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532606 5-Lipoxygenase Inhibitor, MK591 - CAS 147030-01-1 - Calbiochem

MK591; MK0591; 5-LOX inhibitor, 5- Lipoxygenase inhibitor, FLAP

5-Lipoxygenase Inhibitor, MK591 - CAS 147030-01-1 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: FLAP Inhibitor, MK591, sodium 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropanoate, L-686,708, MK-0591

Primary Target: FLAP
532606
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

CAS #Empirical Formula
147030-01-1C₃₄H₃₄ClN₂NaO₃S

Products

KatalógusszámCsomagolás Menny./csomag
5.32606.0001 Üvegpalack 5 mg
Description
OverviewA cell permeable, bioavailable, 2-indolealkanoic acid derived compound that acts as a highly potent and selective inhibitor of leukotriene biosynthesis (IC50 = 3.1 nM in intact human polymorphonuclear leukocytes). Shown to inhibit 5-lipoxygenase (5-LOX) activity in LNCaP prostate cancer cells by high-affinity binding to 5-lipoxygenase activating protein (FLAP; IC50 = 1.6 nM in a FLAP binding assay). Induces apoptosis in LNCaP cells without blocking PI 3 kinase-Akt or ERK activities. Also shown to induce rapid phosphorylation of c-Jun N-terminal Kinase (JNK) and indirectly block PKCε activity. Suppresses the deposition of Ab1-40 and Ab1-42 peptides in Tg2576 mice (~40 mg/kg/day in diet) with concomitant reduction in the levels of presenilin 1, nicastrin, APH-1 and Pen-2, but without affecting notch signaling. Exhibits desirable pharmacokinetic properties with tmax of 3.3 h and t1/2 = ~12 h.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number532606
Brand Family Calbiochem®
SynonymsFLAP Inhibitor, MK591, sodium 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropanoate, L-686,708, MK-0591
References
ReferencesChu, J., et al. 2012. J. Neuroinflamm. 9, 127.
Sarveswaran, S., et al. 2011. Bioch. Biophy. Acta. 1813, 2108.
Sarveswaran, S., et al. 2010. Cancer Lett. 291, 167.
Uematsu, T., et al. 1995. Br. J. Clin. Pharm. 40, 59.
Product Information
CAS number147030-01-1
FormWhite solid
Hill FormulaC₃₄H₃₄ClN₂NaO₃S
Chemical formulaC₃₄H₃₄ClN₂NaO₃S
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetFLAP
Primary Target IC<sub>50</sub>3.1 nM
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalógusszám GTIN
5.32606.0001 04055977240948

Documentation

5-Lipoxygenase Inhibitor, MK591 - CAS 147030-01-1 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Hivatkozások áttekintése
Chu, J., et al. 2012. J. Neuroinflamm. 9, 127.
Sarveswaran, S., et al. 2011. Bioch. Biophy. Acta. 1813, 2108.
Sarveswaran, S., et al. 2010. Cancer Lett. 291, 167.
Uematsu, T., et al. 1995. Br. J. Clin. Pharm. 40, 59.

Brochure

Title
NPI Flyer- Epigenetics and Nuclear Function Feature
New Products - Antibodies, Small Molecule, Inhibitors

Technical Info

Title
White Paper: Further considerations of antibody validation and usage.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision19-December-2014 JSW
SynonymsFLAP Inhibitor, MK591, sodium 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropanoate, L-686,708, MK-0591
DescriptionA cell permeable, bioavailable, 2-indolealkanoic acid derived compound that acts as a highly potent and selective inhibitor of leukotriene biosynthesis (IC50 = 3.1 nM in intact human polymorphonuclear leukocytes). Shown to inhibit 5-lipoxygenase (5-LOX) activity in LNCaP prostate cancer cells by high-affinity binding to 5-lipoxygenase activating protein (FLAP; IC50 = 1.6 nM in a FLAP binding assay). Induces apoptosis in LNCaP cells without blocking PI 3 kinase-Akt or ERK activities. Also shown to induce rapid phosphorylation of c-Jun N-terminal Kinase (JNK) and indirectly block PKCε activity. Suppresses the deposition of Ab1-40 and Ab1-42 peptides in Tg2576 mice (~40 mg/kg/day in diet) with concomitant reduction in the levels of presenilin 1, nicastrin, APH-1 and Pen-2, but without affecting notch signaling. Exhibits desirable pharmacokinetic properties with tmax of 3.3 h and t1/2 = ~12 h.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number147030-01-1
Chemical formulaC₃₄H₃₄ClN₂NaO₃S
Purity≥98% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesChu, J., et al. 2012. J. Neuroinflamm. 9, 127.
Sarveswaran, S., et al. 2011. Bioch. Biophy. Acta. 1813, 2108.
Sarveswaran, S., et al. 2010. Cancer Lett. 291, 167.
Uematsu, T., et al. 1995. Br. J. Clin. Pharm. 40, 59.