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346021

Glucokinase Activator, Cpd A

The Glucokinase Activator, Cpd A, also referenced under CAS 603108-44-7, modulates Glucokinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

Synonym(s):

Glucokinase Activator, Cpd A, Hexokinase D Activator, Hexokinase IV Activator, 2-Amino-5-(4-methyl-4H-(1,2,4)-triazole-3-yl-sulfanyl)-N-(4-methyl-thiazole-2-yl)benzamide, Compound A

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5 MG

CHF 183.00

CHF 183.00

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About This Item

Empirical Formula (Hill Notation):
C14H14N6OS2
CAS Number:
603108-44-7
Molecular Weight:
346.43
MDL number:
MFCD32690802
UNSPSC Code:
41121706
NACRES:
NA.77

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Quality Level

100

Assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

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This Item
550601171256382120
Glucokinase Activator, Cpd A The Glucokinase Activator, Cpd A, also referenced under CAS 603108-44-7, modulates Glucokinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

Sigma-Aldrich

346021

Glucokinase Activator, Cpd A

Pyruvate Kinase Activator The Pyruvate Kinase Activator controls the biological activity of Pyruvate Kinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

Sigma-Aldrich

550601

Pyruvate Kinase Activator

AMPK Activator The AMPK Activator, also referenced under CAS 849727-81-7, modulates the biological activity of AMPK. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

Sigma-Aldrich

171256

AMPK Activator

Histone Acetyltransferase Activator, CTB The Histone Acetyltransferase Activator, CTB, also referenced under CAS 451491-47-7, modulates the biological activity of Histone. This small molecule/inhibitor is primarily used for Cell Structure applications.

Sigma-Aldrich

382120

Histone Acetyltransferase Activator, CTB

form

solid

form

powder

form

solid

form

solid

assay

≥95% (HPLC)

assay

≥98% (HPLC)

assay

≥95% (HPLC)

assay

≥90% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

General description

A cell-permeable thiazolylamide glucokinase (GK; Hexokinase IV/D) activator that reversibly targets a allosteric site that is only exposed for binding in the glucose-bound GK conformation, but not in the unbound "super-open" GK conformation or the GKRP- (GK Regulatory Protein) bound GK, and effectively stabilizes GK in an active conformation as well as prevents its interaction with and nuclear sequestration by GKRP, while exhibiting little effect against Hexokinase I/II/III. Compound A is shown to activate GK activity in cell-free assays (EC50 = 0.42 and 0.14 µM in the presence of 2.5 mM and 10 mM of glucose, respectively) and effectively induce cellular GK activation and increase glucose metabolism both in in rats (10 to 30 mg/kg, p.o.) in vivo and in rat islets and hepatocytes cultures (10 to 30 µM) in vitro.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Iino, T., et al. 2009. Bioorg. Med. Chem. Lett.19, 5531.
Mitsuya, M., et al. 2009. Bioorg. Med. Chem. Lett.19, 2718.
Nishimura, T., et al. 2009. Bioorg. Med. Chem. Lett.19, In press.
Futamura, M., et al. 2006. J. Biol. Chem.281, 1357.
Kamata, K., et al. 2004. Structure12, 429.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Ryota Inoue et al.
iScience, 25(7), 104603-104603 (2022-07-09)
Uncoupling protein 2 (UCP2), a mitochondrial protein, is known to be upregulated in pancreatic islets of patients with type 2 diabetes (T2DM); however, the pathological significance of this increase in UCP2 expression is unclear. In this study, we highlight the
Sophie L Lewandowski et al.
Cell metabolism, 32(5), 736-750 (2020-11-05)
Pancreatic β cells couple nutrient metabolism with appropriate insulin secretion. Here, we show that pyruvate kinase (PK), which converts ADP and phosphoenolpyruvate (PEP) into ATP and pyruvate, underlies β cell sensing of both glycolytic and mitochondrial fuels. Plasma membrane-localized PK

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