260.00 USD

Product Specification

FORMULA:	C₁₂H₁₃ClN₂O₂S . HCl
MW:	284.8 . 36.5
PURITY:	≥98%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO or 100% ethanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Inhibitor of cAMP- and cGMP-dependent protein kinase (PKA and PKG), protein kinase C (PKC), casein kinase I and II, and myosin light chain kinase.

Product Specific Literature References

Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors: M. Inagaki, et al.; Mol. Pharmacol. 29, 577 (1986) Abstract

Further Categories Containing This Product:

Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • Casein Kinase Inhibitors • PKG Inhibitors

ALX-270-067

Revised 04-Mar-05

H-8 . dihydrochloride
SYNONYMS	N-[2-(Methylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKA Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-067-M005		5 mg	40.00 USD
ALX-270-067-M025		25 mg	160.00 USD

Product Specification

FORMULA:	C₁₂H₁₅N₃O₂S . 2HCl
MW:	265.3 . 73.0
CAS NUMBER:	113276-94-1
PURITY:	≥98%
APPEARANCE:	White crystalline solid.
SOLUBILITY:	Soluble in water or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C

Product Description

Potent inhibitor of cAMP- and cGMP-dependent protein kinases (PKA and PKG). Also inhibits myosin light chain kinase.

Product Specific Literature References

Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C: H. Hidaka, et al.; Biochemistry 23, 5036 (1984) Abstract
Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors: M. Inagaki, et al.; Mol. Pharmacol. 29, 577 (1986) Abstract
Specific binding of a novel compound, N-[2-(methylamino)ethyl]-5- isoquinolinesulfonamide (H-8) to the active site of cAMP-dependent protein kinase: M. Hagiwara, et al.; Mol. Pharmacol. 31, 523 (1987) Abstract
Selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives: M. Hagiwara, et al.; Mol. Pharmacol. 32, 7 (1987) Abstract
Differential growth inhibition of isoquinolinesulfonamides H-8 and H-7 towards multidrug-resistant P388 murine leukaemia cells: M. Ido, et al.; Br. J. Cancer 64, 1103 (1991) 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

Further Categories Containing This Product:

Myosin Light Chain Kinase Inhibitors • PKG Inhibitors

ALX-270-069

Revised 04-Feb-05

HA-100 . dihydrochloride
SYNONYMS	1-(5-Isoquinolinylsulfonyl)piperazine . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	PKA Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-069-M005		5 mg	40.00 USD

Product Specification

FORMULA:	C₁₃H₁₅N₃O₂S . 2HCl
MW:	277.3 . 73.0
CAS NUMBER:	84468-24-6
PURITY:	≥99%
APPEARANCE:	Lyophilized solid.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C

Product Description

Inhibitor of myosin light chain kinase, cAMP-dependent protein kinase (PKA) and protein kinase C (PKC).

Product Specific Literature References

Role of protein kinases in stimulation of human polymorphonuclear leukocyte oxidative metabolism by various agonists. Differential effects of a novel protein kinase inhibitor: C. Gerard, et al.; J. Clin. Invest. 77, 61 (1986) Abstract
Selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives: M. Hagiwara, et al.; Mol. Pharmacol. 32, 7 (1987) Abstract

Further Categories Containing This Product:

Myosin Light Chain Kinase Inhibitors • PKC Inhibitors

ALX-270-071

Revised 06-Aug-07

HA-1077 . dihydrochloride
SYNONYMS	Fasudil 1-(5-Isoquinolinesulfonyl)homopiperazine . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Rho-associated Protein Kinases [ROCK]/Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-071-M001		1 mg	21.00 USD
ALX-270-071-M005		5 mg	63.00 USD

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-270-084

Revised 28-Jan-05

ML-9 . hydrochloride
SYNONYMS	1-(5-Chloronaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine . HCl
PRODUCT LINE	Neurobiology
PRODUCT CATEGORY	Myelin Basic Protein/Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-084-M010		10 mg	65.00 USD
ALX-270-084-M025		25 mg	125.00 USD

Product Specification

FORMULA:	C₁₅H₁₇ClN₂O₂S . HCl
MW:	324.8 . 36.5
CAS NUMBER:	105637-50-1
PURITY:	≥98%
APPEARANCE:	White solid.
SOLUBILITY:	Soluble in water or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Inhibitor of myosin light chain kinase, protein kinase C (PKC) and protein cAMP-dependent protein kinase (PKA). Also inhibits catecholamine secretion in intact and permeabilized chromaffin cells.

Product Specific Literature References

The modulatory role of myosin light chain phosphorylation in human platelet activation [published erratum appears in Biochem Biophys Res Commun 1987 Jan 15;142(1):287]: M. Saitoh, et al.; BBRC 140, 280 (1986) Abstract
Effects of myosin light-chain kinase inhibitor on catecholamine secretion from rat pheochromocytoma PC12h cells: T. Nagatsu, et al.; BBRC 143, 1045 (1987) Abstract
Selective inhibition of catalytic activity of smooth muscle myosin light chain kinase: M. Saitoh, et al.; J. Biol. Chem. 262, 7796 (1987) Abstract; Full Text
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
Naphthalenesulfonamide derivatives ML9 and W7 inhibit catecholamine secretion in intact and permeabilized chromaffin cells: J.A. Reig, et al.; Neurochem. Res. 18, 317 (1993) Abstract

Further Categories Containing This Product:

Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKA Inhibitors

ALX-270-088

Revised 07-Apr-05

ML-7 . hydrochloride
SYNONYMS	1-(5-Iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine . HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Tyrosine Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-088-M005		5 mg	40.00 USD
ALX-270-088-M025		25 mg	160.00 USD

Product Specification

FORMULA:	C₁₅H₁₇IN₂O₂S . HCl
MW:	416.0 . 36.5
CAS NUMBER:	110448-33-4
PURITY:	≥98%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO (can be further diluted with water), 100% ethanol (warm) or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Inhibits smooth-muscle myosin light chain kinase, protein kinase C (PKC), and cAMP-dependent protein kinase (PKA).

Product Specific Literature References

Selective inhibition of catalytic activity of smooth muscle myosin light chain kinase: M. Saitoh, et al.; J. Biol. Chem. 262, 7796 (1987) Abstract; Full Text

Further Categories Containing This Product:

Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKA Inhibitors

ALX-270-151

Revised 10-May-05

W-5 . hydrochloride
SYNONYMS	N-(6-Aminohexyl)-1-naphthalenesulfonamide . HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Calmodulin Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-151-M005		5 mg	20.00 USD
ALX-270-151-M025		25 mg	60.00 USD

Product Specification

FORMULA:	C₁₆H₂₂N₂O₂S . HCl
MW:	306.4 . 36.5
CAS NUMBER:	61714-25-8
PURITY:	≥98%
APPEARANCE:	White to off-white crystalline solid.
SOLUBILITY:	Soluble in water, DMSO, 100% ethanol (hot) or methanol (hot).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stable for at least 3 years when stored at -20°C. Stock solutions are stable for up to 6 months when stored at +4°C.
HANDLING:	Protect from light.

Product Description

Antagonist of calmodulin, inhibiting Ca²⁺/calmodulin-regulated phosphodiesterase (PDE I) and myosin light chain kinase.

Product Specific Literature References

Hydrophobic regions function in calmodulin-enzyme(s) interactions: T. Tanaka & H. Hidaka; J. Biol. Chem. 255, 11078 (1980) Abstrac