© 2008 Alexis Corporation
You are here:
Product Lines
>
Signal Transduction
>
Kinases / Related Products
>
Serine / Threonine Kinases / Related Products
>
Myosin Light Chain Kinases / Related Products
> Myosin Light Chain Kinase Inhibitors
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:
C
12
H
13
ClN
2
O
2
S . 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:
PKC Inhibitors
•
PKG Inhibitors
•
Casein Kinase Inhibitors
•
Myosin Light Chain Kinase Inhibitors
ALX-350-325
Revised 25-Jun-07
Altenusin
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antibiotics - Antifungal
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-350-325-M001
1 mg
110.00 USD
ALX-350-325-M005
5 mg
380.00 USD
Product Specification
FORMULA:
C
15
H
14
O
6
MW:
290.3
CAS NUMBER:
31186-12-6
SOURCE/HOST:
Isolated from
Alternaria sp
.
PURITY:
≥97% (HPLC)
APPEARANCE:
Yellow to brown solid.
SOLUBILITY:
Soluble in DMSO or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
IDENTITY:
Identity determined by
1
H-NMR,
13
C-NMR and MS.
Product Description
Antifungal penicillide. Non-competitive, specific neutral sphingomyelinase (N-SMase) and strong pp60c-Src inhibitor. Inhibits cFMS receptor tyrosine kinase (CSF-1/m-CSF receptor tyrosine kinase) which is implicated in cancer and bone diseases. Myosin light chain kinase inhibitor. Exhibits anti-HIV-1 integrase activity.
Product Specific Literature References
Studies in the biochemistry of micro-organisms. 103. Metabolites of Alternaria tenuis Auct.: Culture filtrate products:
T. Rosett, et al.; Biochem. J.
67
, 390 (1957)
Full Text
Studies in the biosynthesis of fungal metabolites. 4. Alternariol monomethyl ether and its relation to other phenolic metabolites of Alternaria tenuis:
R. Thomas; Biochem. J.
80
, 234 (1961)
Abstract
;
Full Text
Metabolites of some Alternaria species. The structures of altenusin and dehydroaltenusin:
R. G. Coombe, et al.; Aus. J. Chem.
23
, 2343 (1970)
Host-specific toxins and chemical structures from alternaria species:
S. Nishimura, et al.; Ann. Rev. Phytopathol.
21
, 87 (1983)
The metabolites of Talaromycesflavus: Part 1. Metabolites of the organic extracts :
W. A. Ayer, et al.; Can. J. Chem.
68
, 2085 (1990)
Isolation of myosin light chain kinase inhibitors from microorganisms: dehydroaltenusin, altenusin, atrovenetinone, and cyclooctasulfur:
S. Nakanishi, et al.; Biosci. Biotechnol. Biochem.
59
, 1333 (1995)
Abstract
Alutenusin, a specific neutral sphingomyelinase inhibitor, produced by Penicillium sp. FO-7436:
R. Uchida, et al.; J. Antibiot.
52
, 572 (1999)
Abstract
Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites:
S.B. Singh, et al.; J. Ind. Microbiol. Biotechnol.
30
, 721 (2003)
Abstract
Fungal metabolites as potent protein kinase inhibitors: Identification of a novel metabolite and novel activities of known metabolites :
M. Oyama, et al.; Lett. Drug Design Discov.
1
, 24 (2004)
New penicillide derivatives isolated from Penicillium simplicissimum:
S. I. Komai, et al.; J. Nat. Med.
60
, 185 (2006)
HIV-1 integrase inhibitors: 2003-2004 update:
R. Dayam, et al.; Med. Res. Rev.
26
, 271 (2006)
Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
•
Myosin Light Chain Kinase Inhibitors
•
Antibiotics - Antiviral / Anti-HIV
ALX-350-027
Revised 19-Aug-08
Calphostin C
SYNONYMS
UCN-1028C
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-350-027-C100
100 µg
85.00 USD
ALX-350-027-M001
1 mg
595.00 USD
Product Specification
FORMULA:
C
44
H
38
O
14
MW:
790.8
CAS NUMBER:
121263-19-2
SOURCE/HOST:
Isolated from
Cladosporium cladosporioides
MST-FP1798.
PURITY:
≥95% (HPLC)
APPEARANCE:
Dark red solid.
SOLUBILITY:
Soluble in 100% ethanol, methanol, DMSO or dimethyl formamide; insoluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
USE/STABILITY:
Stock solutions are stable for 3 months when stored at -20°C.
HANDLING:
Protect from light.
Product Description
Potent and selective inhibitor of the protein kinase C (PKC) regulatory site of diacylglycerol and phorbol esters. At higher concentrations inhibits myosin light chain kinase, cAMP-dependent protein kinase, protein kinase G and pp60v-src protein tyrosine kinase. Induces apoptotic DNA fragmentation and cell death. Kills breast cancer cells. Has antiviral potential. Inhibits cardiac L-type Ca
2+
channels.
Product Specific Literature References
Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C:
E. Kobayashi, et al.; BBRC
159
, 548 (1989)
Abstract
Potent and specific inhibitors of protein kinase C of microbial origin:
T. Tamaoki and H. Nakano; Biotechnology
8
, 732 (1990)
Abstract
Inhibition of protein kinase C by calphostin C is light-dependent:
R.F. Bruns, et al.; BBRC
176
, 288 (1991)
Abstract
Irreversible oxidative inactivation of protein kinase C by photosensitive inhibitor calphostin C:
R. Gopalakrishna, et al.; FEBS Lett.
314
, 149 (1992)
Abstract
Calphostin C, a specific protein kinase C inhibitor, activates human neutrophils: effect on phospholipase A2 and aggregation:
S. Svetlov and S. Nigam; Biochim. Biophys. Acta
1177
, 75 (1993)
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
Growth inhibition of herpes simplex virus-type 1 in calphostin C-treated astrocytes:
C.G. Castagnino, et al.; Intervirology
38
, 332 (1995)
Abstract
Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels:
H.C. Hartzell & A. Rinderknecht; Am. J. Physiol.
270
, C1293 (1996)
Abstract
Pharmacokinetic features and metabolism of calphostin C, a naturally occurring perylenequinone with antileukemic activity:
C.L. Chen, et al.; Pharm. Res.
16
, 1003 (1999)
Abstract
Potent killing of paclitaxel- and doxorubicin-resistant breast cancer cells by calphostin C accompanied by cytoplasmic vacuolization:
B. Guo, et al.; Breast Cancer Res. Treat.
82
, 125 (2003)
Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
•
PKA Inhibitors
•
PKC Inhibitors
•
PKG Inhibitors
•
Myosin Light Chain Kinase Inhibitors
•
Ca2+ Channels (L-type)
•
Natural Products - Antiviral / anti-HIV Agents
•
Natural Products - Apoptosis Inducers & Inhibitors
•
Natural Products - Antitumor Reagents
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:
C
14
H
17
N
3
O
2
S . 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:
PKG Inhibitors
•
Apoptosis Inducers & Inhibitors Other Products
•
PKA Inhibitors
•
Myosin Light Chain Kinase 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:
C
12
H
15
N
3
O
2
S . 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:
PKG Inhibitors
•
Myosin Light Chain Kinase 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:
C
20
H
20
BrN
3
O
2
S . 2HCl
MW:
446.4 . 73.0
CAS NUMBER:
127243-85-0
PURITY:
≥97% (
1
H-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 Ca
2+
/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
•
PKC Inhibitors
•
PKG Inhibitors
•
Apoptosis Inducers & Inhibitors Other Products
•
Casein Kinase Inhibitors
•
Myosin Light Chain Kinase 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:
C
13
H
15
N
3
O
2
S . 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:
PKC Inhibitors
•
Myosin Light Chain Kinase 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:
C
14
H
17
N
3
O
2
S . 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 Ca
2+
/calmodulin-dependent protein kinase II. Inhibits translocation of PKCβI, PKCβII and PKCζ. Cell permeable Ca
2+
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-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:
C
27
H
21
N
3
O
5
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 Ca
2+
/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
•
Alkaloids
•
Staurosporine / Related Products
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